[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole. Analgesic activity and effect on conditioned avoidance response].
Several derivatives of 2-benzylbenzimidazole (dibazole) bearing substituents on positions 5 and 4' were prepared and tested, together with dibazole, for their activity on the acquisition of a conditioned avoidance response and for analgesic activity. Chlorpromazine and acetylsalicylic acid were used as standards. Analgesic activity was found for all these compounds, most of which proved more active than A.S.A. As regards the acquisition of a C.A.R., the 5-chloroderivatives exhibit a strong inhibitory activity, that for compound (VIII) is equal to that of chloropromazine, while dibazole and the 5-trifluormethylderivatives stimulate the acquisition.
Paglietti
G
G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari.
Pirisi
M A
MA
Loriga
M
M
Grella
G E
GE
Sparatore
F
F
Satta
M
M
Manca
P
P
Peana
A
A
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D001562:Benzimidazoles; C004453:bendazole
Preparazione e attività farmacologica di 2-(4'R')benzil-5R-benzimidazoli. Attività analgesica e sull'acquisizione di una risposta condizionata di evitamento.