RS 17053 hydrochloride
(Synonyms: RS-17053) 目录号 : GC17070
An α1A-adrenergic receptor antagonist
Cas No.:169505-93-5
Sample solution is provided at 25 µL, 10mM.
RS 17053 hydrochloride is a novel and selective α1A-adrenoceptor antagonist [1].
α1A-adrenoceptor are widely distributed and activated either by epinephrine released from the adrenal medulla or by norepinephrine released from sympathetic nerve terminals. α1A-adrenoceptor mediate a variety of functions, including cardiac stimulation, contraction of smooth muscle, activation of hepatic gluconeogenesis, glycogenolysis, cellular proliferation and apoptosis.
In rat several tissues, RS-17053 had high affinity for the α1A -adrenoceptor and a 30 ~100-fold selectivity over the α1B - and the α1D -adrenoceptor subtypes [1]. RS 17053 had over 100-fold lower affinity for the α1A -adrenoceptor mediating contraction of the rat portal vein (pKB 7.1) and human prostate (pKB 7.1) compared with its affinity for the α1A -adrenoceptor in the rat epididymal vas deferens or the expressed α1A -clone. Therefore, RS 17053 may distinguish between subtypes of the α1A -adrenoceptor in the rat portal vein and human prostate compared with those in the rat epididymal vas deferens or the expressed α1A -clones [2].
References:
[1]. Ford AP, Arredondo NF, Blue DR Jr, et al. RS 17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine hydrochloride, a selective α1A-adrenoceptor antagonist, displays low affinity for functional α1-adrenoceptors in human prostate: implications for adrenoceptor classification. Mol Pharmacol, 1996, 49(2): 209-215.
[2]. Marshall I, Burt RP, Green GM, et al. Different subtypes of α1A-adrenoceptor mediating contraction of rat epididymal vas deferens, rat hepatic portal vein and human prostate distinguished by the antagonist RS 17053. Br J Pharmaco, 1996, 119(2): 407-415.
Animal experiment: | Rats[2]Adult male rats (n=56 to 8 per group) are pretreated (IP) with either 0, 0.1, 0.5, 2.5, or 10.0 mg/kg RS 17053 hydrochloride or with 2.0 mg/kg of the prototypical α1-Adrenoceptor antagonist prazosin. Five minutes later, each rat was treated (IP) with either 0, 5, 10 or 15 mg/kg PPA. Food and water intakes are recorded for a 30 min period starting 10 min after the treatment injection. Rats pretreated with vehicle and then treated with PPA exhibite a dose-dependent suppression of feeding with a maximal effect evident at the 15 mg/kg dose of PPA. Pretreatment with 2.0 mg/kg prazosin reverses the anorexic activity of PPA[2]. |
References: [1]. Ford AP, et al. RS-17053 (N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha, alpha-dimethyl-1H-indole-3-ethanamine hydrochloride), a selective alpha 1A-adrenoceptor antagonist, displays low affinity for functional alpha 1-adrenoceptors in human prostate: implications for adrenoceptor classification. Mol Pharmacol. 1996 Feb;49(2):209-15. |
Cas No. | 169505-93-5 | SDF | |
别名 | RS-17053 | ||
化学名 | 1-(5-chloro-1H-indol-3-yl)-N-(2-(2-(cyclopropylmethoxy)phenoxy)ethyl)-2-methylpropan-2-amine hydrochloride | ||
Canonical SMILES | CC(CC1=CNC2=C1C=C(Cl)C=C2)(NCCOC3=CC=CC=C3OCC4CC4)C.Cl | ||
分子式 | C24H29N2O2Cl.HCl | 分子量 | 449.42 |
溶解度 | <22.47mg/ml in DMSO | 储存条件 | Store at RT |
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1 mg | 5 mg | 10 mg |
1 mM | 2.2251 mL | 11.1255 mL | 22.2509 mL |
5 mM | 0.445 mL | 2.2251 mL | 4.4502 mL |
10 mM | 0.2225 mL | 1.1125 mL | 2.2251 mL |
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