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Titolo:
Combined histamine H-1 and H-3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion
Autore:
McLeod, RL; Mingo, GG; Herczku, C; DeGennaro-Culver, F; Kreutner, W; Egan, RW; Hey, JA;
Indirizzi:
Schering Plough Corp, Res Inst, Dept Allergy, Kenilworth, NJ 07033 USA Schering Plough Corp Kenilworth NJ USA 07033 gy, Kenilworth, NJ 07033 USA
Titolo Testata:
AMERICAN JOURNAL OF RHINOLOGY
fascicolo: 5, volume: 13, anno: 1999,
pagine: 391 - 399
SICI:
1050-6586(199909/10)13:5<391:CHHAHR>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
R-ALPHA-METHYLHISTAMINE; ACOUSTIC RHINOMETRY; GUINEA-PIG; INHIBITION; LORATADINE; RESPONSES; H3-RECEPTORS; PHARMACOLOGY; ACTIVATION; CHILDREN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Hey, JA Schering Plough Corp, Res Inst, Dept Allergy, 2015 Galloping Hill Rd, Kenilworth, NJ 07033 USA Schering Plough Corp 2015 Galloping Hill Rd Kenilworth NJ USA 07033
Citazione:
R.L. McLeod et al., "Combined histamine H-1 and H-3 receptor blockade produces nasal decongestion in an experimental model of nasal congestion", AM J RHINOL, 13(5), 1999, pp. 391-399

Abstract

We studied the pharmacological actions of combined histamine H-1/H-3 receptor blockade on the increase in nasal airway resistance (NAR) and decrease in :nasal cavity volume-produced by nasal exposure to compound 48/80, a mast cell degranulator. In the anesthetized cat compound 48/80 (1%) produced amaximum increase in NAR of 9.1 +/- 0.7 cmH(2)O . L/minute. The increase inNAR in animals pretreated with a combination of the H-1 antagonist, chlorpheniramine (CTM; 0.8 mg/kg i.v.) and increasing doses of the H-3 antagonist, thioperamide (THIO; 1.0, 3.0, and 10.0 mg/kg i.v.) were (6.1 +/- 2.1, 4.2+/- 1.0) and 2.2 +/- 0.7 cmH(2)O . Lminute, respectively. A second H-3 antagonist, clobenpropit (CLOB: 0.03, 0.3, and 1.0 mg/kg i.v.) combined with CTM(0.8 mg/kg i.v.) also inhibited the nasal effects of compound 48/80. Whenthe nonsedating H-1 antihistamine, loratadine (3.0 mg/kg i.v.), was substituted for CTM. it also reduced nasal congestion when given in combination with THIO (TO mg/kg i.v.). In contrast, treatment with CTM (1.0 mg/kg i.v.) and the H-2 antagonist, ranitidine (RAN; 1.0 mg/kg. i.v.) were without activity. Loratadine, CTM, CLOB, RAN, or THIO administered alone were inactive. The alpha-adrenergic agonist, phenylpropanolamine (PPA; 3.0 mg/kg i.v.) demonstrated decongestant;effects, but in contrast to H-1/H-3 blockade, PPA produced :a significant hypertensive effect. Using acoustic rhinometry (AcR)we found that combined i.v. CTM (1.0 mg/kg) and THIO (10 mg/kg) and combined oral CTM (10 mg/kg) and THIO (30 mg/kg) blocked the decrease in nasal cavity volume produced by intranasal compound 48/80 (1%, 50 mu L). The conclude that combined H-1/H-3 histamine receptor blockade enhances the efficacy of it H-1 antagonist by conferring decongestant activity to the H-1 antihistamine. We propose that :the decongestant activity of combined H-1/H-3, blockade may provide a novel approach for the treatment of allergic nasal congestion workout the hypertensive liability of current therapies.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 16/01/21 alle ore 22:22:15