RS 17053 hydrochloride

Research use only, not for human use.

RS 17053 hydrochloride is an effective and selective antagonist of α1A-adrenergic receptor with pA2 of 9.8 in functional assays and pKi of 9.1 in the native cell membrane.

RS 17053 hydrochloride is an effective and selective antagonist of α1A-adrenergic receptor with pA2 of 9.8 in functional assays and pKi of 9.1 in the native cell membrane.(In Vitro):RS 17053 hydrochloride antagonizes responses to NE only at high concentrations in isolated smooth muscle preparations from human LUT tissues. RS 17053 hydrochloride displays a high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8) in several tissues from rat and cloned adrenoceptors .(In Vivo):RS 17053 hydrochloride has a rapid onset of action and a duration of action exceeding 60 min. RS-17053 (10 mg/kg ) significantly suppresses food intake. RS 17053 hydrochloride pretreatment obviously alters food intake .

In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8). However, in isolated smooth muscle preparations from human LUT tissues, RS 17053 hydrochloride antagonizes responses to NE only at high concentrations. Estimates of affinity (pA2) at α1-adrenoceptors mediating NE-induced contractions are 7.5 in prostatic periurethral longitudinal smooth muscle (compared with 8.6 for prazosin), 6.9 in anterior fibromuscular stroma (prazosin, 8.9), and 7.1 in bladder neck (prazosin, 8.5).

RS 17053 hydrochloride has a rapid onset of action, and a duration of action exceeding 60 min. RS 17053 hydrochloride pretreatment significantly alteres food intake [F(4, 132) 5 6.28, p , 0.0001]. 10 mg/kg RS-17053 significantly suppresses food intake.

RS-17053

Others

Other Targets

Proton pump

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169505-93-5

449.42

C24H30Cl2N2O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (222.51 mM)

Cl.CC(C)(Cc1c[nH]c2ccc(Cl)cc12)NCCOc1ccccc1OCC1CC1

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(-20℃)

With Ice Pack

≥ 2 years