RS 17053 hydrochloride (Synonyms: RS-17053) |
Catalog No.GC17070 |
Le chlorhydrate de RS 17053 est un antagoniste puissant et sélectif des récepteurs adrénergiques α1A, avec une valeur de pKi de 9,1 dans la membrane cellulaire native et une valeur de pA2 de 9,8 dans les tests fonctionnels.
Products are for research use only. Not for human use. We do not sell to patients.
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.
Average Rating: 5
(Based on Reviews and 40 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *