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Titolo:
DESENSITIZATION OF THE NEUROKININ-1 RECEPTOR IS MEDIATED BY THE RECEPTOR CARBOXY-TERMINAL REGION, BUT IS NOT CAUSED BY RECEPTOR INTERNALIZATION
Autore:
SANDERS MA; LEVINE H;
Indirizzi:
WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES,DEPT NEUROSCI PHARMACOL,2800 PLYMOUTH RD ANN ARBOR MI 48105 WARNER LAMBERT PARKE DAVIS,PARKE DAVIS PHARMACEUT RES,DEPT NEUROSCI PHARMACOL ANN ARBOR MI 48105 UNIV MICHIGAN,DEPT BIOL ANN ARBOR MI 48109
Titolo Testata:
Journal of neurochemistry
fascicolo: 6, volume: 67, anno: 1996,
pagine: 2362 - 2372
SICI:
0022-3042(1996)67:6<2362:DOTNRI>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
SUBSTANCE-P RECEPTOR; AGONIST-INDUCED DESENSITIZATION; PROTEIN-COUPLED RECEPTOR; PLATELET-ACTIVATING-FACTOR; BETA-ADRENERGIC RECEPTORS; MOLECULAR CHARACTERIZATION; TACHYKININ RECEPTORS; MUSCARINIC RECEPTOR; ASTROCYTOMA-CELLS; FUNCTIONAL CDNA;
Keywords:
RECEPTOR DESENSITIZATION; RECEPTOR INTERNALIZATION; PHOSPHOINOSITIDE HYDROLYSIS; CHIMERIC RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
52
Recensione:
Indirizzi per estratti:
Citazione:
M.A. Sanders e H. Levine, "DESENSITIZATION OF THE NEUROKININ-1 RECEPTOR IS MEDIATED BY THE RECEPTOR CARBOXY-TERMINAL REGION, BUT IS NOT CAUSED BY RECEPTOR INTERNALIZATION", Journal of neurochemistry, 67(6), 1996, pp. 2362-2372

Abstract

The carboxy-terminal cytoplasmic regions of the rat neurokinin 1 (substance P) and neurokinin 2 (neurokinin A) receptors have been exchanged to determine if this region of the neurokinin 1 receptor is involvedin its desensitization. When expressed at similar levels in stably transfected Chinese hamster ovary (CHO) cell lines, receptors containingthe carboxy-terminal region of the neurokinin 1 receptor desensitizedsignificantly more (as measured by reduction of the inositol 1,4,5-trisphosphate response) when preexposed for 1 min to I mu M neurokinin, indicating a role for the carboxy-terminal region of the neurokinin 1 receptor in its desensitization. Measurement of receptor internalization using radiolabeled neurokinins (0.3 nM) indicated that similar to 75-80% of the receptors were internalized in each cell line after 10 min at 37 degrees C, with no observable correlation between neurokinin receptor desensitization and internalization. Measurement of loss of receptor surface sites for cell lines CHO NK1 and CHO NK1NK2 following exposure to 1 mu M substance P also indicated no obvious relationship between the percent desensitization and percent of receptors internalized, Also, two inhibitors of neurokinin 1 receptor internalization, phenylarsine oxide and hyperosmolar sucrose, did not inhibit neurokinin 1receptor desensitization. The protein kinase inhibitors Ro 31-8220, staurosporine, and Zn2+ had no effect on neurokinin 1 receptor desensitization, indicating that the kinases affected by these agents are not rate-limiting in neurokinin 1 receptor desensitization in this system.

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Documento generato il 29/03/20 alle ore 12:19:57