96449-05-7

96449-05-7 structure

Name: Rispenzepine
Chemical Name: 11-[(1-methyl-piperidine-3-yl)-carbonyl]-6,11-dihydro-5H-pyrido[2,3-b][1,5]-benzodiazepine-5-one
CAS Number: 96449-05-7
Molecular Formula: C₁₉H₂₀N₄O₂
Molecular Weight: 336.38800
Catalog: Signaling Pathways GPCR/G Protein mAChR
Create Date: 2016-10-14 14:44:44
Modify Date: 2024-01-09 12:20:31
Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.

Name	11-[(1-methyl-piperidine-3-yl)-carbonyl]-6,11-dihydro-5H-pyrido[2,3-b][1,5]-benzodiazepine-5-one
Synonyms	rispenzepine

Description	Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mAChR Signaling Pathways >> Neuronal Signaling >> mAChR Research Areas >> Neurological Disease
Target	M1, and M3 receptor[1]
In Vitro	The presence of muscarinic autoreceptors in human and guinea pig trachea is investigated by comparing the effects of the muscarinic receptor antagonists Pirenzepine (M1), Methoctramine (M2), 4-DAMP (M3), and Rispenzepine (M1/M3) on cholinergic neural contractile responses evoked by electrical field stimulation (EFS) and [3H]ACh release. The M1, M1/M3, or M3 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 M3 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; pD2 value of 7.31±0.15) [1].
References	[1]. Patel HJ, et al. Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea. Am J Respir Crit Care Med. 1995 Sep;152(3):872-8.