HTL9936相较于其他两种M1受体激动剂77-LH-28-1和GSK1034702而言,具有更广泛稳定的结合模式,重要的是在人M2、M3、M5受体上未表现出可检测到的激动作用,而在M4受体上仅观察到部分激动剂活性。大鼠海马切片的电生理记录表明,HTL9936增加了CA1...
HTL9936相较于其他两种M1受体激动剂77-LH-28-1和GSK1034702而言,具有更广泛稳定的结合模式,重要的是在人M2、M3、M5受体上未表现出可检测到的激动作用,而在M4受体上仅观察到部分激动剂活性。大鼠海马切片的电生理记录表明,HTL9936增加...
Doods HN, Mathy MJ, Davidesko D, van Charldorp KJ, de Jonge A, van Zwieten PA. Selectivity of muscarinic antagonists in radioligand and in vivo experiments for the putative M1, M2 and M3 receptors. J Pharmacol Exp Ther. 1987; 242 :257–262....
Instead, the data offer evidence for the presence of M3 receptors localized to the same areas where M1 receptors previously had been suggested to be present (Gillberg et al., 1988; Villiger and Faull, 1985). The distribution of M2 binding sites corresponds well to previous results (Villiger ...
While the M1, M2, M3 and M6 remained highly active while respecting ADMET's characteristics. Molecular docking results showed compound M2 better with acetylcholinesterase than compound 22. The interactions are classical hydrogen bonding with residues TYR:124, TYR:72, and SER:293, which play a ...
Muscarinic receptors have an important role in the regulation of human nasal glandular secretion and mucus production, but it is not known which of the five muscarinic receptor subtypes are involved. The effect of nonselective and M1-, M2-, and M3-selective muscarinic antagonists on methacholine ...
靶点 M1 receptor x M2 receptor x M3 receptor x M4 receptor x M5 receptor x β2-adrenergic receptor 作用机制 M1 receptor拮抗剂 [+5] 在研机构 GlaxoSmithKline (Ireland) Ltd. [+3] 原研机构 GSK Plc 在研适应症 慢性阻塞性肺疾病 非在研适应症- 最高研发阶段批准上市 首次获批国家/地区 美国 ...
Rat thoracic spinal cord contains M2, M3, and M4 but not M1, muscarinic (mAChR) subtypes A. Hglund,H Baghdoyan 被引量: 0发表: 1996年 Characterization of Muscarinic Receptor Subtypes That Mediate Antinociception in the Rat Spinal Cord Spinal cholinergic receptors are involved in mediating antinoc...
a通常,阿托品作为麻醉前用药减少腺体分泌,但是阿托品是非选择性M受体阻滞药,使用后增加心率,增加心肌耗氧,而长托宁选择性作用于M1,M3受体,对M2受体几乎没有作用,不增加心脏氧耗,可以比较安全用于老年患者和心肌缺血患者。 Usually, the atropine took before the anaesthesia applies drugs the reduced gland secretion,...
Here, we show that all muscarinic acetylcholine receptors (M1-M5) are expressed in mouse brain microvascular endothelial cells. The mRNA expression of M2, M3, and M5correlates with their respective protein abundance, but a mismatch exists for M1and M4mRNA versus protein levels. Acetylcholine ...