Identification | Back Directory | [Name]
1-(4-AMINO-5-CHLORO-2-METHOXYPHENYL)-3-[1-BUTYL-4-PIPERIDINYL]-1-PROPANONE HYDROCHLORIDE | [CAS]
168986-60-5 | [Synonyms]
RS67333HCl RS 67333 hydrochlori RS 67333 HYDROCHLORIDE RS 67333 hydrochloride >=98% (HPLC) 1-(4-AMINO-5-CHLORO-2-METHOXYPHENYL)-3-[1-BUTYL-4-PIPERIDINYL]-1-PROPANONE HYDROCHLORIDE 1-(4-AMino-5-chloro-2-Methoxyphenyl)-3-(1-butylpiperidin-4-yl)propan-1-one hydrochloride 1-Propanone, 1-(4-amino-5-chloro-2-methoxyphenyl)-3-(1-butyl-4-piperidinyl)-, hydrochloride (1:1) | [Molecular Formula]
C19H30Cl2N2O2 | [MDL Number]
MFCD00938576 | [MOL File]
168986-60-5.mol | [Molecular Weight]
389.36 |
Chemical Properties | Back Directory | [storage temp. ]
Store at RT | [form ]
Powder | [color ]
Light yellow to yellow | [Water Solubility ]
Soluble to 25 mM in water with gentle warming |
Hazard Information | Back Directory | [Uses]
RS 67333 Hydrochloride is a 5-HT4 receptor agonist. | [Biological Activity]
A potent and highly selective 5-HT 4 partial agonist, with pK i values of 8.7 at 5-HT 4 sites in guinea pig striatum and > 6 at various other receptors, including 5-HT 1A , 1D , 2A , 2C , D 1 , D 2 and M 1-3 . Active in vivo , with an intrinsic activity relative to 5-HT of 0.5. | [Biochem/physiol Actions]
RS 67333 is a selective, high affinity (pKi = 8.7 for the 5-HT4 binding site in guinea-pig striatum) partial agonist toward 5-HT4 receptor that relaxes carbachol-contracted rat oesphageal muscularis mucosae ex vivo (pEC50/%reversal = 8.7/50 with RS 67333 vs. 8.2/100 with 5-HT) and induces tachycardia (tachyarrhythmia) of anaesthetized micropigs in vivo (ED50 via i.p. in μg/kg over max heart rate increase in beats/min = 4.9/35 with RS 67333 vs. 3.2/95 with 5-HT). RS 67333 is also reported to show high affinity for sigma receptors (pKi = 8.9/σ1 and 8.0/σ2), while exhibiting much reduced affinity toward a panel of other receptors, including 5-HT1A, 5-HT2A, 5-HT2C, 5-HT3 (pKi <6.4), muscarinic receptors (pKi = 5.2/M1 & 5.3/M2), and adrenoceptors (pKi <6.7 for α1A, α1B, α2A, α2B, β1, β2). | [storage]
Store at RT |
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