Lactones, XXVII: “Lactonized” Pimocide - Stability and Dopamine Receptor Affinity of its Enantiomers and Ring Open Derivatives

✍ Scribed by Anja Radwansky; Jochen Lehmann

• Book ID: 101639230
• Publisher: John Wiley and Sons
• Year: 1993
• Tongue: English
• Weight: 161 KB
• Volume: 326
• Category: Article
• ISSN: 0365-6233
• DOI: 10.1002/ardp.19933261113

✦ Synopsis

Considering the possibility of an in vivo equilibrium 1 + 3a, the "lactonized" neuroleptic 1 is supposed to have quite different pharmakokinetic properties compared to the analogous diphenylbutylpiperidine pimocide. 1 showed little affinity to the 5-HT*-') but high (Ki = 17 nmolj) to the dopamine D*-binding site of rat striatum'). Now we want to report on the affinity of 1, its enantiomers and its ring open derivatives 3a,b to the dopamine receptors in bovine