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1.
J Pharmacol Exp Ther ; 377(1): 20-28, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33431609

RESUMO

Treatment of chronic pain remains an unmet medical need. The neuronal voltage-gated potassium Kv7/KCNQ/M channel has been implicated as a therapeutic target for chronic pain. However, whether pharmacological activation of the Kv7 channel can alleviate pain remains elusive. In this study, we show that selective activation of native M-currents by a novel channel opener SCR2682 reduces repetitive firings of dorsal root ganglia (DRG) sensory neurons. Intraperitoneal administration of SCR2682 relieves mechanical allodynia and thermal hyperalgesia in rat models of pain induced by complete Freund's adjuvant (CFA) or spared nerve injury (SNI) in a dose-dependent manner without affecting locomotor activity. The antinociceptive efficacy of SCR2682 can be reversed by the channel-specific blocker XE991. Furthermore, SCR2682 increases Kv7.2/KCNQ2 mRNA and protein expression in DRG neurons from rats in the SNI model of neuropathic pain. Taken together, pharmacological activation of neuronal Kv7 channels by opener SCR2682 can alleviate pain in rats, thus possessing therapeutic potential for chronic pain or hyperexcitability-related neurologic disorders. SIGNIFICANCE STATEMENT: A novel voltage-gated potassium Kv7 channel opener SCR2682 inhibits action potential firings in dorsal root ganglia sensory neurons and exhibits efficacy in antinociception, thus possessing a developmental potential for treatment of chronic pain or epilepsy.


Assuntos
Analgésicos/uso terapêutico , Dor Crônica/tratamento farmacológico , Canal de Potássio KCNQ2/metabolismo , Moduladores de Transporte de Membrana/uso terapêutico , Piridinas/uso terapêutico , Potenciais de Ação , Analgésicos/farmacologia , Animais , Células Cultivadas , Gânglios Espinais/efeitos dos fármacos , Gânglios Espinais/metabolismo , Gânglios Espinais/fisiologia , Canal de Potássio KCNQ2/agonistas , Masculino , Moduladores de Transporte de Membrana/farmacologia , Piridinas/farmacologia , Ratos , Ratos Sprague-Dawley
2.
Artigo em Inglês | MEDLINE | ID: mdl-21806504

RESUMO

We report the application of Vitamin D3 (VD(3)) in nanoparticles of oleoyl alginate ester (OAE)(OAE-VD(3)). The internalization of fluorescent OAE-VD(3) by Caco-2 cells was visualized by confocal laser scanning microscopy. In vivo pharmacokinetic studies showed that incorporation into OAE nanoparticles resulted in increased absorption of VD(3). Its application in the treatment of rickets was assayed using a model of nutritionally induced vitamin D-deficiency rickets. The results showed that the encapsulated VD(3) had better efficacy than that of the free drug in vivo. Our studies provide evidence that OAE nanoparticles are valuable as nutraceutical delivery vehicles to enhance the absorption of VD(3).


Assuntos
Alginatos/química , Colecalciferol , Suplementos Nutricionais , Portadores de Fármacos/química , Interações Hidrofóbicas e Hidrofílicas , Nanopartículas/química , Administração Oral , Animais , Transporte Biológico , Densidade Óssea/efeitos dos fármacos , Células CACO-2 , Cápsulas , Colecalciferol/administração & dosagem , Colecalciferol/farmacocinética , Colecalciferol/farmacologia , Portadores de Fármacos/metabolismo , Fêmur/efeitos dos fármacos , Fêmur/fisiologia , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Humanos , Masculino , Camundongos , Ratos
3.
Zhong Xi Yi Jie He Xue Bao ; 5(4): 383-91, 2007 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-17631800

RESUMO

OBJECTIVE: To study the efficacy and safety of Yiqi Tongmai Oral Liquid (YQTM), a traditional compound Chinese herbal medicine, in treating angina pectoris in patients with coronary heart disease. METHODS: A multicentric, randomized, double blinded and paralleled controlled trial was conducted on 110 patients in trial group treated with YQTM, and 109 patients in control group treated with Shuxin Oral Liquid (SX). Cure and effective rates in both groups were evaluated. Frequency and duration of angina attack were counted and measured. Coronary angiography (CAG), electrocardiogram (ECG) and flat exercise test were taken in both groups. Blood lipid indexes, such as cholesterol (CH), triglyceride (TG), low-density lipoprotein (LDL), high density lipoprotein (HDL), were determined at pre- and post-treatment. The hemodynamic indexes, such as whole blood viscosity (J2), high-shear reduced viscosity (Eh), low-shear reduced viscosity (Ei), red cell aggregation index (Lb), red cell rigidity index (Rh), fibrinogen (Fb), blood sedimentation rate (BSR) and hematocrit (HCT), were determined at pre-and post-treatment. The indicated scores of symptoms and signs of traditional Chinese medicine (TCM) pattern, such as chest pain, chest constriction, breath shortness, palpitation, fatigue, dim complexion, spontaneous perspiration and tongue proper, tongue coating were evaluated in week 0, 1, 2, 3, 4 during the treatment course. The safety indexes, such as body temperature, pulse, respiration and blood pressure were observed. Routine tests of blood, urine and stool, hepatic function test and renal function test were taken at pre- and post-treatment. RESULTS: There was no significant difference between the total effective rate of the trial group and that of the control group, which were 91.82% and 85.32%, respectively (P>0.05). Trial groups percentile of cure rate is significantly higher than that of the control group (P<0.01). The frequency and duration of angina attack, the positive ratio of CAG and flat exercise test of both groups were lowered, while the effect of the trial group on frequency and duration of angina attack was better. No significant difference was found in ECG features between the two groups (P>0.05). The levels of CH, TG and LDL of both groups were lowered significantly (P<0.05). The effect of lowering CH, TG and LDL of the trial group was stronger than that of the control group (P<0.05). The hemodynamic indexes, such as J2, Eh, Ei, Lb, Rh, Fb, BSR and HCT were improved significantly in both groups (P<0.05). The improvements of J2, Eh, Ei, Lb, Rh, Fb and SR in the trial group were greater than those of control group (P<0.05). The TCM symptoms and signs, such as chest pain, chest constriction, breath shortness, palpitation, fatigue, dim complexion, spontaneous perspiration were improved significantly in both groups (P<0.05). The improvements of chest constriction, palpitation, fatigue and spontaneous perspiration in the trial group were greater than those of the control group (P<0.05). The total indicated score of TCM symptoms and signs was lowered more significantly than that of the control group (P<0.01). No significant changes were found at pre- and post-treatment in safety indexes, such as routine tests for blood, urine and stool, hepatic function test and renal function test. There was no significant difference in safety features of both groups (P>0.05). CONCLUSION: Yiqi Tongmai Oral Liquid bears good therapeutic effect on angina pectoris without adverse reaction, and is superior to Shuxin Oral Liquid. Yiqi Tongmai Oral Liquid is a new effective and safe medicine for the treatment of angina pectoris in patients with coronary heart disease.


Assuntos
Angina Pectoris/tratamento farmacológico , Doença das Coronárias/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Medicina Tradicional Chinesa , Fitoterapia , Adulto , Idoso , Angina Pectoris/etiologia , Angiografia Coronária , Doença das Coronárias/complicações , Diagnóstico Diferencial , Método Duplo-Cego , Eletrocardiografia , Teste de Esforço , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Resultado do Tratamento
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