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Category:
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7TM Receptors Acetylcholine (Muscarinic) ReceptorsAntagonists
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Cat.No.
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Product Name
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2507 |
J 104129 fumarate
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Price and Availability
Click here for full price details of
J 104129
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Chemical Name:
(aR)-a-Cyclopentyl-a-hydroxy-N-[1-(4-methyl-3-pentenyl)
-4-piperidinyl]benzeneacetamide fumarate |
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Biological Activity:
Potent
M3 muscarinic receptor antagonist that displays ~ 120-fold
selectivity over M2 receptors (Ki values are 4.2, 19 and
490 nM for human M3, M1 and M2 receptors
respectively). Exhibits > 250-fold bronchial selectivity; inhibits
ACh-induced bronchoconstriction but not ACh-induced bradycardia (KB
values are 3.3 and 170 nM for rat trachea M3 and rat right atria M2
receptors respectively).
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Mitsuya et al (1999) J-104129, a
novel muscarinic M3 receptor antagonist with high selectivity for M3
over M2 receptors. Bioorg.Med.Chem. 7 2555. Mitsuya
et al (1999) Stereoselective synthesis of a new muscarinic M3
receptor antagonist, J-104129. Bioorrg.Med.Chem.Lett. 9 2037. Mitsuya
et al (2000) Discovery of a muscarinic M3 receptor antagonist
with high selectivity for M3 over M2 receptors among
2-[(1S,3S)-3-sulfonylaminocyclopentyl]phenylacetamide
derivatives. Bioorg.Med.Chem. 8 825.
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Keywords: J 104129, Acetylcholine (Muscarinic) Receptors, Potent, Selective M3 Antagonist, J104129, Tocris Bioscience
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