Ceruletide, ceruletide analogues and cholecystokinin octapeptide (CCK-8): effects on motor behaviour, hexobarbital-induced sleep and harman-induced convulsions.
Ten ceruletide analogues and cholecystokinin octapeptide (CCK-8) were compared with ceruletide regarding neuropharmacological effects in mice after subcutaneous administration. The effects under study were catalepsy, prolongation of hexobarbital-induced sleep and delay in onset of harman-induced convulsions. Ceruletide and several analogues were more potent than the reference drugs, diazepam and haloperidol. Desulfation, deamidation and shortening of the peptide chain by five amino acids strongly reduced or abolished the pharmacological activities of ceruletide. Other chemical modulations mostly weakened the efficacy, but to an unequal extent for the three effects, which altered the pharmacological selectivity.
D000818:Animals; D002108:Ceruletide / Q000031:analogs & derivatives* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002766:Cholecystokinin / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006247:Harmine / Q000031:analogs & derivatives; D006591:Hexobarbital / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects*; D010446:Peptide Fragments / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced*; D012844:Sincalide; D012890:Sleep / Q000187:drug effects*; D013329:Structure-Activity Relationship
D010446:Peptide Fragments; D006247:Harmine; C005010:harman; D002108:Ceruletide; D002766:Cholecystokinin; D006591:Hexobarbital; D012844:Sincalide