Substance-P antagonists: effect on spontaneous and drug-induced locomotor activity in the rat.
The substance P (SP) antagonists (D-Pro4, D-Trp7,9, Leu11) SP(4-11), (D-Pro4, D-Trp7,9, Phe11)SP(4-11) and (D-Pro4, D-Trp7,9,10, Leu11) SP (4-11) were infused into the lateral ventricles (i.c.v.) and their effects on spontaneous and drug-induced locomotor activity were investigated. The drug DiMeC7, the stable substance P agonist, was used to stimulate locomotor activity because of its prolonged action. Only (D-Pro4, D-Trp7,9,10) SP (4-11) was found to attenuate the drug-induced increases in motor activity, indicating that it is a substance P antagonist with activity in the CNS.
D000818:Animals; D001921:Brain / Q000187:drug effects*; D004298:Dopamine / Q000502:physiology; D007276:Injections, Intraventricular; D008297:Male; D009043:Motor Activity / Q000187:drug effects*; D010446:Peptide Fragments / Q000494:pharmacology*; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D051381:Rats; D011919:Rats, Inbred Strains; D013373:Substance P / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors* / Q000494:pharmacology
D010446:Peptide Fragments; D013373:Substance P; C032720:substance P (5-11), pGlu(5)-MePhe(8)-MeGly(9)-; C053122:substance P (4-11), Pro(4)-Trp(7,9)-LeuNH2(11)-; C053124:substance P (4-11), Pro(4)-Trp(7,9)-PheNH2(11)-; C053123:substance P(4-11), Pro(4)-Trp(7,9,10)-LeuNH2(11)-; D011761:Pyrrolidonecarboxylic Acid; D004298:Dopamine