Description
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 . 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 . 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 . Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 168986-61-6
Molecular Weight: 454.41
Formula: C18H29Cl2N3O4S
Chemical Name: N-(2-{4-[3-(4-amino-5-chloro-2-methoxyphenyl)-3-oxopropyl]piperidin-1-yl}ethyl)methanesulfonamide hydrochloride
Smiles: Cl.COC1C=C(N)C(Cl)=CC=1C(=O)CCC1CCN(CCNS(C)(=O)=O)CC1
InChiKey: GFWKWEHKHLTRRF-UHFFFAOYSA-N
InChi: InChI=1S/C18H28ClN3O4S.ClH/c1-26-18-12-16(20)15(19)11-14(18)17(23)4-3-13-5-8-22(9-6-13)10-7-21-27(2,24)25;/h11-13,21H,3-10,20H2,1-2H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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