Basic information Safety Supplier Related

Rec 15-2739

Basic information Safety Supplier Related

Rec 15-2739 Basic information

Product Name:
Rec 15-2739
Synonyms:
  • 4H-1-Benzopyran-8-carboxamide, N-(3-(4-(2-methoxyphenyl)-1-piperazinyl)propyl)-3-methyl-4-oxo-2-phenyl-
  • Sb 216469-s
  • Unii-txg28R7G4y
  • Upidosin
  • Rec 15-2739
  • N-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]-3-methyl-4-oxo-2-phenylchromene-8-carboxamide
  • Recordati 15/2739
  • SB 216469
CAS:
152735-23-4
MF:
C31H33N3O4
MW:
511.61
Mol File:
152735-23-4.mol
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Rec 15-2739 Chemical Properties

Boiling point:
688.9±55.0 °C(Predicted)
Density 
1.208±0.06 g/cm3(Predicted)
storage temp. 
4°C, protect from light
pka
14.40±0.40(Predicted)
form 
Solid
color 
White to off-white
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Rec 15-2739 Usage And Synthesis

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].

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

Rec 15-2739Supplier

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