title: A bioactive peptide from the transmembrane 5-intracellular loop 3 region of the human 5HT1a receptor.
abstract: 15 amino acid peptide from the transmembrane 5-intracellular loop 3 region of the human 5HT1a receptor produced concentration-dependent decreases in agonist binding. This result is consistent with a competitive interaction between peptide, receptor, and G protein at the receptor-G protein interface. Bombesin and a 13 amino acid peptide from the carboxyl terminus region of the receptor were inactive. Additionally, the peptide decreased forskolin-mediated cAMP elevation. Overall, these results suggest that amino acid residues from this region of the receptor are involved in receptor-G protein coupling and that G protein is activated by the receptor.
authors: Department of Pharmaceutical Sciences, School of Pharmacy, University of Montana, Missoula 59812-1075, USA.
authors: K
authors: K
authors: Hayataka
authors: M F
authors: MF
authors: O'Connor
authors: N
authors: N
authors: Kinzler
authors: J T
authors: JT
authors: Weber
authors: K K
authors: KK
authors: Parker
mesh_terms: D000818:Animals; D001839:Bombesin / Q000494:pharmacology; D016466:CHO Cells; D006224:Cricetinae; D000242:Cyclic AMP / Q000037:antagonists & inhibitors / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D019204:GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D010455:Peptides / Q000494:pharmacology; D011817:Rabbits; D011985:Receptors, Serotonin / Q000737:chemistry*; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists / Q000378:metabolism
chemical_list: D010455:Peptides; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists; D000242:Cyclic AMP; D019204:GTP-Binding Proteins; D001839:Bombesin