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1.
J Vector Borne Dis ; 49(3): 181-7, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23135014

RESUMO

BACKGROUND & OBJECTIVES: In the present study, Icon®Life net, a long-lasting polyethylene net, 100 denier and bursting strength of minimum 280 kpa incorporated with deltamethrin @ 65 mg/m2 was evaluated for its efficacy in reducing the density of malaria vector Anopheles culicifacies and impact on malaria prevalence in a malaria endemic area of District Gautam Budh Nagar, India. METHODS: Wash resistance of Icon®Life LLIN was determined up to 20 serial washings using An. culicifacies in cone bioassays under field conditions. Efficacy of Icon®Life LLIN was determined in the field in three sets of villages in District Gautam Budh Nagar (Uttar Pradesh), India, selected randomly for the intervention with Icon®Life LLIN, untreated nets and a control without any intervention for the period of August 2008-July 2009. Entomological and malariometric indices in all the three villages were compared during pre- and post-intervention periods for one year against An. culicifacies. A survey was also conducted in the village provided with Icon®Life LLIN to assessing the perception of community regarding acceptance of these nets by the community. RESULTS: In cone bioassays on Icon®Life LLIN with An. culicifacies, >95% knockdown within 1 h and 100% mortality after 24 h exposure were reported even after 20× serial washings under field conditions. Results of the field study revealed reduced entry rate, resting density and parity rate of An. culicifacies in the village with Icon®Life LLIN when compared to no net and untreated net villages. Number of malaria cases reported were less in the Icon®Life LLIN used villages when compared to other two villages. The community compliance and acceptance was high and no adverse health events were reported by the households using these nets. CONCLUSIONS: Icon®Life LLIN is an effective intervention for the control of An. culicifacies transmitted malaria in India. Long-term studies are indicated for the duration of effectiveness and to ascertain the epidemiological impact of the use of Icon®Life nets.


Assuntos
Anopheles/efeitos dos fármacos , Mosquiteiros Tratados com Inseticida/estatística & dados numéricos , Malária/prevenção & controle , Controle de Mosquitos/métodos , Animais , Anopheles/parasitologia , Feminino , Índia , Inseticidas/farmacologia , Malária/transmissão , Malation/farmacologia , Nitrilas/administração & dosagem , Nitrilas/química , Densidade Demográfica , Prevalência , Piretrinas/administração & dosagem , Piretrinas/química , Estações do Ano , Fatores de Tempo
2.
Indian J Med Res ; 133: 426-30, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21537097

RESUMO

BACKGROUND & OBJECTIVES: Repellents are commonly used personal protection measures to avoid mosquito bites. In the present study, Advanced Odomos cream (12% N, N-diethyl-benzamide) was tested for its efficacy against mosquitoes in comparison to DEET (N,N-diethyl-3-methyl benzamide). METHODS: Bioassays were conducted to assess the repellency of Advanced Odomos and DEET creams against Anopheles stephensi and Aedes aegypti. Their efficacy was tested on human volunteers applied with different concentrations of test creams ranging from 1 to 12 mg/cm 2 and by exposing them to mosquitoes at hourly intervals. Field evaluation was also carried out to test the duration of protection of the test creams against Anopheles and Aedes mosquitoes during whole night and day time collections, respectively on human volunteers. Mosquito collections were done using torch light and aspirator. RESULTS: Complete (100%) protection was achieved at 10 mg/cm 2 cream formulation of Advanced Odomos (1.2 mg a.i/cm 2 ) dose against An. stephensi and 12 mg/cm 2 (1.44 mg a.i./cm 2 ) against Ae. aegypti on human baits. There was no statistically significant differences in per cent protection against mosquito bites between Advanced Odomos and DEET cream (P>0.05) in respective doses. Complete protection up to 11 h was observed against Anopheles mosquitoes during whole night collections and up to 6 h against Ae. aegypti in day time collections. No adverse reactions such as itching, irritation, vomiting, nausea, etc. were reported by the volunteers. INTERPRETATION & CONCLUSIONS: Advanced Odomos cream applied at 10 mg/cm 2 concentration provided 100% protection from Anopheles mosquitoes up to 11 h whereas about 6 h protection was recorded against Ae. aegypti. The laboratory and field trials indicate that for longer protection against Anopheles mosquitoes 10 mg/cm 2 will be appropriate and in case of Ae. aegypti more than 10 mg/cm 2 application is required for complete protection. In conclusion, the Advanced Odomos cream was comparable to the known repellent cream DEET for prolonged protection against malaria and dengue vectors.


Assuntos
Culicidae , DEET/análogos & derivados , Mordeduras e Picadas de Insetos/prevenção & controle , Repelentes de Insetos/administração & dosagem , Insetos Vetores , Administração Tópica , Aedes , Animais , Anopheles , DEET/administração & dosagem , Humanos
3.
J Am Mosq Control Assoc ; 27(4): 423-8, 2011 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-22329276

RESUMO

Long-lasting insecticidal nets (LLIN) have been developed for wash resistance and long-lasting effects against mosquito vectors. In this study we evaluated 2 LLIN products, Olyset net and Permanet 2.0, washed for 0, 5, 10, 15, and 20 times, against Anopheles stephensi, an urban malaria vector in India. We assessed the wash resistance and efficacy of these nets in relation to bloodfeeding inhibition and percent mortality in cone and tunnel test bioassays. Both Olyset and Permanet showed >80% mortality of An. stephensi in cone bioassays after 20 washes. In tunnel tests there was no significant difference between Olyset and Permanet 2.0 in causing total mosquito mortality (immediate and delayed) up to 10 washes and bloodfeeding inhibition and entry rate up to 15 washes. After the 20th wash, Permanet 2.0 was significantly more effective than the Olyset net in causing total mosquito mortality, whereas Olyset net showed less bloodfeeding and entry of mosquitoes as compared to Permanet 2.0. There was a gradual decline in efficacy of both LLIN products as the number of washings increased. Cone bioassays indicated a strong wash resistance in both the LLIN products after 20 washes. However, the tunnel tests demonstrated a gradual decline in efficacy of both products with the number of washings.


Assuntos
Anopheles/efeitos dos fármacos , Mosquiteiros Tratados com Inseticida , Lavanderia , Nitrilas/farmacologia , Permetrina/farmacologia , Piretrinas/farmacologia , Animais , Comportamento Alimentar , Índia , Inseticidas/química , Inseticidas/farmacologia , Nitrilas/química , Permetrina/química , Piretrinas/química
4.
J Vector Borne Dis ; 48(3): 138-43, 2011 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21946712

RESUMO

BACKGROUND & OBJECTIVES: Prevention of malaria is a major technical and operational problem in displaced and mobile populations such as refugee camps and temporary labour settlements. Insecticide incorporated plastic sheeting is a new technology to control mosquitoes in emergency shelters and also temporary habitations at different locations. In view of this, efficacy of ZeroFly® , an insecticide incorporated plastic sheeting (factory treated with deltamethrin 2.0 g/kg or 265 mg/m2 ) was evaluated for its efficacy against malaria vectors and its impact on malaria incidence in temporary labour settlements in two urban areas in India. METHODS: This trial was conducted in two labour settlements in two urban areas, Delhi and Noida (U.P.), India with ~ 250 populations. In an area, two localities were selected for intervention with ZeroFly and untreated plastic sheets (control). Entomological and epidemiological data were collected using standard methods for one year. RESULTS: Baseline studies on the susceptibility of mosquitoes in Delhi and Noida areas revealed 100% susceptibility of the malaria vector species Anopheles culicifacies and An. stephensi to deltamethrin. Cone bioassay tests performed against An. culicifacies and An. stephensi to determine the efficacy of ZeroFly sheets showed 100% mortality against An. culicifacies and An. stephensi with 3 min exposure and after 24 h recovery period. Against Culex quinquefasciatus and housefly 100% mortality was obtained after 30 min of exposure period. Intervention with the ZeroFly plastic sheets resulted in almost complete reduction in the resting density of An. culicifacies and An. stephensi, the two major malaria vectors and also in the reduction of malaria cases in ZeroFly camps as compared to control camps. The ZeroFly plastic sheeting was found to be safe for human. Barring some complaints of skin irritation and itching, which were temporary in nature, no adverse health effects were reported by the users. The community acceptance was high. CONCLUSION: Results of the present study revealed that ZeroFly® plastic sheeting is highly effective in reducing the indoor resting density of mosquitoes, man -vector contact and malaria incidences in labour populations living in temporary shelters.


Assuntos
Anopheles/efeitos dos fármacos , Roupas de Cama, Mesa e Banho , Culex/efeitos dos fármacos , Controle de Insetos/métodos , Inseticidas/farmacologia , Malária/epidemiologia , Animais , Anopheles/crescimento & desenvolvimento , Culex/crescimento & desenvolvimento , Feminino , Humanos , Incidência , Índia/epidemiologia , Malária/prevenção & controle , Masculino
5.
J Vector Borne Dis ; 47(4): 243-8, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21178218

RESUMO

BACKGROUND & OBJECTIVES: Long-lasting insecticidal nets (LLINs) have been introduced in India recently into the vector control programme. A study was undertaken to assess the community perception regarding use of LLIN, their acceptability, collateral benefits, etc. in certain villages of District Gautam Budh Nagar, Uttar Pradesh, India where LLINs are in use by the community. METHOD: A randomized community-based survey was undertaken during April- May 2009 covering 596 respondents in LLIN villages where LLINs have been distributed along with 307 respondents in untreated net villages where untreated nets were distributed using structured questionnaire. Qualitative data were collected and the difference in proportion was calculated by z-test. RESULTS: A substantial number of respondents had good knowledge of the symptoms of malaria. According to respondents, LLINs were very much effective in bringing down the malaria incidence in their families. About 98.3% of the respondents asserted the use of LLINs as their use not only reduced the number of mosquitoes as well as other non-target insects, but also reduced the malaria incidence. About 93.2% of the respondents were ready to purchase LLINs if available at nominal prices. All the respondents were satisfied about the performance of the LLINs in reducing the mosquito nuisance, safety of use and collateral benefits in LLIN villages. CONCLUSION: LLINs are safe, socially acceptable and should be promoted for vector control to reduce the disease burden in the communities.


Assuntos
Atitude Frente a Saúde , Malária/prevenção & controle , Malária/psicologia , Controle de Mosquitos/métodos , Mosquiteiros/estatística & dados numéricos , Saúde da População Rural , Adulto , Feminino , Humanos , Índia/epidemiologia , Malária/epidemiologia , Masculino , Aceitação pelo Paciente de Cuidados de Saúde , Características de Residência , Adulto Jovem
6.
Science ; 177(4047): 442-4, 1972 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-5043146

RESUMO

Delta1-Tetrahydrocannabinol, which is resinous and insoluble in water and therefore difficult to study pharmacologically, can be converted to a watersoluble derivative without loss of its biological activity. This has been achieved by preparing esters bearing a nitrogen moiety with the use of carbodiimide as the condensing agent. The availability of such water-soluble derivatives will allow the evaluation of Delta1-tetrahydrocannabinol in self-administration studies in monkeys for its addiction liability potential in man. This technique of water solubilization is also applicable to other compounds of chemical and biological significance.


Assuntos
Cannabis/síntese química , Anfetamina/farmacologia , Animais , Comportamento Animal/efeitos dos fármacos , Pressão Sanguínea/efeitos dos fármacos , Depressão Química , Cães , Dronabinol/administração & dosagem , Dronabinol/síntese química , Dronabinol/farmacologia , Interações Medicamentosas , Epinefrina/farmacologia , Iminas , Raios Infravermelhos , Injeções Intravenosas , Espectroscopia de Ressonância Magnética , Atividade Motora/efeitos dos fármacos , Norepinefrina/farmacologia , Solubilidade , Análise Espectral
7.
Indian J Med Res ; 129(5): 593-8, 2009 May.
Artigo em Inglês | MEDLINE | ID: mdl-19675390

RESUMO

BACKGROUND & OBJECTIVE: A longitudinal study was carried out to assess the impact of indoor residual spray with Vectron 20 WP (etofenprox) against Anopheles culicifacies and on malaria transmission in a selected village of Dadri primary health centre (PHC), District Gautam Budh Nagar, Uttar Pradesh, India. METHODS: Two villages, namely Patadi and Anandpur in District Gautam Budh Nagar, Uttar Pradesh, with similar malaria incidence and vector prevalence were selected for the present evaluation. In one village two rounds of indoor spraying of etofenprox (0.1 g/m(2)) were done at an interval of 12 wk and the other village was kept as control where no intervention except intensive active surveillance for early detection and prompt treatment (EDPT) was undertaken during the study period. Entomological and epidemiological data were collected using standard procedures. RESULTS: Persistence of the effectiveness of etofenprox against An. culicifacies was observed up to 12 wk. Spraying of etofenprox significantly reduced the density (P<0.001) and proportion of parous An. culicifacies mosquitoes (P<0.05) in the experimental village. There was a significant reduction in malaria cases in the experimental village during the post-spray period when compared to the control village (P<0.05). No adverse effect was reported by the spraymen and inhabitants during and after the spray. INTERPRETATION & CONCLUSION: Indoor residual spray of etofenprox (0.1 g/m(2)) with an interval of three months in between two rounds of spray produced the desired impact in reducing the indoor resting density of vector mosquitoes and also in curtailing malaria transmission in the sprayed village when compared with the control village without spray.


Assuntos
Anopheles/efeitos dos fármacos , Inseticidas/toxicidade , Malária/prevenção & controle , Piretrinas/toxicidade , Animais , Anopheles/patogenicidade , Relação Dose-Resposta a Droga , Humanos , Índia , Estudos Longitudinais , Malária/transmissão
8.
Neuroscience ; 152(3): 753-60, 2008 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-18304750

RESUMO

Cannabinoid receptor activation has been shown to modulate both neurotransmission (CB(1)) and neuroinflammatory (CB(2)) responses. There are conflicting reports in the literature describing the influence of cannabinoid receptor activation on ischemic/reperfusion injury. The goal of this study was to evaluate how changing the balance between CB(1) and CB(2) activation following cerebral ischemia influences outcome. CB(1) and CB(2) expression were tested at different times after transient middle cerebral artery occlusion (MCAO) in mice by real-time RT-PCR. Animals subjected to 1 h MCAO were randomly assigned to receive different treatments: a CB(1) antagonist, a CB(2) antagonist, a CB(2) agonist, a CB(1) antagonist plus CB(2) agonist, a CB(2) antagonist plus CB(2) agonist or an equal volume of vehicle as control. Cerebral blood flow was continuously monitored during ischemia; cerebral infarction and neurological deficit were tested 24 h after MCAO. Cerebral CB(1) and CB(2) mRNA expression undertook dynamic changes during cerebral ischemia. The selective CB(1) antagonist significantly decreased cerebral infarction by 47%; the selective CB(2) antagonist increased infarction by 26% after 1 h MCAO followed by 23 h reperfusion in mice. The most striking changes were obtained by combining a CB(1) antagonist with a CB(2) agonist. This combination elevated the cerebral blood flow during ischemia and reduced infarction by 75%. In conclusion, during cerebral ischemia/reperfusion injury, inhibition of CB(1) receptor activation is protective while inhibition of CB(2) receptor activation is detrimental. The greatest degree of neuroprotection was obtained by combining an inhibitor of CB(1) activation with an exogenous CB(2) agonist.


Assuntos
Isquemia Encefálica/tratamento farmacológico , Moduladores de Receptores de Canabinoides/farmacologia , Fármacos Neuroprotetores/farmacologia , Receptor CB1 de Canabinoide/metabolismo , Receptor CB2 de Canabinoide/metabolismo , Traumatismo por Reperfusão/tratamento farmacológico , Animais , Isquemia Encefálica/metabolismo , Isquemia Encefálica/fisiopatologia , Moduladores de Receptores de Canabinoides/metabolismo , Moduladores de Receptores de Canabinoides/uso terapêutico , Canabinoides/farmacologia , Canabinoides/uso terapêutico , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/metabolismo , Córtex Cerebral/fisiopatologia , Infarto Cerebral/tratamento farmacológico , Infarto Cerebral/metabolismo , Infarto Cerebral/prevenção & controle , Combinação de Medicamentos , Sinergismo Farmacológico , Infarto da Artéria Cerebral Média/tratamento farmacológico , Infarto da Artéria Cerebral Média/metabolismo , Infarto da Artéria Cerebral Média/fisiopatologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Fármacos Neuroprotetores/uso terapêutico , RNA Mensageiro/efeitos dos fármacos , RNA Mensageiro/metabolismo , Receptor CB1 de Canabinoide/efeitos dos fármacos , Receptor CB1 de Canabinoide/genética , Receptor CB2 de Canabinoide/efeitos dos fármacos , Receptor CB2 de Canabinoide/genética , Traumatismo por Reperfusão/metabolismo , Traumatismo por Reperfusão/fisiopatologia , Fatores de Tempo , Resultado do Tratamento
9.
Br J Pharmacol ; 150(5): 613-23, 2007 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17245363

RESUMO

BACKGROUND AND PURPOSE: A nonpsychoactive constituent of the cannabis plant, cannabidiol has been demonstrated to have low affinity for both cannabinoid CB1 and CB2 receptors. We have shown previously that cannabidiol can enhance electrically evoked contractions of the mouse vas deferens, suggestive of inverse agonism. We have also shown that cannabidiol can antagonize cannabinoid receptor agonists in this tissue with a greater potency than we would expect from its poor affinity for cannabinoid receptors. This study aimed to investigate whether these properties of cannabidiol extend to CB1 receptors expressed in mouse brain and to human CB2 receptors that have been transfected into CHO cells. EXPERIMENTAL APPROACH: The [35S]GTPS binding assay was used to determine both the efficacy of cannabidiol and the ability of cannabidiol to antagonize cannabinoid receptor agonists (CP55940 and R-(+)-WIN55212) at the mouse CB1 and the human CB2 receptor. KEY RESULTS: This paper reports firstly that cannabidiol displays inverse agonism at the human CB2 receptor. Secondly, we demonstrate that cannabidiol is a high potency antagonist of cannabinoid receptor agonists in mouse brain and in membranes from CHO cells transfected with human CB2 receptors. CONCLUSIONS AND IMPLICATIONS: This study has provided the first evidence that cannabidiol can display CB2 receptor inverse agonism, an action that appears to be responsible for its antagonism of CP55940 at the human CB2 receptor. The ability of cannabidiol to behave as a CB2 receptor inverse agonist may contribute to its documented anti-inflammatory properties.


Assuntos
Anti-Inflamatórios/farmacologia , Benzoxazinas/antagonistas & inibidores , Encéfalo/efeitos dos fármacos , Canabidiol/farmacologia , Agonistas de Receptores de Canabinoides , Cicloexanos/antagonistas & inibidores , Morfolinas/antagonistas & inibidores , Naftalenos/antagonistas & inibidores , Fenóis/antagonistas & inibidores , Animais , Anti-Inflamatórios/metabolismo , Benzoxazinas/farmacologia , Encéfalo/metabolismo , Células CHO , Canfanos/farmacologia , Canabidiol/metabolismo , Antagonistas de Receptores de Canabinoides , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Cricetinae , Cricetulus , Cicloexanos/farmacologia , Cicloexanóis , Relação Dose-Resposta a Droga , Guanosina 5'-O-(3-Tiotrifosfato)/metabolismo , Humanos , Técnicas In Vitro , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Knockout , Morfolinas/farmacologia , Naftalenos/farmacologia , Fenóis/farmacologia , Piperidinas/farmacologia , Ligação Proteica , Pirazóis/farmacologia , Receptor CB1 de Canabinoide/agonistas , Receptor CB2 de Canabinoide/agonistas , Receptores de Canabinoides/genética , Receptores de Canabinoides/metabolismo , Rimonabanto , Transfecção
10.
Br J Pharmacol ; 150(5): 586-94, 2007 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17245367

RESUMO

BACKGROUND AND PURPOSE: To follow up in vitro evidence that Delta(9)-tetrahydrocannabivarin extracted from cannabis (eDelta(9)-THCV) is a CB(1) receptor antagonist by establishing whether synthetic Delta(9)-tetrahydrocannabivarin (O-4394) and Delta(8)-tetrahydrocannabivarin (O-4395) behave as CB(1) antagonists in vivo. EXPERIMENTAL APPROACH: O-4394 and O-4395 were compared with eDelta(9)-THCV as displacers of [(3)H]-CP55940 from specific CB(1) binding sites on mouse brain membranes and as antagonists of CP55940 in [(35)S]GTPgammaS binding assays performed with mouse brain membranes and of R-(+)-WIN55212 in mouse isolated vasa deferentia. Their ability to antagonize in vivo effects of 3 or 10 mg kg(-1) (i.v.) Delta(9)-tetrahydrocannabinol in mice was then investigated. KEY RESULTS: O-4394 and O-4395 exhibited similar potencies to eDelta(9)-THCV as displacers of [(3)H]-CP55940 (K (i)=46.6 and 64.4 nM, respectively) and as antagonists of CP55940 in the [(35)S]GTPgammaS binding assay (apparent K (B)=82.1 and 125.9 nM, respectively) and R-(+)-WIN55212 in the vas deferens (apparent K (B)=4.8 and 3.9 nM respectively). At i.v. doses of 0.1, 0.3, 1.0 and/or 3 mg kg(-1) O-4394 and O-4395 attenuated Delta(9)-tetrahydrocannabinol-induced anti-nociception (tail-flick test) and hypothermia (rectal temperature). O-4395 but not O-4394 also antagonized Delta(9)-tetrahydrocannabinol-induced ring immobility. By themselves, O-4395 and O-4394 induced ring immobility at 3 or 10 mg kg(-1) (i.v.) and antinociception at doses above 10 mg kg(-1) (i.v.). O-4395 also induced hypothermia at 3 mg kg(-1) (i.v.) and above. CONCLUSIONS AND IMPLICATIONS: O-4394 and O-4395 exhibit similar in vitro potencies to eDelta(9)-THCV as CB(1) receptor ligands and as antagonists of cannabinoid receptor agonists and can antagonize Delta(9)-tetrahydrocannabinol in vivo.


Assuntos
Encéfalo/efeitos dos fármacos , Antagonistas de Receptores de Canabinoides , Dronabinol/análogos & derivados , Dronabinol/antagonistas & inibidores , Psicotrópicos/antagonistas & inibidores , Ducto Deferente/efeitos dos fármacos , Analgésicos não Narcóticos/antagonistas & inibidores , Animais , Benzoxazinas/farmacologia , Ligação Competitiva , Temperatura Corporal/efeitos dos fármacos , Encéfalo/metabolismo , Agonistas de Receptores de Canabinoides , Cicloexanos/metabolismo , Cicloexanos/farmacologia , Cicloexanóis , Relação Dose-Resposta a Droga , Dronabinol/metabolismo , Dronabinol/farmacologia , Estimulação Elétrica , Guanosina 5'-O-(3-Tiotrifosfato)/metabolismo , Técnicas In Vitro , Locomoção/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Morfolinas/farmacologia , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Músculo Liso/metabolismo , Naftalenos/farmacologia , Medição da Dor , Limiar da Dor/efeitos dos fármacos , Fenóis/metabolismo , Fenóis/farmacologia , Ligação Proteica , Receptor CB1 de Canabinoide/antagonistas & inibidores , Receptor CB2 de Canabinoide/antagonistas & inibidores , Receptores de Canabinoides/metabolismo , Ducto Deferente/metabolismo
11.
J Am Mosq Control Assoc ; 23(2): 220-3, 2007 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-17847857

RESUMO

Bioefficacy of PermaNet was evaluated in both the laboratory and field against Anopheles culicifacies and An. stephensi, major malaria vectors in India. Contact bioassays were carried out after repeated washings and ring net bioassays to determine the median knockdown time of mosquitoes. Three villages were selected for the field trial: in the 1st village PermaNets were distributed, in the 2nd village untreated nets were distributed, and the 3rd village was a control. Entomological data were collected using standard procedures. The PermaNet contact bioassays showed high mortality (>80%) even after 20 washes against both the vector species. The median knockdown time of An. culicifacies and An. stephensi was 392 and 480 sec when exposed to fresh PermaNets and 472 and 986 sec when exposed to PermaNets that had been washed 20 times, respectively. PermaNets showed high efficacy in reducing the person-vector contact as evidenced by reduced person-hour density in the PermaNet village. Long-term field trials are indicated to test the impact of use of PermaNets in controlling malaria.


Assuntos
Anopheles/efeitos dos fármacos , Roupas de Cama, Mesa e Banho , Inseticidas/farmacologia , Malária/transmissão , Controle de Mosquitos/métodos , Animais , Índia , Malária/prevenção & controle
12.
J Vector Borne Dis ; 44(2): 137-44, 2007 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-17722868

RESUMO

BACKGROUND & OBJECTIVES: Efficacy of Olyset nets, long-lasting insecticidal nets were tested from August 2003 to August 2006 against Anopheles culicifacies, the vector which transmits 60% of all malaria cases in rural India. METHODS: Three villages in District Gautam Budh Nagar (Uttar Pradesh), India were selected for the trial and Olyset nets were distributed in one village, in another village untreated nets were distributed and the third village was kept as control where nets were not used. Entomological, and epidemiological data were collected using standard methods. RESULTS: The use of Olyset nets reduced the indoor resting density of An. culicifacies and also reduced mosquito entry into the structures where Olyset nets were used. No mosquitoes were caught landing on the Olyset nets. There was a reduction in the parity rate of An. culicifacies in the Olyset net village as compared with untreated net and no net villages. The impact of Olyset nets was observed on malaria incidence and only one case of Plasmodiumfalciparum malaria was reported in the Olyset net village but these continued to be found in the village with untreated nets and the control. CONCLUSION: Results of the present study confirmed that Olyset nets are highly effective in reducing the indoor resting density of mosquitoes, man-vector contact and malaria incidence.


Assuntos
Anopheles , Roupas de Cama, Mesa e Banho , Insetos Vetores , Inseticidas/administração & dosagem , Malária/prevenção & controle , Malária/transmissão , Animais , Humanos , Índia , Controle de Mosquitos/métodos , Saúde da População Rural
13.
J Am Mosq Control Assoc ; 22(1): 102-6, 2006 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-16646330

RESUMO

Olyset nets are highly effective in killing anopheline mosquitoes within 3 min of exposure, as evidenced in cone bioassay tests. These nets also showed their efficacy on other vector mosquitoes (Aedes aegypti and Cx. quinquefasciatus) at higher exposure periods. The efficacy remained at approximately 90% even after 20 washings at an interval of 24 h against Anopheles culicifacies and Cx. quinquefasciatus. Use of the nets inside the house also resulted in drastic reduction of daytime resting density of mosquitoes because of high repellency, excitorepellency, and killing action of the nets. Pilot studies are indicated to evaluate the impact of use of Olyset nets on vector-borne diseases, particularly malaria, and its cost-effectiveness in comparison to conventional indoor residual spraying.


Assuntos
Controle de Mosquitos/métodos , Aedes , Animais , Anopheles , Roupas de Cama, Mesa e Banho , Culex , Índia , Permetrina
14.
J Am Mosq Control Assoc ; 21(4): 432-6, 2005 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-16506568

RESUMO

Hilmilin (diflubenzuron), an insect growth regulator, was tested for efficacy against Anopheles stephensi, Anopheles culicifacies, Aedes aegypti, and Culex quinquefasciatus in the laboratory and in field conditions. Fifty percent and 90% lethal concentrations (LC50 and LC90) of Hilmilin formulations were determined by exposing early 4th-stage larvae to serial dilutions of the formulation, and data were subjected to log probit analysis. Two doses (0.004 and 0.008 g/m2) were applied in different breeding habitats of mosquitoes with the help of stirrup pumps. Percent inhibition of adult emergence was compared according to a previously described procedure. Laboratory results revealed that both 25WP (wettable powder) and 22SL (semiliquid) formulations showed more or less the same degree of efficacy against tested mosquito species (P < 0.05). Of 4 species tested, An. stephensi was more susceptible, followed by An. culicifacies, Ae. aegypti, and Cx. quinquefasciatus. One hundred percent inhibition of adult emergence was observed at a dose of 0.0125 ppm (25WP and 22SL) against all mosquitoes tested in the laboratory. Both formulations showed almost similar effect when applied in the field at doses of 0.004 and 0.008 g/m2 in their respective preferential breeding habitats. However, the effect was more pronounced at a higher concentration (0.008 g/m2) against all species of mosquitoes. Hilmilin at a dose of 0.008 g/m2 can be used to contain mosquito breeding in stone quarries, pools, cement tanks, unused wells, unused coolers, and irrigation channels.


Assuntos
Aedes , Anopheles , Culex , Diflubenzuron , Inseticidas , Animais , Índia , Larva , Dose Letal Mediana , Fatores de Tempo
15.
J Vector Borne Dis ; 42(3): 95-9, 2005 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16294807

RESUMO

BACKGROUND AND OBJECTIVES: Various plant-based products are safe and biodegradable alternatives to synthetic chemicals for use against mosquitoes. Oil of Pinus longifolia is traditionally used for protection against mosquitoes in some rural areas but there is no documented report of its use against mosquitoes. The present study was undertaken to scientifically evaluate the activity of Pine oil against mosquitoes. METHODS: The oil was procured from the market and its contents were chemically analysed. Larvicidal activity of oil was tested in laboratory bioassays, while repellent action was studied during whole night bait collections in field by direct application on the skin and after its impregnation on mats. RESULTS: Results showed varying degree of larvicidal activity of Pine oil against mosquitoes with LC50 values ranging between 82 and 112 ppm. The Pine oil had strong repellent action against mosquitoes as it provided 100% protection against Anopheles culicifacies for 11 h and 97% protection against Culex quinquefasciatus for nine hours respectively. Electrically heated mats prepared from Pine oil provided, 94 and 88% protection against An. culicifacies and Cx. quinquefasciatus for 10 and seven hours respectively. INTERPRETAION AND CONCLUSION: Pine oil is effective against mosquito larvae at very higher doses which are not of any practical utility. However, Pine oil showed strong repellent action against An. culicifacies (malaria vector) and Cx. quinquefasciatus (pest mosquito). Thus its use could be popularised as mosquito repellent.


Assuntos
Culicidae , Repelentes de Insetos/química , Pinus/química , Óleos de Plantas/química , Animais , Temperatura Alta , Larva , Dose Letal Mediana , Especificidade da Espécie
16.
Neuropharmacology ; 35(12): 1793-804, 1996.
Artigo em Inglês | MEDLINE | ID: mdl-9076759

RESUMO

delta 8-Tetrahydrocannabinol (delta 8-THC) is a naturally occurring cannabinoid with a characteristic pharmacological profile of in vivo effects. Previous studies have shown that modification of the structure of delta 8-THC by inclusion of a nitrogen-containing functional group alters this profile and may alkylate the cannabinoid receptor, similar to the manner in which beta-funaltrexamine (beta-FNA) alkylates the micro-opioid receptor. Two novel analogs of delta 8-THC were synthesized: a nitrogen mustard analog with a dimethylheptyl side chain (NM-delta 8-THC) and a cyano analog with a dimethylpentyl side chain (CY-delta 8-THC). Both analogs showed high affinity for brain cannabinoid receptors and when administered acutely, produced characteristic delta 9-THC-like effects in mice, including locomotor suppression, hypothermia, antinociception and catalepsy. CY-delta 8-THC shared discriminative stimulus effects with CP 55,940; for NM-delta 8-THC, these effects also occurred, but were delayed. Although both compounds attenuated the effects of delta 9-THC in the mouse behavioral tests, evaluation of potential antagonist effects of these compounds was complicated by the fact that two injections of delta 9-THC produced similar results, suggesting that acute tolerance or desensitization might account for the observations. NM-delta 8-THC, but not CY-delta 8-THC, attenuated the discriminative stimulus effects of CP 55,940 in rats several days following injection. Hence, addition of a nitrogen-containing functional group to a traditional cannabinoid structure does not eliminate agonist effects and may produce delayed attenuation of cannabinoid-induced pharmacological effects.


Assuntos
Dronabinol/análogos & derivados , Dronabinol/farmacologia , Aprendizagem em Labirinto/efeitos dos fármacos , Atividade Motora/efeitos dos fármacos , Compostos de Mostarda Nitrogenada/farmacologia , Dor/fisiopatologia , Animais , Regulação da Temperatura Corporal/efeitos dos fármacos , Canabinoides/farmacologia , Catalepsia , Cicloexanóis/farmacologia , Dronabinol/síntese química , Masculino , Camundongos , Camundongos Endogâmicos ICR , Compostos de Mostarda Nitrogenada/síntese química , Ratos , Ratos Sprague-Dawley , Receptores de Canabinoides , Receptores de Droga/agonistas , Receptores de Droga/antagonistas & inibidores , Relação Estrutura-Atividade
17.
J Med Chem ; 19(5): 719-21, 1976 May.
Artigo em Inglês | MEDLINE | ID: mdl-1271414

RESUMO

Two cyclic analogues 8 and 9 of dimethylheptylpyran (DMHP, 1) were synthesized by the Pechmann condensation of the resorcinol 4 with ethyl 4-methyl-2-cyclohexanone-1-carboxylate followed by Grignard addition with MeMgI. In selected pharmacological tests both analogues 8 and 9 were considered inactive compared to DMHP as CNS and cardiovascular agents.


Assuntos
Benzopiranos/síntese química , Cannabis/síntese química , Animais , Benzopiranos/farmacologia , Pressão Sanguínea/efeitos dos fármacos , Cannabis/farmacologia , Ciclização , Camundongos , Atividade Motora/efeitos dos fármacos , Ratos , Relação Estrutura-Atividade
18.
J Med Chem ; 19(11): 1328-30, 1976 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-1003411

RESUMO

Two delta8-THC derivatives, 4a and 4b, with functionalized side chains were synthesized. Treatment of (+)-trans-p-mentha-2,8-dien-1-ol with the resorcinal 2b followed by removal of the dithiol group with HgO--BF3-Et2O gave the aldehyde 3b. A Wittig reaction of dimethyl (2-oxoheptyl)phosphate with 3b furnished 4a, which was reduced to 4b. Compounds 4a and 4b showed potent cannabinoid-like activity in mice.


Assuntos
Dronabinol/análogos & derivados , Psicotrópicos/síntese química , Animais , Comportamento Animal/efeitos dos fármacos , Di-Hidroxifenilalanina/farmacologia , Dronabinol/síntese química , Dronabinol/farmacologia , Sinergismo Farmacológico , Camundongos , Psicotrópicos/farmacologia , Tempo de Reação/efeitos dos fármacos , Relação Estrutura-Atividade
19.
J Med Chem ; 25(8): 986-90, 1982 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-7120287

RESUMO

A direct conversion of deoxydihydrothebaine-phi (1) to 3-methoxymorphinan-6-one (3Ca) and its trans isomer 3Ta was achieved in excellent yield by the catalytic reduction of 1 in AcOH containing CF3COOH. Treatment of 3Ca or 3Ta with NaH and diethyl carbonate formed the corresponding 7-carbethoxy derivatives 4a which, on O-demethylation, furnished the 3-hydroxy compounds 4b. The analgesic N-methyl compounds 3 were converted to the 17-(cyclopropylmethyl) or 17-(cyclobutylmethyl) derivatives 6--8. Two of these compounds, one in the cis (7Ca) and the other in the trans (7Ta) series, showed mixed agonist/antagonist activity in the pentazocine range.


Assuntos
Morfinanos/síntese química , Antagonistas de Entorpecentes/síntese química , Entorpecentes/síntese química , Animais , Fenômenos Químicos , Química , Camundongos , Morfinanos/farmacologia , Ratos , Tempo de Reação/efeitos dos fármacos
20.
J Med Chem ; 25(8): 983-6, 1982 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-6181259

RESUMO

A series of 7-alkanoyl-substituted hydromorphone derivatives were prepared by acylation of the morpholine enamines. The most potent compound (6i) of the series was found to have agonist activity of the same order of magnitude as that of buprenorphine. The N-cyclopropylmethyl-substituted series was found to exhibit structure-activity relationships for analgesia and narcotic antagonism similar to those of the endo-ethanotetrahydrooripavines.


Assuntos
Hidromorfona/análogos & derivados , Antagonistas de Entorpecentes/síntese química , Entorpecentes/síntese química , Animais , Fenômenos Químicos , Química , Hidromorfona/síntese química , Hidromorfona/farmacologia , Camundongos , Tempo de Reação/efeitos dos fármacos
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