alpha 1-adrenoceptor

BMY 7378 dihydrochloride (BMY7378 HCl) 是选择性 α1D 肾上腺素受体拮抗剂，也是5-HT1A 受体部分激动剂。它同表达克隆大鼠 α1D-AR 的膜结合的亲和力 (Ki=2 nM)  是同克隆大鼠 α1A-AR (Ki=800 nM) 或仓鼠 α1B-AR (Ki=600 nM) 结合的亲和力 的100 以上。

α1 adrenoceptor-MO-1（S 对映体）对α1肾上腺素受体具有亲和力，具有抗α-肾上腺素能和镇痛作用。α1 adrenoceptor-MO-1比R 对映体更具活性。

Arbutamine (GP 21213) 是一种新型非选择性β-肾上腺素受体激动剂，具有α-1-拟交感神经活性。Arbutamine 促进心脏应激，增加心率、心脏收缩力。Arbutamine 可用于研究心脏应激和冠状动脉疾病。

Bunazosin Hydrochloride (E 1015) 是一种 α(1)-adrenoceptor 拮抗剂，用作全身性抗高血压药和降眼压药。

Azepexole (B-HT 933) dihydrochloride 是一种有效的选择性α 2肾上腺素受体激动剂，对 α2A-、α2B- 和 α2C- 肾上腺素受体亚型的 pKi 分别为 8.3、7.6 和 7.5。Azepexole dihydrochloride 引起浓度依赖性的蠕动收缩抑制，IC50值为 78.72 nM。

Dilevalol, the RR-stereoisomer of labetalol, is a non-cardioselective beta-adrenoceptor antagonist with substantial partial beta 2-agonist and negligible alpha 1-blocking activity.

Abanoquil is an antagonist of alpha-1 adrenoceptor.

SKF 89748 is an agonists of alpha 1-adrenoceptor.

Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2 |1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., 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 II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997).

Indanidine hydrochloride is an alpha 1 adrenoceptor agonist.

Ocoteine is an alpha 1-adrenoceptor antagonist.

Dicentrine HCl is the salt form of Dicentrine, an alpha 1-adrenoceptor antagonist effective against human hyperplastic prostates.

DC 015 is a novel potent and selective alpha 1-adrenoceptor antagonist.

HSR-175 HCl is an alpha 1-adrenoceptor antagonist.

HV-723 fumarate is an alpha-1 adrenoceptor antagonist.

Beta-Yohimbine has approximately twice as toxic as yohimbine and corynanthine about one fifth as toxic. Beta-yohimbine has alpha-1 and alpha-2 adrenoceptor blocking activities, it has cardiovascular effects. Beta-Yohimbine has anti-plasmodial and anti-mal

l-Stephanine is a potent and highly selective alpha 1 adrenoceptor blocker, inhibits anococcygeus muscle contraction induced by phenylephrine with pA2 values of 6.76. Stephanine shows significant antiplasmodial activities with IC(50) ranged from 1.2 uM to 52.3 uM. Stephanine and crebanine have high inhibitory activity against gram-positive animal pathogenic bacteria, with MIC values of 0.078-0.312g l, but low inhibitory activity against gram-negative animal pathogenic bacteria, they also inhibit hyphal growth of the plant pathogens Cercospora kaki.