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Titolo:
Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology
Autore:
Smart, D; Jerman, JC; Gunthorpe, MJ; Brough, SJ; Ranson, J; Cairns, W; Hayes, PD; Randall, AD; Davis, JB;
Indirizzi:
SmithKline Beecham Pharmaceut, Neurosci Res, Harlow CM19 5AW, Essex, England SmithKline Beecham Pharmaceut Harlow Essex England CM19 5AW ssex, England SmithKline Beecham Pharmaceut, Biotechnol & Genet, Harlow CM19 5AW, Essex,England SmithKline Beecham Pharmaceut Harlow Essex England CM19 5AW Essex,England
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 1-2, volume: 417, anno: 2001,
pagine: 51 - 58
SICI:
0014-2999(20010406)417:1-2<51:CUFOHV>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
ROOT GANGLION NEURONS; RAT SENSORY NEURONS; CAPSAICIN RECEPTOR; PAIN; HEAT; HYPERALGESIA; PROTONS; CHANNEL; SENSITIZATION; ACTIVATION;
Keywords:
vanilloid; capsaicin; Ca2+; ligand-gated ion channel; FLIPR; nociception;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
36
Recensione:
Indirizzi per estratti:
Indirizzo: Smart, D SmithKline Beecham Pharmaceut, Neurosci Res, New Frontiers Sci Pk,3rd Ave,Harlow CM19 5AW, Essex, England SmithKline Beecham Pharmaceut New Frontiers Sci Pk,3rd Ave Harlow Essex England CM19 5AW
Citazione:
D. Smart et al., "Characterisation using FLIPR of human vanilloid VR1 receptor pharmacology", EUR J PHARM, 417(1-2), 2001, pp. 51-58

Abstract

A full pharmacological characterisation of the recently cloned human vanilloid VR1 receptor was undertaken. In whole-cell patch damp studies, capsaicin (10 muM) elicited a slowly activating/deactivating inward current in human embryonic kidney (HEK293) cells stably expressing human vanilloid VR1 receptor, which exhibited pronounced outward rectification (reversal potential -2.1 +/- 0.2 mV) and was abolished by capsazepine (10 muM). In FLIPR(TM)-based Ca2+ imaging studies the rank order of potency was resiniferatoxin > olvanil > capsaicin > anandamide, and all were full agonists. Isovelleral and scutigeral were inactive (1 nM-30 muM) The potencies of capsaicin, olvanil and resiniferatoxin, but not anandamide, were enhanced 2- to 7-fold at pH 6.4. Capsazepine, isovelleral and ruthenium red inhibited the capsaicin (100 nM)-induced Ca2+ response (pK(B) = 6.58 +/- 0.02, 5.33 +/- 0.03 and 7.64 +/- 0.03, respectively). In conclusion, the recombinant human vanilloid VR1 receptor stably expressed in HEK293 cells acted as a ligand-gated, Ca2+-permeable channel with similar agonist and antagonist pharmacology to rat vanilloid VR1 receptor, although there were some subtle differences. (C) 2001 Published by Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/04/20 alle ore 09:12:08