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Titolo:
THE RESPONSES OF RAT TRIGEMINAL GANGLION NEURONS TO CAPSAICIN AND 2 NONPUNGENT VANILLOID RECEPTOR AGONISTS, OLVANIL AND GLYCERYL NONAMIDE
Autore:
LIU L; LO YC; CHEN IJ; SIMON SA;
Indirizzi:
DUKE UNIV,MED CTR,DEPT NEUROBIOL DURHAM NC 27710 DUKE UNIV,MED CTR,DEPT NEUROBIOL DURHAM NC 27710 DUKE UNIV,MED CTR,DEPT ANESTHESIOL DURHAM NC 27710 DEPT PHARMACOL KAOHSIUNG 80708 TAIWAN
Titolo Testata:
The Journal of neuroscience
fascicolo: 11, volume: 17, anno: 1997,
pagine: 4101 - 4111
SICI:
0270-6474(1997)17:11<4101:TRORTG>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
EFFERENT FUNCTION; ANALOGS; RESINIFERATOXIN; MECHANISM; NE-19550; ANTAGONIST; CURRENTS; INVITRO; FIBERS; POTENT;
Keywords:
PAIN; TASTE; VANILLOID RECEPTORS; PUNGENT; OLVANIL; CAPSAICIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
L. Liu et al., "THE RESPONSES OF RAT TRIGEMINAL GANGLION NEURONS TO CAPSAICIN AND 2 NONPUNGENT VANILLOID RECEPTOR AGONISTS, OLVANIL AND GLYCERYL NONAMIDE", The Journal of neuroscience, 17(11), 1997, pp. 4101-4111

Abstract

Capsaicin, the pungent ingredient in hot pepper, activates and subsequently desensitizes a subset of polymodal nociceptors. Because its initial application to skin produces pain, nonpungent analogs such as olvanil and glyceryl nonivamide (GLNVA) were synthesized to enhance its clinical use. To explore how these nonpungent analogs differ from capsaicin, whole-cell patch-clamp recordings were performed on cultured rattrigeminal ganglion neurons. In neurons held at -60 mV, capsaicin, olvanil, and GLNVA were found to activate one or two kinetically distinct inward currents. Two inward currents were also activated when extracellular Ca2+ was replaced with Ba2+ and also when intracellular chloride was replaced by aspartate. The reversal potentials of the rapidly and slowly activating currents were 15.3 +/- 6 and -4.0 +/- 2.5 mV, respectively. These data provide strong evidence for subtypes of vanilloid receptors. One difference among these agonists is that, on average, the activation kinetics of the currents evoked by 1 mu M olvanil and 30 mu M GLNVA are considerably slower than those evoked by 1 mu M capsaicin. Measurements of the peak current, Ip, versus agonist concentration were fit to the Hill equation to yield values of the half maximal concentrations (K-1/2), and the Hill coefficients (n), For capsaicin, olvanil, and GLNVA, K-1/2 = 0.68, 0.59, and 27.0 mu M; and n = 1.38, 1.32, and 1.24, respectively. We propose that olvanil and GLNVA are nonpungent because they activate different subtypes of receptors and/or because of their activation kinetics (compared with capsaicin) are, on average, slower than the rate they inhibit action potentials from polymodal nociceptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 14:05:48