Rispenzepine

Modify Date: 2024-01-09 12:20:31

Rispenzepine Structure
Rispenzepine structure
Common Name Rispenzepine
CAS Number 96449-05-7 Molecular Weight 336.38800
Density N/A Boiling Point N/A
Molecular Formula C19H20N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Rispenzepine


Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.

 Names

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

 Rispenzepine Biological Activity

Description Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.
Related Catalog
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.

 Chemical & Physical Properties

Molecular Formula C19H20N4O2
Molecular Weight 336.38800
Exact Mass 336.15900
PSA 70.99000
LogP 2.35990
Storage condition 2-8℃

 Synonyms

rispenzepine