RS 17053 hydrochloride
Modify Date: 2024-01-14 08:11:22
RS 17053 hydrochloride structure
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Common Name | RS 17053 hydrochloride | ||
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| CAS Number | 169505-93-5 | Molecular Weight | 449.41300 | |
| Density | N/A | Boiling Point | 580.1ºC at 760 mmHg | |
| Molecular Formula | C24H30Cl2N2O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 304.7ºC | |
Use of RS 17053 hydrochlorideRS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays. |
| Name | RS 17053 hydrochloride,(N-[2-(2-Cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine)hydrochloride |
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| Synonym | More Synonyms |
| Description | RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays. |
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| Related Catalog | |
| Target |
pKi: 9.1 (α1A adrenoceptor in native cell membrane) pA2: 9.8 (α1A adrenoceptor)[1]. |
| In Vitro | 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)[1]. |
| In Vivo | 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[2]. |
| Animal Admin | 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 |
| Boiling Point | 580.1ºC at 760 mmHg |
|---|---|
| Molecular Formula | C24H30Cl2N2O2 |
| Molecular Weight | 449.41300 |
| Flash Point | 304.7ºC |
| Exact Mass | 448.16800 |
| PSA | 46.28000 |
| LogP | 6.79270 |
| Vapour Pressure | 1.88E-13mmHg at 25°C |
| Kifunensine |
| RS 17053 hydrochloride |