1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Zamifenacin

Zamifenacin (Synonyms: UK-76654)

Cat. No.: HY-123337
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Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.

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Zamifenacin Chemical Structure

Zamifenacin Chemical Structure

CAS No. : 127308-82-1

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Description

Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].

IC50 & Target

Muscarinic M3 receptor[1]

In Vivo

Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg)[2].
Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg)[2].

Animal Model: Male CDl mice (mean weight 23 g)[2]
Dosage: 5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (2.1 h).
Animal Model: Male and female CD rats (mean weight 210 g)[2]
Dosage: 5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h).
Animal Model: Male and two female beagle dogs (13-16 kg)[2]
Dosage: 1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h).
Molecular Weight

415.52

Formula

C₂₇H₂₉NO₃

CAS No.

127308-82-1

SMILES

N1(C[[email protected]@H](CCC1)OC(C2=CC=CC=C2)C3=CC=CC=C3)CCC4=CC5=C(C=C4)OCO5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ZamifenacinUK-76654UK76654UK 76654mAChRMuscarinic acetylcholine receptorgutmuscarinicM3colonicmotilityirritablebowelsyndromeInhibitorinhibitorinhibit

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