Pharmacology of stomoxytachykinin receptor depends on second messenger system.
STKR is a neurokinin receptor derived from the stable fly, Stomoxys calcitrans. Insect tachykinin-related peptides, also referred to as "insectatachykinins", produce dose-dependent calcium and cyclic AMP responses in cultured Drosophila melanogaster Schneider 2 (S2) cells that were stably transfected with the cloned STKR cDNA. Pronounced differences in pharmacology were observed between agonist-induced calcium and cyclic AMP responses. The results indicate that the pharmacological properties of STKR depend on its coupling to a unique second messenger system. Therefore, a model postulating the existence of multiple active receptor conformations is proposed. This article presents the first evidence that an insect peptide receptor with dual coupling properties to second messenger systems can display agonist-dependent functional differences.
Poels
Jeroen
J
Laboratory for Developmental Physiology, Genomics and Proteomics, Zoological Institute, Naamsestraat 59, B-3000 Leuven, Belgium.
Nachman
Ronald J
RJ
Akerman
Karl E
KE
Oonk
Hendrica B
HB
Guerrero
Felix
F
De Loof
Arnold
A
Janecka
Anna E
AE
Torfs
Herbert
H
Vanden Broeck
Jozef
J
D000818:Animals; D002118:Calcium / Q000378:metabolism; D002478:Cells, Cultured; D000242:Cyclic AMP / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004331:Drosophila melanogaster / Q000187:drug effects* / Q000378:metabolism; D010455:Peptides / Q000494:pharmacology*; D015290:Second Messenger Systems / Q000187:drug effects*; D015320:Tachykinins / Q000494:pharmacology*
D010455:Peptides; D015320:Tachykinins; D000242:Cyclic AMP; D002118:Calcium