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Category:
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7TM Receptors Adrenergic Receptors Alpha-1 Receptors Antagonists
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Cat.No.
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Product Name
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2398 |
SNAP 5089
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Price and Availability
Click here for full price details of
SNAP 5089
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Chemical Name:
5-[[[3-(4,4-Diphenyl-1-piperidinyl)propyl]amino]carbony
l]-1,4-dihydro-2,6-dimethyl-4-(4-nitrophenyl)-3-pyridin
ecarboxylic acid methyl ester hydrochloride |
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Biological Activity:
Subtype selective α1A-adrenoceptor
antagonist that displays > 600-fold selectivity over other adrenoceptors (Ki
values are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B
and α2A
subtypes respectively and 540 nM for L-type Ca2+ channels). Inhibits
noradrenaline-induced contractions in rabbit vascular and lower urinary
tissues.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Wetzel et al
(1995) Discovery of α1a-adrenergic
receptor antagonists based on the L-type Ca2+ channel antagonist
niguldipine. J.Med.Chem. 38 1579. Leonardi et al
(1997) Pharmacological characterization of the uroselective alpha-1
antagonist Rec 15-2739 (SB 216469): role of the alpha-1L adrenoceptor in
tissue selectivity, Part I. J.Pharmacol.Exp.Ther. 281 1272. Kava
et al (1998) α1L-adrenceptor
mediation of smooth muscle contraction in rabbit bladder neck: a model for
lower urinary tract tissues of man. Br.J.Pharmacol. 123 1359.
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Keywords: SNAP 5089, Adrenergic Receptors, Subtype Selective A1A-adrenoceptor Antagonist, Tocris Bioscience
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