96449-05-7
96449-05-7 结构式
基本信息
Unii-W99llm73R7
Rispenzepine [inn]
5H-Pyrido[2,3-b][1,5]benzodiazepin-5-one, 6,11-dihydro-11-[(1-methyl-3-piperidinyl)carbonyl]-
11-[(1-methyl-piperidine-3-yl)-carbonyl]-6,11-dihydro-5H-pyrido[2,3-b][1,5]-benzodiazepine-5-one
常见问题列表
M 1 , and M 3 receptor
The presence of muscarinic autoreceptors in human and guinea pig trachea is investigated by comparing the effects of the muscarinic receptor antagonists Pirenzepine (M 1 ), Methoctramine (M 2 ), 4-DAMP (M 3 ), and Rispenzepine (M 1 /M 3 ) on cholinergic neural contractile responses evoked by electrical field stimulation (EFS) and [ 3 H]ACh release. The M 1 , M 1 /M 3 , or M 3 antagonists inhibit the EFS-evoked cholinergic contractile response in a concentration-dependent manner (4-DAMP > Rispenzepine > Pirenzepine), whereas Methoctramine facilitates this response at low concentrations (<3 μM). In ACh release studies, the M 3 antagonist has no significant effect, whereas Pirenzepine, Methoctramine, and Rispenzepine significantly increase ACh release in guinea pig trachea. Rispenzepine almost completely inhibits cholinergic, contractile responses at 0.3 μM (92.7±6.2% inhibition, n=6, p<0.05; pD 2 value of 7.31±0.15) .