five

CHRM1,3,5 bind CHRM1,3,5 antagonists

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reactome.org2025-01-15 收录
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A muscarinic receptor (CHRM) antagonist is a type of anticholinergic agent that blocks the activity of human muscarinic acetylcholine receptors 1-5 (Caulfield & Birdsall 1998, Dorje et al. 1991, Bolden & Richelson 1992). Muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often described as "rest-and-digest", and includes slowing of the heart, narrowing of airways, an increased digestion rate, promotion of urination, and sexual arousal. Most muscarinic antagonists are synthetic but two of the most commonly used ones are belladonna alkaloids (from deadly nightshade plants), namely scopolamine and atropine. Scopolamine is used to treat motion sickness (Golding & Gresty 2015) whereas atropine can counter organophosphate poisoning (Bajracharya et al. 2016). Both are used for comsetic purposes to promote pupil dilation (Tran et al. 2018).<br><br>Muscarinic antagonists are widely used in the treatment of low heart rate (Harvey 2012), overactive bladder (Nadeau et al. 2014, Franco et al. 2020), peptic and gastric ulcers (Ehlert et al. 2012, Shamburek & Schubert 1993), asthma and COPD (Alagha et al. 2014), and neurological problems such as Parkinson's disease (Ztaou & Amalric 2019) and Alzheimer's disease (Clader & Wang 2005).

一种毒蕈碱受体(CHRM)拮抗剂属于抗胆碱能药物类别,该药物能够阻断人类毒蕈碱乙酰胆碱受体1-5(Caulfield & Birdsall 1998,Dorje et al. 1991,Bolden & Richelson 1992)的活性。毒蕈碱拮抗剂可降低副交感神经系统的激活。副交感神经系统的正常功能常被描述为“休息与消化”,包括心率减慢、气道狭窄、消化速率增加、促进排尿以及性唤起。大多数毒蕈碱拮抗剂为合成制剂,但其中最常用的两种为颠茄生物碱(来自致命的曼陀罗植物),即阿托品和莨菪碱。阿托品用于治疗晕动症(Golding & Gresty 2015),而莨菪碱则可对抗有机磷中毒(Bajracharya et al. 2016)。两者均用于美容目的以促进瞳孔扩张(Tran et al. 2018)。毒蕈碱拮抗剂在治疗低心率(Harvey 2012)、过度活跃的膀胱(Nadeau et al. 2014,Franco et al. 2020)、消化性溃疡和胃溃疡(Ehlert et al. 2012,Shamburek & Schubert 1993)、哮喘和慢性阻塞性肺疾病(Alagha et al. 2014)以及神经性疾病,如帕金森病(Ztaou & Amalric 2019)和阿尔茨海默病(Clader & Wang 2005)中应用广泛。
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