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Category: 7TM ReceptorsarrowAcetylcholine (Muscarinic) ReceptorsarrowAntagonists
Cat.No. Product Name
2579 Zamifenacin fumarate
Alternative name(s): UK 76654
Price and Availability

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Zamifenacin
Chemical Name: (3R)-1-[2-(1-,3-Benzodioxol-5-yl)ethyl]-3-(diphenylmeth oxy)piperidine fumarate

Biological Activity:

Selective M3 muscarinic receptor antagonist (pKi values are 8.52, 7.93, 7.90 and 7.78 for M3, M2, M1 and M4 receptors respectively). Displays higher affinity at ileal M3 receptors (pKi = 9.3) compared to oesophageal and tracheal M3 receptors (pKi values are 8.8 and 8.2 respectively). In vivo, inhibits gastrointestinal motility in the absence of cardiovascular effects.

Technical Data:

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M.Wt: 531.6
Formula: C27H29NO3.C4H4O4
Storage: Desiccate at +4°C
Solubility: Soluble to 100 mM in DMSO and to 25 mM in Ethanol
Purity: >99%
CAS No: [127308-98-9]

Resources:

  • Certificate of Analysis / MSDS:

    Certificate of Analysis: View current batch
    Product/Material Safety Data Sheet: View current batch

    References:

    Wallis (1995) Pre-clinical and clinical pharmacology of selective muscarinic M3 receptor antagonists. Life Sci. 56 861. Watson et al (1995) Characterization of the interaction of zamifenacin at muscarinic receptors in vitro. Eur.J.Pharmacol. 285 135. Choppin (2002) Muscarinic receptors in isolated urinary bladder smooth muscle from different mouse strains. Br.J.Pharmacol. 137 522.
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    Keywords: Zamifenacin, Acetylcholine (Muscarinic) Receptors, Selective M3 Antagonist, UK 76654, Tocris Bioscience

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