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您的检索式：作者名="Devin HTaylor"
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| 1 | The impact of cannabinoid type 2 receptors(CB2Rs)in neuroprotection against neurological disorders显示文摘Cannabinoids have long been used for their psychotropic and possible medical properties of symptom relief.In the past few years,a vast literature shows that cannabinoids are neuroprotective under different pathological situations.Most of the effects of cannabinoids are mediated by the well-characterized cannabinoid receptors,the cannabinoid type 1 receptor(CB1R)and cannabinoid type 2 receptor(CB2R).Even though CB1Rs are highly expressed in the central nervous system(CNS),the adverse central side effects and the development of tolerance resulting from CB1R activation may ultimately limit the clinical utility of CB1R agonists.In contrast to the ubiquitous presence of CB1Rs,CB2Rs are less commonly expressed in the healthy CNS but highly upregulated in glial cells under neuropathological conditions.Experimental studies have provided robust evidence that CB2Rs seem to be involved in the modulation of different neurological disorders.In this paper,we summarize the current knowledge regarding the protective effects of CB2R activation against the development of neurological diseases and provide a perspective on the future of this field.A better understanding of the fundamental pharmacology of CB2R activation is essential for the development of clinical applications and the design of novel therapeutic strategies. | Qing Xin Fei Xu Devin HTaylor Jing-fu Zhao Jie Wu | 2020 | Acta Pharmacologica Sinica2020，41，12： | 1 |
| 2 | Levo-tetrahydropalmatine inhibits α4β2 nicotinic receptor response to nicotine in cultured SH-EP1 cells显示文摘Nicotine, a major component of tobacco, is highly addictive and acts on nicotinic acetylcholine receptors (nAChRs) to stimulate reward-associated circuits in the brain. It is well known that nAChRs play critical roles in mediating nicotine reward and addiction. Current FDA-approved medications for smoking cessation are the antidepressant bupropion and the nicotinic partial agonist varenicline, yet both are limited by adverse side effects and moderate efficacy. Thus, development of more efficacious medications with fewer side effects for nicotine addiction and smoking cessation is urgently needed. l-Tetrahydropalmatine (l-THP) is an active ingredient of the Chinese medicinal herb Corydalis ambigua that possesses rich neuropharmacological actions on dopamine (DA) receptors in the mesocorticolimbic dopaminergic reward pathway. L-THP has been explored as anti-addiction treatments for drug abuse including nicotine. However, the targets and mechanisms of l-THP-caused anti-nicotine effects are largely unknown. In this study we address this question by elucidating the effects of l-THP on human neuronal nAChRs using patch-clamp recordings. Human neuronal α4β2-nAChRs were heterologously expressed in SH-EP1 human epithelial cells. Bath application of nicotine (0.1–100 μM) induced inward currents, co-application of l-THP (3 μM) inhibited nicotine-induced currents in the transfected cells. L-THP-caused inhibition was concentration-dependent (the EC50 values for inhibiting the peak and steady-state current were 18 and 2.1 μM, respectively) and non-competitive. Kinetic analysis of the whole-cell currents showed that l-THP slowed rising time and accelerated decay time constants. L-THP specifically modulated α4β2-nAChRs, as it did not affect α7-nAChRs or α1*-nAChRs (muscle type). Interestingly, two putative α4β2-nAChR isoforms, namely sazetidine A-activated, high-sensitive one (α42β23-nAChR) and cytisine-activated, low-sensitive one (α43β22-nAChR) were pharmacologically separated, and the low-sensitive one was more susceptible to l-THP inhibition than the high-sensitive one. In conclusion, we demonstrate that l-THP blocks neuronal α4β2-nAChR function, which may underlie its inhibition on nicotine addiction. | Yuan-bing Huang Ze-gang Ma Chao Zheng Xiao-kuang K.Ma Devin HTaylor Ming Gao Ronald J.Lukas Jie Wu | 2022 | Acta Pharmacologica Sinica2022，43，4： | 0 |
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