<Suppliers Price>

Rispenzepine

Names

[ CAS No. ]:
96449-05-7

[ Name ]:
Rispenzepine

[Synonym ]:
rispenzepine

Biological Activity

[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.


[Related Small Molecules]

Carbachol | Darifenacin HBr | Arecoline hydrobromide | Pirenzepine, Dihydrochloride | Glycopyrrolate | Imidafenacin | Benztropine Mesylate | Xanomeline oxalate | Batefenterol | Bethanechol chloride | Cevimeline hydrochloride hemihydrate | Otilonium Bromide | solifenacin | VU0467154 | Anisodamine

Chemical & Physical Properties

[ Molecular Formula ]:
C19H20N4O2

[ Molecular Weight ]:
336.38800

[ Exact Mass ]:
336.15900

[ PSA ]:
70.99000

[ LogP ]:
2.35990

[ Storage condition ]:
2-8℃


Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.