A muscarinic M1 receptor antagonist
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Pirenzepine (hydrochloride)

Item No. 29527

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,11-dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, dihydrochloride
CAS Number
29868-97-1
Synonyms
  • Gastrozepin
Molecular Formula
C19H21N5O2 • 2HCl
Formula Weight
424.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): 10 mg/ml
λmax
280 nm
SMILES
O=C1NC2=C(N=CC=C2)N(C(CN3CCN(C)CC3)=O)C4=C1C=CC=C4.Cl.Cl
InChi Code
InChI=1S/C19H21N5O2.2ClH/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24;;/h2-8H,9-13H2,1H3,(H,21,26);2*1H
InChi Key
FFNMBRCFFADNAO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 mg

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    1 g

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    5 g

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    Product Description

    Pirenzepine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 11.48 nM).1 It is selective for M1 over M2, M3, and M4 receptors (Kis = 602.56, 151.36, and 199.53 nM, respectively). Pirenzepine inhibits ascending reflex contraction of the circular smooth muscle in isolated guinea pig ileal segments induced by intraluminal balloon inflation (IC50 = 501.19 nM). It inhibits methacholine-induced increases in ileal pressure in guinea pigs (ID50 = 724.44 nmol/kg). Pirenzepine inhibits oxotremorine-induced gastric ulcer, gastric acid secretion, and salivation in rats (ED50s = 13, 37.5, and 620 μg/kg i.v., respectively).2 It prevents form-deprivation myopia (FDM) in a chick model of experimental myopia.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Doods, H.N., Entzeroth, M., Ziegler, H., et al. Pharmacological profile of selective muscarinic receptor antagonists on guinea-pig ileal smooth muscle. Eur. J. Pharmacol. 253(3), 275-281 (1994).

    2. Del Soldato, P., and Pagani, F. Pharmacodynamic evaluation of selective antimuscarinic properties of pirenzepine in the rat. Pharmacol. Res. Commun. 14(3), 279-287 (1982).

    3. Luft, W.A., Ming, Y., and Stell, W.K. Variable effects of previously untested muscarinic receptor antagonists on experimental myopia. Invest. Ophthalmol. Vis. Sci. 44(3), 1330-1338 (2003).