A muscarinic M3 receptor antagonist
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Zamifenacin (fumarate)

Item No. 32848

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R)-1-[2-(1,3-benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)-piperidine, (2E)-2-butenedioate
CAS Number
127308-98-9
Synonyms
  • UK 76654
Molecular Formula
C27H29NO3 • C4H4O4
Formula Weight
531.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/mlEthanol: 20 mg/ml
SMILES
OC(/C=C/C(O)=O)=O.C(C1=CC=CC=C1)(C2=CC=CC=C2)O[C@H]3CN(CCC3)CCC4=CC=C(OCO5)C5=C4
InChi Code
InChI=1S/C27H29NO3.C4H4O4/c1-3-8-22(9-4-1)27(23-10-5-2-6-11-23)31-24-12-7-16-28(19-24)17-15-21-13-14-25-26(18-21)30-20-29-25;5-3(6)1-2-4(7)8/h1-6,8-11,13-14,18,24,27H,7,12,15-17,19-20H2;1-2H,(H,5,6)(H,7,8)/b;2-1+/t24-;/m1./s1
InChi Key
PMHKTAIGYOVZEZ-ZHWJIHCSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $186

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    Product Description

    Zamifenacin is an antagonist of M3 muscarinic acetylcholine receptors (Ki = 10 nM for the human receptor).1 It is selective for M3 over M1, M2, M4, and M5 receptors in radioligand binding assays using cells expressing recombinant human receptors (Kis = 55, 153, 68, and 34 nM, respectively). Zamifenacin inhibits cholecystokinin-induced small bowel motility (ED50 = 0.9 mg/kg) but does not increase heart rate (ED150 = 80.0 mg/kg) in dogs.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Moriya, H., Takagi, Y., Nakanishi, T., et al. Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland. Life Sci. 64(25), 2351-2358 (1999).

    2. Wallis, R.M. Pre-clinical and clinical pharmacology of selective muscarinic M3 receptor antagonists. Life Sci. 56(11-12), 861-868 (1995).