| CAS NO: | 168986-61-6 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 168986-61-6 |
| 化学名 | N-(2-(4-(3-(4-amino-5-chloro-2-methoxyphenyl)-3-oxopropyl)piperidin-1-yl)ethyl)methanesulfonamide hydrochloride |
| Canonical SMILES | ClC(C=C(C(OC)=C1)C(CCC2CCN(CCNS(=O)(C)=O)CC2)=O)=C1N.Cl |
| 分子式 | C18H28ClN3O4S.HCl |
| 分子量 | 454.41 |
| 溶解度 | Soluble to 80 mM in Water |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | pKi: 8.8 RS 67506 hydrochloride is a potent and selective 5-HT4 partial agonist. Selective agonists of 5-HT4 receptor can not only enhance congnitive performance, facilitate gastrointestinal motility, and also correct micturation disturbances which is associated with detrusor hypomotilityor actas analgesics. In vitro: RS 67506 acted as a potent partial agonist with respect to 5-HT at the 5-HT4 receptor regulating relaxation of the carbachol-precontracted oesophagus. Relaxant responses to RS 67506 was surmountably antagonized with apparent affinities (pKB) of 9.0. RS 67506, therefore, acted as potent, partial 5-HT4 receptor agonists in vitro. The compound may have been used in elucidating the physiological role in 5-HT4 receptors by virtue of their high potency and selectivity [1]. In vivo: RS 67506 induced dose-dependent potentiates heart rate of the anaesthetized micropig (ED50 5.4 pg kg-1, i.v.) with maximal increases of 47 beats min-1 [1]. In addition, in a rat model of spatial learning and memory, the effects of two novel potent and selective 5-HT4 receptor agonists (RS67333 and RS67506) were studied. By contrast, there was no effect seen to RS67506 (0.1, 10 and 1000 pg/kg, i.p.) of equivalent potency and selectivity to RS67333.This differential result may suggest the enhanced ability of RS67333 to enter the CNS, with respect to RS67506 [2]. Clinical trial: So far, no clinical study has been conducted. References: |
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