Catalog Number: 2398
Chemical Name: 5-[[[3-(4,4-Diphenyl-1-piperidinyl)propyl]amino]carbonyl]-1,4-dihydro-2,6-dimethyl-4-(4-nitrophenyl)-3-pyridinecarboxylic acid methyl ester hydrochloride
Biological Activity
Subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues 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 noradrenalin-induced contractions in rabbit vascular and lower urinary tissues.
Technical Data
  • M.Wt:
    645.19
  • Formula:
    C36H40N4O5.HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    157066-77-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Discovery of α1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
    Wetzel et al.
    J.Med.Chem., 1995;38:1579
  2. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15-2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, Part I.
    Leonardi et al.
    J.Pharmacol.Exp.Ther., 1997;281:1272
  3. α1L-adrenceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man.
    Kava et al.
    Br.J.Pharmacol., 1998;123:1359

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