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.
Perrine
S A
SA
Department of Neurobiology and Pharmacology, Northeastern Ohio Universities College of Medicine, 4209 State Route 44, PO Box 95, Rootstown, OH 44272-0095, USA.
Bennett
V J
VJ
Simmons
M A
MA
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