Neurokinin receptor antagonists inhibit the binding of growth hormone-releasing peptide to EP-1 human neuroblastoma cells.
KP-102, a second generation growth hormone-releasing peptide, specifically bound to the human neuroblastoma cell line, EP-1, cultured in vitro with a Kd value comparable to that in cell membranes of rat pituitary and hypothalamus. By crosslinking study, the molecular size of the KP-102-receptor complex was found to be approximately 80kDa. Substance P analogue, as well as nonpeptidyl antagonists of the neurokinin receptor, competed with KP-102 in its binding to EP-1 cells, although neither substance P nor substance K affected the binding. These results suggest that KP-102 binds to a receptor-like molecule resembling neurokinin receptor.
Tai
S
S
Department of Medicine, Kobe University School of Medicine, Japan.
Kaji
H
H
Okimura
Y
Y
Abe
H
H
Chihara
K
K
D000527:Alprostadil / Q000494:pharmacology; D000818:Animals; D001285:Atropine / Q000494:pharmacology; D002217:Carbachol / Q000494:pharmacology; D002460:Cell Line; D013007:Growth Hormone-Releasing Hormone / Q000378:metabolism; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D007031:Hypothalamus / Q000378:metabolism; D007700:Kinetics; D009447:Neuroblastoma; D009479:Neuropeptides / Q000494:pharmacology; D009842:Oligopeptides / Q000378:metabolism*; D010902:Pituitary Gland / Q000378:metabolism; D051381:Rats; D018039:Receptors, Tachykinin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D009479:Neuropeptides; D009842:Oligopeptides; D018039:Receptors, Tachykinin; D006165:Guanylyl Imidodiphosphate; D001285:Atropine; D002217:Carbachol; D013007:Growth Hormone-Releasing Hormone; C091874:growth hormone-releasing peptide-2; D000527:Alprostadil