Rispenzepine 

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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

336.39

C₁₉H₂₀N₄O₂

96449-05-7

O=C1C2=CC=CN=C2N(C(C3CN(C)CCC3)=O)C4=CC=CC=C4N1

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• [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.  [Content Brief]