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Titolo:
Functional and desensitizing effects of the novel synthetic vanilloid-likeagent 12-phenylacetate 13-acetate 20-homovanillate (PPAHV) in the perfusedrat hindlimb
Autore:
Griffiths, CD; Vincent, MA; Szallasi, A; Colquhoun, EQ; Geraghty, DP;
Indirizzi:
Univ Tasmania, Sch Biomed Sci, Launceston 7250, Australia Univ Tasmania Launceston Australia 7250 Sci, Launceston 7250, Australia Univ Tasmania, Discipline Biochem, Hobart, Tas 7001, Australia Univ Tasmania Hobart Tas Australia 7001 chem, Hobart, Tas 7001, Australia Washington Univ, Med Ctr, Dept Pathol, St Louis, MO 63110 USA Washington Univ St Louis MO USA 63110 Dept Pathol, St Louis, MO 63110 USA
Titolo Testata:
BRITISH JOURNAL OF PHARMACOLOGY
fascicolo: 7, volume: 131, anno: 2000,
pagine: 1408 - 1412
SICI:
0007-1188(200012)131:7<1408:FADEOT>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITIVE COOPERATIVITY; CAPSAICIN RECEPTOR; OXYGEN-UPTAKE; RESINIFERATOXIN BINDING; SUBTYPES; NEURONS; MUSCLE;
Keywords:
vanilloids; vanilloid receptors; perfused rat hindlimb; oxygen consumption; perfusion pressure; tachyphylaxis;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Geraghty, DP Univ Tasmania, Sch Biomed Sci, Launceston 7250, Australia Univ Tasmania Launceston Australia 7250 ton 7250, Australia
Citazione:
C.D. Griffiths et al., "Functional and desensitizing effects of the novel synthetic vanilloid-likeagent 12-phenylacetate 13-acetate 20-homovanillate (PPAHV) in the perfusedrat hindlimb", BR J PHARM, 131(7), 2000, pp. 1408-1412

Abstract

1 In the present study, the effects of the novel vanilloid agonist, 12-phenylacetate 13-acetate 20-homovanillate (PPAHV), on oxygen consumption (VO2)and vascular resistance (perfusion pressure, PP) were investigated in the constant flow, perfused rat hindlimb. The acute desensitizing properties ofthis novel synthetic agent were also examined.2 Maximum stimulation of VO2 was produced by 0.2 muM PPAHV (Delta VO2, 0.83 +/- 0.06 mu mol g(-1) h (1)) and was accompanied by mild vasoconstriction(increase in PP; 8.0 +/- 1.1 mmHg). The highest concentration of PPAHV tested (2 muM) caused inhibition of VO2 (Delta VO2. -2.73+/-0.51 mu mol g(-1) h(-1)) and strong vasoconstriction (Delta PP, 42.0+/-1.2 mmHg).3 Capsazepine (10 muM) caused a parallel shift to the right of both VO2 and PP concentration-response curves for PPAHV (pK(b) = 5.00), indicative of competitive binding to vanilloid receptors.4 The stimulation of VO2 produced by 0.2 muM PPAHV decreased, but was not completely abolished, after repeated infusion of PPAHV (change in VO2, first infusion, 0.66+/- 0.18 mu mol g (1) h (1): sixth infusion, 0.29+/-0.08 mumol g(-1) h(-1), P<0.05), an acute tachyphylactic response not previously seen with the repeated infusion of other vanilloid analogues. Conversely, the PP response to repeated PPAHV infusion increased (<Delta>PP, first infusion, 5.8+/-0.7 mmHg; sixth infusion. 9.0+/-0.6 mmHg, P<0.05).5 In conclusion, PPAHV produces vasoconstriction and a biphasic effect on VO2 in the perfused rat hindlimb very similar to that induced by naturally occurring vanilloids. Both effects are blocked by the competitive antagonist capsazepine. Since, the metabolic response to low concentrations of PPAHV(stimulation of VO2) undergoes tachyphylaxis, the present data suggest that PPAHV desensitizes putative vanilloid receptors in the hindlimb.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 16:07:46