Upidosin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.

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 pA2 value of 8.74 compared to blood pressure with a pA2 value of 7.51.

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GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

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152735-23-4

511.61

C31H33N3O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (488.65 mM; 超声助溶 )

COc1ccccc1N1CCN(CCCNC(=O)c2cccc3c2oc(c(C)c3=O)-c2ccccc2)CC1

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(-20℃)

With Ice Pack

≥ 2 years