| Identification | Back Directory | [Name]
Rec 15-2739 | [CAS]
152735-23-4 | [Synonyms]
Upidosin
Rec 15-2739
Sb 216469-s
Unii-txg28R7G4y
N-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]-3-methyl-4-oxo-2-phenylchromene-8-carboxamide
4H-1-Benzopyran-8-carboxamide, N-(3-(4-(2-methoxyphenyl)-1-piperazinyl)propyl)-3-methyl-4-oxo-2-phenyl- | [Molecular Formula]
C31H33N3O4 | [MOL File]
152735-23-4.mol | [Molecular Weight]
511.61 |
| Chemical Properties | Back Directory | [Boiling point ]
688.9±55.0 °C(Predicted) | [density ]
1.208±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [form ]
Solid | [pka]
14.40±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction[1]. | [in vivo]
Upidosin shows greater selectivity than any other α-1 AR antagonist terazosin and tamsulosin in the anesthetized dog[1].
Upidosin (1-300 μg/kg; i.v.) is a more potent antagonist of phenylephrine mediated increases in prostatic pressure with a pA2 value of 8.74 compared to blood pressure with a pA2 value of 7.51[3]. | [storage]
4°C, protect from light | [References]
[1] Leonardi A, et al. 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. 1997 Jun;281(3):1272-83. PMID:9190863
[2] Testa R, et al. Functional antagonistic activity of Rec 15/2739, a novel alpha-1 antagonist selective for the lower urinary tract, on noradrenaline-induced contraction of human prostate and mesenteric artery. J Pharmacol Exp Ther. 1996 Jun;277(3):1237-46. PMID:8667184
[3] Kenny BA, et al. Evaluation of the pharmacological selectivity profile of alpha 1 adrenoceptor antagonists at prostatic alpha 1 adrenoceptors: binding, functional and in vivo studies. Br J Pharmacol. 1996 Jun;118(4):871-8. DOI:10.1111/j.1476-5381.1996.tb15480.x |
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