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Category: 7TM ReceptorsarrowAdrenergic ReceptorsarrowAlpha-1 ReceptorsarrowAntagonists
Cat.No. Product Name
2398 SNAP 5089
Price and Availability

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SNAP 5089
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

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.

Technical Data:

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M.Wt: 645.19
Formula: C36H40N4O5.HCl
Storage: Store at +4°C
Solubility: Soluble to 100 mM in DMSO and to 100 mM in Ethanol
Purity: >98%
CAS No: [157066-76-7]

Resources:

  • Certificate of Analysis / MSDS:

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

    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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