The antagonism of bombesin in the CNS by substance P analogues.
The ability of substance P analogues to inhibit the action of bombesin in the CNS was investigated using receptor binding and biological assays. The putative substance P antagonists inhibited binding to central receptors for both substance P and bombesin-like peptides. Spantide, which was the most potent analogue tested, reversed the bombesin induced hypothermia and grooming. Therefore the putative substance P antagonists may also antagonize the actions of bombesin in the CNS.
D000818:Animals; D001833:Body Temperature Regulation / Q000187:drug effects; D001839:Bombesin / Q000037:antagonists & inhibitors*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D006120:Grooming / Q000187:drug effects; D008297:Male; D010455:Peptides / Q000037:antagonists & inhibitors*; D010803:Physalaemin / Q000494:pharmacology; D051381:Rats; D018004:Receptors, Bombesin; D011956:Receptors, Cell Surface / Q000378:metabolism; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter / Q000378:metabolism; D013373:Substance P / Q000031:analogs & derivatives* / Q000494:pharmacology
D010455:Peptides; D018004:Receptors, Bombesin; D011956:Receptors, Cell Surface; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter; D010803:Physalaemin; D013373:Substance P; C041817:substance P, Pro(2)-Phe(7)-Trp(9)-; C032132:substance P, prolyl(2)-tryptophan(7,9)-; C042867:spantide; D001839:Bombesin