| Name | RS 17053 hydrochloride |
| Description | RS 17053 hydrochloride is a potent and selective antagonist of the α1A adrenoceptor, with a pKi value of 9.1 in native cell membranes and a pA2 value of 9.8 in functional assays. |
| 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 [1]. |
| In vivo | RS 17053 hydrochloride exhibits a rapid onset and a duration of action exceeding 60 minutes. At a dosage of 10 mg/kg, RS-17053 significantly suppresses food intake and its pretreatment notably alters food intake [F(4, 132) = 6.28, p < 0.0001] [2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 125 mg/mL (278.14 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.9 mM), Sonication is recommended.
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| Keywords | α1A-adrenergic receptor | α1A | RS-17053 Hydrochloride | RS17053 Hydrochloride | RS17053 | RS 17053 | AdrenergicReceptor | Adrenergic Receptor |
| Inhibitors Related | Trifluoperazine dihydrochloride | Mirtazapine | Octopamine hydrochloride | Gemfibrozil | Buflomedil hydrochloride | Dexmedetomidine hydrochloride | Isoprenaline hydrochloride | D-Mannitol | Mianserin hydrochloride | Trazodone hydrochloride | Atenolol | Doxepin hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compounds Library Max | Adrenergic Receptor-Targeted Compound Library | GPCR Compound Library | Anti-Cancer Compound Library |
United States
