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Upidosin

目录号: PL14239 纯度: ≥99%

Upidosin (Rec 15/2739) 是 α-1 肾上腺素受体 (α-1 AR) 拮抗剂。Upidosin 具有对 α-1A AR 亚型的中等选择性。Upidosin 具有尿选择性，在尿道和前列腺有更高的亲和力，Kb 值为 2-3 nM，在耳动脉和主动脉的 Kb 值为 20-100 nM。Upidosin 抑制 [3H]prazosin 与人 α-1A 肾上腺素受体结合。Upidosin 可用于尿道梗阻的研究。

CAS No. :152735-23-4

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中文名称	Upidosin
英文名称	Upidosin
英文别名	4H-1-Benzopyran-8-carboxamide,N-[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]-3-methyl-4-oxo-2-phenyl-;N-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]-3-methyl-4-oxo-2-phenylchromene-8-carboxamide;AC1L3XX2;ACMC-20n6iu;Rec 15-2739;Rec-15-2739;SB 216469-S;UNII-TXG28R7G4Y;UPIDOSIN
Cas No.	152735-23-4
分子式	C₃₁H₃₃N₃O₄
分子量	511.61
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
详情描述	Upidosin (Rec 15/2739) 是 α-1 肾上腺素受体 (α-1 AR) 拮抗剂。Upidosin 具有对 α-1A AR 亚型的中等选择性。Upidosin 具有尿选择性，在尿道和前列腺有更高的亲和力，Kb 值为 2-3 nM，在耳动脉和主动脉的 Kb 值为 20-100 nM。Upidosin 抑制 [3H]prazosin 与人 α-1A 肾上腺素受体结合。Upidosin 可用于尿道梗阻的研究。

产品详情	Upidosin (Rec 15/2739) 是 α-1 肾上腺素受体 (α-1 AR) 拮抗剂。Upidosin 具有对 α-1A AR 亚型的中等选择性。Upidosin 具有尿选择性，在尿道和前列腺有更高的亲和力，K_b 值为 2-3 nM，在耳动脉和主动脉的 K_b 值为 20-100 nM。Upidosin 抑制 [3H]prazosin 与人 α-1A 肾上腺素受体结合。Upidosin 可用于尿道梗阻的研究。
生物活性	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 K b value of 2-3 nM higher than in ear artery and aorta with a K b 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.
性状	Solid
体外研究(In Vitro)	Upidosin is one of the most potent compounds action on the prostate with comparing the apparent pKB values, but its potency is slightly lower than that of tamsulosin and is higher than the potencies of prazosin, terazosin and 5-methylurapidil. Upidosin shows binding affinities to cloned humanα1A, humanα1B, humanα1D adrenoceptors with pKi value of 9.0, 7.5 and 8.6, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Upidosin shows greater selectivity than any other α-1 AR antagonist terazosin and tamsulosin in the anesthetized dog. Upidosin (1-300 μg/kg; i.v.) is a more potent antagonist of phenylephrine mediated increases in prostatic pressure with a pA 2 value of 8.74 compared to blood pressure with a pA 2 value of 7.51. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献	[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. [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.

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[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.
[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.

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