Tachykinin peptide-induced activation and desensitization of neurokinin 1 receptors.
The actions of four tachykinins on inhibition and desensitization of the M-current of bullfrog sympathetic neurons have been characterized. Radioligand binding parameters of the tachykinins were determined at a neurokinin receptor in a heterologous expression system. The correlation between binding, signaling and receptor regulation was investigated. A correlation between receptor binding and signaling was found between the peptides; however, their ability to produce desensitization was not correlated with binding and signaling. These results show that the ability of a tachykinin peptide to induce signal activation is not indicative of its ability to induce receptor regulation.
Department of Neurobiology and Pharmacology, Northeastern Ohio Universities College of Medicine, 4209 State Route 44, PO Box 95, Rootstown, OH 44272-0095, USA.
S A
SA
Perrine
V J
VJ
Bennett
M A
MA
Simmons
D000595:Amino Acid Sequence; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D015536:Down-Regulation / Q000187:drug effects*; D004594:Electrophysiology; D008024:Ligands; D011188:Potassium / Q000378:metabolism; D011485:Protein Binding; D011892:Rana catesbeiana; D018040:Receptors, Neurokinin-1 / Q000819:agonists* / Q000378:metabolism*; D015320:Tachykinins / Q000737:chemistry / Q000494:pharmacology*
D008024:Ligands; D018040:Receptors, Neurokinin-1; D015320:Tachykinins; D011188:Potassium