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1.
Zootaxa ; 3760: 539-52, 2014 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-24870104

RESUMO

A new species of the gekkonid Hemiphyllodactylus banaensis sp. nov. is described from Ba Na-Nui Chua Nature Reserve in central Vietnam. Previously included within H. yunnanensis, the new species is distinguished from all other congeners by having the unique combination of a maximum SVL of 48.2 mm in males and 51.0 mm in females; seven chin scales extending transversely from the union of the first and second infralabials and posterior margin of mental; enlarged postmental scales; 9-12 supralabials; 9-11 infralabials; 18-20 longitudinally arranged dorsal scales at midbody contained within one eye diameter; 20-21 precloacal and femoral pore-bearing scales contiguous in males and 0-20 contiguous pore-bearing precloacal scales in females; dorsal pattern on body composed of transverse blotches and two whitish stripes across shoulder extending to sacrum; postsacral mark whitish brown and bearing anteriorly projecting arms; and caecum and oviducts unpigmented.


Assuntos
Lagartos/anatomia & histologia , Lagartos/classificação , Animais , Demografia , Feminino , Lagartos/genética , Lagartos/fisiologia , Masculino , Filogenia , Especificidade da Espécie , Vietnã
2.
J Obstet Gynaecol ; 32(5): 413-8, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22663308

RESUMO

Vasa praevia can cause acute severe fetal haemorrhage prior to or during rupture of the membranes, contributing to perinatal morbidity and mortality. There are no large prospective studies relating to vasa praevia and there is no place for a randomised controlled trial as it would be ethically unjustifiable given the poor prognosis. There are no national guidelines for the management of vasa praevia. Identification of vasa praevia by the 3rd trimester of pregnancy warrants the offer of delivery by planned caesarean section to avoid the complications. This is essentially intuitive and logical rather than based on any randomised trials. A universal screening programme for vasa praevia is not currently supported by a robust evidence base; however, the role of prenatal diagnosis requires an informed debate, as high quality data may not be forthcoming, given the low evidence of the condition. Increasing awareness and understanding of the clinical situations can accumulate information, which identify and treat this tragic complication of childbirth.


Assuntos
Diagnóstico Pré-Natal , Vasa Previa/diagnóstico , Cesárea , Feminino , Doenças Fetais/etiologia , Idade Gestacional , Hemorragia/etiologia , Humanos , Programas de Rastreamento , Mortalidade Perinatal , Gravidez , Vasa Previa/terapia
3.
BJOG ; 117(13): 1643-50, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21078058

RESUMO

OBJECTIVE: The Paediatric and Adolescent Gynaecology service (PAG) at Kettering General Hospital is a designated service meeting the needs of children with gynaecological problems. National guidelines reinforce the fact that children should be seen within specific paediatric areas in hospital. We aim to review the role of such a service in the context of a British district general hospital. DESIGN: Retrospective review spanning 15 years. SETTING: The outpatient/inpatient service of a UK district general hospital. POPULATION: A total of 800 patients were included in the study. METHODS: We identified patients attending the PAG clinic between 1994 and 2009. Medical notes were reviewed individually. MAIN OUTCOME MEASURES: Demographics, referral source, presenting symptoms, examination findings, diagnosis, management, admissions and referrals to tertiary centres. RESULTS: In total, 86% of patients were referred from primary care. The age distribution was bimodal at 4 and 15 years of age: the average age was 10 years. Sixty percent of patients were followed-up, giving a total of 2023 appointments. The commonest presentations were vulvovaginitis (18%), labial adhesions (14%), abdominal pain (7%) and precocious puberty (6%). A total of 15% of patients were admitted, largely for planned procedures, of which vaginoscopy was the most frequent. CONCLUSIONS: The PAG service has enabled pathways for care that were previously non-existent, as well as the development of 'best practice'. The British Society for Paediatric and Adolescent Gynaecology has been seeking to develop a network of similar services at secondary and tertiary level throughout the UK. This approach should be encouraged and promoted by those in charge of healthcare policy and provider trusts in general.


Assuntos
Serviços de Saúde do Adolescente/estatística & dados numéricos , Serviços de Saúde da Criança/estatística & dados numéricos , Hospitais de Distrito/estatística & dados numéricos , Hospitais Gerais/estatística & dados numéricos , Serviços de Saúde da Mulher/estatística & dados numéricos , Adolescente , Criança , Pré-Escolar , Inglaterra , Feminino , Doenças dos Genitais Femininos/terapia , Genitália Feminina/anormalidades , Humanos , Lactente , Distúrbios Menstruais/terapia , Gravidez , Gravidez na Adolescência , Puberdade Precoce/terapia , Estudos Retrospectivos , Delitos Sexuais , Transtornos Urinários/terapia , Vulvovaginite/terapia
4.
Zootaxa ; 4766(2): zootaxa.4766.2.7, 2020 Apr 20.
Artigo em Inglês | MEDLINE | ID: mdl-33056602

RESUMO

A new species of insular Bent-toed Gecko, Cyrtodactylus culaochamensis sp. nov. of the C. irregularis group is described from Cu Lao Cham Mountain, from Hon Lao Island, Hoi An City, Quang Nam Province, Cham Islands, central Vietnam. Cyrtodactylus culaochamensis sp. nov. is the sister species of C. pseudoquadrivirgatus from Ba Na Nui Chua from Danang City, central Vietnam. It differs from all congeners by having a maximum SVL of 79.8 mm (n=5); dark spots on the head edged in white; a fragmented nuchal loop; irregularly shaped, broad, completed or broken dorsal bands; 19-21 interorbital scales across the frontal bone; 28-32 scales between the eye and nostril; 45-50 rows of ventral scales between the ventrolateral folds; scattered, smooth tubercles; 20-22 irregular, longitudinal rows of weakly keeled tubercles at midbody between the ventrolateral folds; seven or eight precloacal pores in a chevron pattern in males; no enlarged femoral scales, no femoral pores; 13-15 subdigital lamellae on first toe; 20-23 subdigital lamellae on fourth toe; and very slightly enlarged subcaudal scales.


Assuntos
Lagartos , Distribuição Animal , Estruturas Animais , Animais , Tamanho Corporal , Ecossistema , Masculino , Vietnã
5.
Eur J Obstet Gynecol Reprod Biol ; 235: 30-35, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30780074

RESUMO

BACKGROUND: The British Society of Paediatric and Adolescent Gynaecology (BritSPAG) was created in 2000 with specific aims to include raising the profile of paediatric and adolescent gynaecology (PAG) within the United Kingdom (UK). The Society has since developed a set of clinical standards for all acute hospitals providing gynaecological services to enable successful provision of paediatric and adolescent gynaecology care. AIMS: To determine the depth of knowledge that obstetric and gynaecology trainees have with regards to the PAG services provided at their Hospital, reflecting how widely PAG services have had an impact on trainees. METHOD: The national survey was distributed to all deaneries in the UK for circulation to all their trainees via e mail during Nov 2017-March 2018. RESULTS: 28% of the trainees said there was a PAG clinic at their hospital, 46.9% did not have a clinic and 24.7% were unsure. 41.6% of the respondents were aware of BritSPAG, however only 10.4% were aware of the BritSPAG clinical standards for service planning with regards to PAG clinics. Nearly half were aware of the PAG specialist centre for their region but only 6.5% were aware of the BritSPAG UK map of services. A large majority (93.24%) didn't believe that trainees in O&G received adequate exposure to PAG in their training. CONCLUSION: This study represents the largest and first national survey to seek obstetric and gynaecology trainees' thoughts on the provision of PAG training in the UK today. Given that only 28% of trainees answering said that they were aware of a PAG clinic at their hospital, this indicates not only that many hospitals did not have a dedicated PAG clinic but more worryingly five of the trainees were not aware of the existence of a confirmed PAG clinic at their hospital, and therefore are potentially losing out on training opportunities. Disappointingly the results of our survey reveal that trainees in Obstetrics and Gynaecology still have very little experience or exposure to PAG during their training despite there being opportunities to do so.


Assuntos
Ginecologia/educação , Conhecimentos, Atitudes e Prática em Saúde , Serviços de Saúde Materna , Obstetrícia/educação , Estudantes de Medicina/psicologia , Adolescente , Medicina do Adolescente/métodos , Adulto , Criança , Feminino , Ginecologia/métodos , Humanos , Masculino , Pessoa de Meia-Idade , Obstetrícia/métodos , Pediatria/métodos , Gravidez , Pesquisa Qualitativa , Inquéritos e Questionários , Reino Unido
6.
J Bone Joint Surg Br ; 89(5): 615-9, 2007 May.
Artigo em Inglês | MEDLINE | ID: mdl-17540746

RESUMO

A consecutive series of 23 patients (25 ankles) with osteoarthritis of the ankle and severe varus or valgus deformity were treated by open arthrodesis using compression screws. Primary union was achieved in 24 ankles one required further surgery to obtain a solid fusion. The high level of satisfaction in this group of patients reinforces the view that open arthrodesis, as opposed to ankle replacement or arthroscopic arthrodesis, continues to be the treatment of choice when there is severe varus or valgus deformity associated with the arthritis.


Assuntos
Articulação do Tornozelo/cirurgia , Artrodese/métodos , Deformidades Articulares Adquiridas/cirurgia , Osteoartrite/cirurgia , Adulto , Idoso , Idoso de 80 Anos ou mais , Articulação do Tornozelo/diagnóstico por imagem , Articulação do Tornozelo/fisiopatologia , Artrodese/efeitos adversos , Artrodese/reabilitação , Parafusos Ósseos , Feminino , Humanos , Deformidades Articulares Adquiridas/diagnóstico por imagem , Deformidades Articulares Adquiridas/etiologia , Masculino , Pessoa de Meia-Idade , Osteoartrite/complicações , Osteoartrite/diagnóstico por imagem , Satisfação do Paciente , Radiografia , Recuperação de Função Fisiológica , Resultado do Tratamento
7.
J Bone Joint Surg Br ; 88(8): 1032-8, 2006 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-16877602

RESUMO

Between 1999 and 2005, 23 failed total ankle replacements were converted to arthrodeses. Three surgical techniques were used: tibiotalar arthrodesis with screw fixation, tibiotalocalcaneal arthrodesis with screw fixation, and tibiotalocalcaneal arthrodesis with an intramedullary nail. As experience was gained, the benefits and problems became apparent. Successful bony union was seen in 17 of the 23 ankles. The complication rate was higher in ankles where the loosening had caused extensive destruction of the body of the talus, usually in rheumatoid arthritis. In this situation we recommend tibiotalocalcaneal arthrodesis with an intramedullary nail. This technique can also be used when there is severe arthritic change in the subtalar joint. Arthrodesis of the tibiotalar joint alone using compression screws was generally possible in osteoarthritis because the destruction of the body of the talus was less extensive. Tibiotalocalcaneal arthrodesis fusion with compression screws has not been successful in our experience.


Assuntos
Articulação do Tornozelo/cirurgia , Artrodese/métodos , Artroplastia de Substituição/métodos , Articulações do Pé/cirurgia , Adulto , Idoso , Articulação do Tornozelo/diagnóstico por imagem , Artrite Reumatoide/diagnóstico por imagem , Artrite Reumatoide/cirurgia , Pinos Ortopédicos , Parafusos Ósseos , Calcâneo , Feminino , Articulações do Pé/diagnóstico por imagem , Humanos , Masculino , Pessoa de Meia-Idade , Osteoartrite/diagnóstico por imagem , Osteoartrite/cirurgia , Complicações Pós-Operatórias , Desenho de Prótese , Falha de Prótese , Radiografia , Reoperação , Articulação Talocalcânea/patologia , Tálus , Tíbia , Falha de Tratamento
8.
Zootaxa ; 4061(1): 1-17, 2016 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-27395475

RESUMO

A new species of Bent-toed Gecko, Cyrtodactylus gunungsenyumensis sp. nov. of the sworderi complex, is described from Hutan Lipur Gunung Senyum, Pahang, Peninsular Malaysia and is differentiated from all other species in the sworderi complex by having a unique combination of characters including a maximum SVL of 74.7 mm; low, rounded, weakly keeled, body tubercles; 34-40 paravertebral tubercles; weak ventrolateral body fold lacking tubercles; 38-41 ventral scales; an abrupt transition between the posterior and ventral femoral scales; 20-23 subdigital lamellae on the fourth toe; enlarged femoral scales; no femoral or precloacal pores; no precloacal groove; wide caudal bands; and an evenly banded dorsal pattern. Cyrtodactylus gunungsenyumensis sp. nov. is a scansorial, karst forest-adapted specialist endemic to the karst ecosystem surrounding Gunung Senyum and occurs on the vertical walls of the limestone towers as well as the branches, trunks, and leaves of the vegetation in the associated karst forest. Cyrtodactylus gunungsenyumensis sp. nov. is the seventh species of karst forest-adapted Cyrtodactylus and the sixteenth endemic species of karst ecosystem reptile discovered in Peninsular Malaysia in the last seven years from only 12 different karst forests. This is a clear indication that many species remain to be discovered in the approximately 558 isolated karst ecosystems in Peninsular Malaysia not yet surveyed. These data continue to underscore the importance of karst ecosystems as reservoirs of biodiversity and microendemism and that they constitute an important component of Peninsular Malaysia's natural heritage and should be protected from the quarrying interests of foreign industrial companies.


Assuntos
Lagartos/classificação , Distribuição Animal , Estruturas Animais/anatomia & histologia , Estruturas Animais/crescimento & desenvolvimento , Animais , Tamanho Corporal , Conservação dos Recursos Naturais , Indústria da Construção , Ecossistema , Espécies em Perigo de Extinção , Feminino , Florestas , Lagartos/anatomia & histologia , Lagartos/genética , Lagartos/crescimento & desenvolvimento , Malásia , Masculino , Tamanho do Órgão , Filogenia
10.
Zootaxa ; 3980(1): 106-26, 2015 Jun 26.
Artigo em Inglês | MEDLINE | ID: mdl-26249941

RESUMO

An integrative taxonomic analysis of the distantly related Cyrtodactylus condorensis and intermedius species complexes of the Mekong Delta revealed that C. paradoxus is a junior synonym of C. condorensis and that C. thochuensis is a junior synonym of C. leegrismeri. Additionally, the analysis revealed that a cave-dwelling ecomorpholgy has evolved independently early on in the evolution of both complexes (represented by C. hontreensis in the intermedius complex and C. grismeri and C. eisenmani in the condorensis complex) and cave ecomorphs exist in sympatry-but not syntopy-with general scansorial ecomorphs. Multiple, recent, cyclical, glacioeustatic driven changes in sea levels across the Sunda Shelf are hypothesized to account for the evolution and distribution of the widely separated, conspecific insular populations of C. condorensis and C. leegrismeri. The independent evolution of cave ecomorphology is proposed to have been driven by competition avoidance. Habitat islands across the Mekong Delta are an important source of endemism and in need of protection.


Assuntos
Distribuição Animal , Cavernas , Lagartos/classificação , Animais , Ecossistema , Lagartos/anatomia & histologia , Lagartos/genética , Lagartos/fisiologia , Filogenia , Especificidade da Espécie , Tailândia
11.
Zootaxa ; 3985(2): 203-18, 2015 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-26250030

RESUMO

A new, diminutive species of Rock Gecko Cnemaspis mahsuriae sp. nov. of the affinis group, is described from Gunung Raya on Pulau Langkawi, Kedah, Peninsular Malaysia and is differentiated from all other species in the affinis group by having a unique combination of characters including a maximum SVL of 36.6 mm; keeled subtibials and ventrals; 21-24 paravertebral tubercles; no tubercles in the lateral caudal furrows; caudal tubercles not encircling tail; no precloacal pores; 23-26 subdigital lamellae on the fourth toe; no white ocelli in the shoulder region; no yellow postscapular band; and faint yellow bars on the flanks. Cnemaspis mahsuriae sp. nov. is a forest-dwelling species living in close sympatry or paraptry with the insular endemic C. roticanai Grismer & Chan. The Langkawi Archipelago harbors a unique mix of Malaysian and Indochinese taxa and the frequency of new discoveries from this group of islands is increasing.


Assuntos
Lagartos/classificação , Distribuição Animal , Estruturas Animais/anatomia & histologia , Estruturas Animais/crescimento & desenvolvimento , Animais , Tamanho Corporal , Feminino , Lagartos/anatomia & histologia , Lagartos/genética , Lagartos/crescimento & desenvolvimento , Malásia , Masculino , Tamanho do Órgão , Filogenia
12.
Zootaxa ; 3948(1): 1-23, 2015 Apr 20.
Artigo em Inglês | MEDLINE | ID: mdl-25947760

RESUMO

An integrative taxonomic analysis is used to identify and describe two new species of the agamid genus Bronchocela (Kuhl) from Peninsular Malaysia: an upland species B. shenlong sp. nov. from Bukit Larut, Perak in the Bintang Mountain Range and Parit Falls, Cameron Highlands, Pahang in the Titiwangsa Mountain Range and an insular species, B. rayaensis sp. nov., from Pulau Langkawi, Kedah off the northwest coast on the border with Thailand. Both species are diagnosed from each other and all other species of Bronchocela on the basis of body shape, scale morphology, and color pattern. The analysis also demonstrates the remarkable genetic similarity of B. cristatella (Kuhl) throughout 1120 km of its range from northern Peninsular Malaysia to western Borneo despite its highly variable coloration and pattern. The two new species are appended to a rapidly growing list of newly described lizard species (60 to date) from Peninsular Malaysia tallied within the last decade.


Assuntos
Lagartos/classificação , Distribuição Animal , Estruturas Animais/anatomia & histologia , Estruturas Animais/crescimento & desenvolvimento , Animais , Tamanho Corporal , Ecossistema , Feminino , Lagartos/anatomia & histologia , Lagartos/genética , Lagartos/crescimento & desenvolvimento , Malásia , Masculino , Tamanho do Órgão , Filogenia
13.
Neurobiol Aging ; 5(4): 269-74, 1984.
Artigo em Inglês | MEDLINE | ID: mdl-6531064

RESUMO

Acetylcholinesterase (AchE) activity (nmol/ml/min) was measured in lumbar CSF from 11 patients with dementia of the Alzheimer type (DAT), 8 patients with Korsakoff psychosis and 33 patients with low back pain who were undergoing myelography (controls). There was no significant difference in enzyme activity between the three groups. There was no significant correlation between age and AchE activity. AchE was also measured in 20 two-ml samples of CSF collected sequentially by lumbar puncture in two neurosurgical patients who had been recumbent for at least 8 hours. Variations in AchE between samples were small. In neither patient was there an increase in AchE activity with progressive sampling. These data indicate that (1) AchE is unchanged in Korsakoff psychosis (2) decreases in brain AchE which are found in DAT are not readily reflected in lumbar CSF (3) AchE in lumbar CSF has a diffuse origin including spinal cord (4) CSF AchE activity is unlikely to be a useful clinical marker for DAT.


Assuntos
Acetilcolinesterase/líquido cefalorraquidiano , Demência/enzimologia , Adulto , Idoso , Transtorno Amnésico Alcoólico/enzimologia , Doença de Alzheimer/enzimologia , Demência/psicologia , Feminino , Humanos , Cinética , Masculino , Pessoa de Meia-Idade , Testes Neuropsicológicos
14.
Neuropharmacology ; 30(4): 399-401, 1991 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-1852270

RESUMO

Morphine was shown to enhance dopamine release in the rat olfactory tubercle, nucleus accumbens, prefrontal cortex and pyriform cortex, as assessed by increased 3-methoxytyramine (3-MT) levels and 3-MT accumulation after pargyline treatment. In contrast, both 3-MT levels and accumulation after pargyline were unaffected by morphine in the rat striatum. These data suggest that the mesolimbic and mesocortical dopaminergic projections in the rat can be activated by opiates and lead to changes in cortical function which may be involved in some of the complex behavioral actions of opiates and opioid peptides.


Assuntos
Encéfalo/efeitos dos fármacos , Dopamina/análogos & derivados , Dopamina/metabolismo , Morfina/farmacologia , Animais , Encéfalo/metabolismo , Córtex Cerebral/metabolismo , Corpo Estriado/metabolismo , Masculino , Núcleo Accumbens/metabolismo , Bulbo Olfatório/metabolismo , Ratos , Ratos Endogâmicos
15.
Neuropharmacology ; 21(4): 349-54, 1982 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-6806676

RESUMO

Meclofenoxate, the p-cholorophenoxyacetic acid ester of deanol, was found to dramatically elevate choline (Ch) levels in the rat CNS. In the hippocampus, this elevation in choline was accompanied by a new elevated steady state level in acetylcholine (ACh). No such coupling was observed in the striatum or parietal cortex. Deanol also elevated choline levels in the CNS but was about half as potent as meclofenoxate; p-chlorophenoxyacetic acid was inactive in this respect. Lesions of striatal neurons with kainic acid and of hippocampal cholinergic nerve endings with surgical section of the fimbria indicated that the changes in choline levels were mainly extraneuronal. In spite of the changes in choline and ACh levels, no consistant alterations in ACh turnover were measured. In summary, meclofenoxate induced dramatic alterations in CNS choline metabolism and may, therefore, be a useful therapeutic tool for potentiating depressed cholinergic neurons.


Assuntos
Encéfalo/efeitos dos fármacos , Colina/metabolismo , Glicolatos/farmacologia , Meclofenoxate/farmacologia , Animais , Encéfalo/metabolismo , Corpo Estriado/efeitos dos fármacos , Relação Dose-Resposta a Droga , Hipocampo/efeitos dos fármacos , Masculino , Lobo Parietal/efeitos dos fármacos , Ratos , Ratos Endogâmicos , Tálamo/efeitos dos fármacos
16.
Neuropharmacology ; 21(12): 1305-10, 1982 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-6296716

RESUMO

Using local injections of drugs and hemisection experiments, a comparison was made of the actions of morphine on the dopaminergic nigrostriatal system of the rat and mouse. In the rat, morphine appeared to act exclusively at presynaptic opiate receptors on dopaminergic nerve endings in the striatum. Activation of these receptors resulted in enhanced dopamine synthesis but with no associated increase in dopamine release. In the mouse, morphine acted at the level of the substantia nigra to enhance both striatal dopamine synthesis and release. The exact localization of these receptors in the substantia nigra remains to be determined.


Assuntos
Corpo Estriado/efeitos dos fármacos , Morfina/farmacologia , Receptores Opioides/efeitos dos fármacos , Substância Negra/efeitos dos fármacos , Ácido 3,4-Di-Hidroxifenilacético/metabolismo , Animais , Dopamina/análogos & derivados , Dopamina/metabolismo , Ácido Homovanílico/metabolismo , Masculino , Camundongos , Naloxona/farmacologia , Ratos , Ratos Endogâmicos , Especificidade da Espécie
17.
Neuropharmacology ; 21(10): 969-72, 1982 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-6292769

RESUMO

Neurochemical and immunohistocytochemical studies have demonstrated a nucleus accumbens-substantia innominata GABAergic pathway. The present authors' data with muscimol given parenterally, as well as local injections into the substantia innominata, further support an inhibitory function for this pathway in the regulation of the substantia innominata-cortical cholinergic projection.


Assuntos
Acetilcolina/metabolismo , Encéfalo/efeitos dos fármacos , Córtex Cerebral/efeitos dos fármacos , Sistema Nervoso Parassimpático/efeitos dos fármacos , Ácido gama-Aminobutírico/farmacologia , Animais , Encéfalo/metabolismo , Sistema Límbico/efeitos dos fármacos , Masculino , Muscimol/farmacologia , Ratos , Ratos Endogâmicos , Receptores de Superfície Celular/fisiologia , Receptores de GABA-A
18.
Neuropharmacology ; 21(3): 215-9, 1982 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-6122185

RESUMO

A study has been made of the inactivation of mu(mu) ([3H]-dihydromorphine), delta (delta) ([3H](D-ala2-D-leu5)enkephalin) and kappa (kappa) ([3H]ethylketazocine) opiate receptor binding sites by N-ethylmaleimide (NEM) and it was observed that in contrast to mu and delta sites, the kappa sites of rat brain membrane preparations were resistant to low concentrations of N-ethylmaleimide. Furthermore, this kappa site was selectively protected, from inactivation with high concentrations of N-ethylmaleimide, by the kappa agonists ethylketazocine and (-)-alpha-(1R,5R,9R)-5,9-dimethyl-2-(L-tetrahydrofurfuryl)-2'-hydroxy-6,7-benzo morphan (MR-2034) but not by morphine or (D-ala2-D-leu5)-enkephalin. These studies suggest that a unique kappa receptor is present in the rat CNS.


Assuntos
Analgésicos Opioides/metabolismo , Ciclazocina/análogos & derivados , Receptores Opioides/metabolismo , Animais , Ciclazocina/metabolismo , Encefalinas/farmacologia , Etilcetociclazocina , Etilmaleimida/farmacologia , Ratos , Receptores Opioides/análise , Receptores Opioides/efeitos dos fármacos , Trítio
19.
Neuropharmacology ; 26(7A): 775-8, 1987 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-2442653

RESUMO

Benzodiazepine receptor ligands are known to modulate the binding of [35S]TBPS to the chloride channel via an allosteric action. In the cases of diazepam, zopiclone and CGS 9895, the enhanced binding of [35S]TBPS induced by these benzodiazepine agonists was antagonized by CGS 8216. This antagonism was characterized both by a shift to the right and a decrease in the maximal stimulation, for the dose-response curves of diazepam and zopiclone. In the case of CGS 9895, the maximal response was not decreased. These data indicate that CGS 8216 is a noncompetitive antagonist of classical benzodiazepine receptor agonists but is a competitive inhibitor of the partial agonist, CGS 9895.


Assuntos
Benzodiazepinas/antagonistas & inibidores , Compostos Bicíclicos Heterocíclicos com Pontes , Compostos Bicíclicos com Pontes/metabolismo , Hidrocarbonetos Aromáticos com Pontes/metabolismo , Cloretos/metabolismo , Canais Iônicos/metabolismo , Pirazóis/farmacologia , Receptores de GABA-A/fisiologia , Animais , Benzodiazepinas/fisiologia , Ratos , Radioisótopos de Enxofre
20.
Neuropharmacology ; 26(11): 1585-8, 1987 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-2893309

RESUMO

Dopaminergic pathways in the brain of the rat have been shown to possess both mu and delta opioid regulatory inputs. In contrast, studies with synthetic kappa opiate agonists have demonstrated a lack of regulation of these dopaminergic systems by kappa opioids. The present authors have extended these observations, to study the effects of the putative endogenous kappa agonists, dynorphin (1-13), on the metabolism of nigrostriatal dopamine in the rat after intraventricular administration. The stability of the intraventricularly administered dynorphin was confirmed in vivo by measuring corticosterone in plasma in the same animals utilized for neurochemical analyses. This is a neuroendocrine parameter which has been demonstrated to possess central regulation by independent mu and kappa receptors. While morphine given parenterally elevated both the level of corticosterone in plasma and the central metabolism of dopamine, neither the parenteral administration of the kappa agonist, U50488H, or the intraventricular administration of dynorphin altered central metabolism of dopamine. However, in both cases, levels of corticosterone in plasma were dramatically elevated, clearly demonstrating the bioavailability of the kappa agonists. The actions of morphine on the metabolism of dopamine, which can be antagonized by pretreatment with synthetic kappa agonists, were not antagonized by dynorphin(1-13). To summarize, the present data indicated that the nigrostriatal dopaminergic pathway in the rat lacks kappa opioid regulation. In addition, while synthetic kappa agonists also possessed mu antagonist actions, the endogenous ligand, dynorphin, did not.


Assuntos
Corpo Estriado/metabolismo , Dopamina/metabolismo , Dinorfinas/farmacologia , Morfina/farmacologia , Fragmentos de Peptídeos/farmacologia , Substância Negra/metabolismo , Ácido 3,4-Di-Hidroxifenilacético/metabolismo , Animais , Corpo Estriado/efeitos dos fármacos , Corticosterona/sangue , Ácido Homovanílico/metabolismo , Masculino , Ratos , Ratos Endogâmicos , Substância Negra/efeitos dos fármacos
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