Histamine H3 receptor desensitization in the guinea-pig ileum

被引：16

作者：

Pérez-García, C ^{[1
]}

Morales, L ^{[1
]}

Alguacil, LF ^{[1
]}

机构：

[1] Univ San Pablo CEU, Pharmacol Lab, Madrid 28660, Spain

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1998年 / 341卷 / 2-3期

关键词：

histamine H-3 receptor; R-alpha-methylhistamine; receptor desensitization; ileum; guinea-pig;

D O I：

10.1016/S0014-2999(97)01446-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Histamine H-3 receptor ligands are usually tested in guinea-pig intestine preparations. A possible desensitization of agonist-induced twitch inhibition was studied in longitudinal muscle-myenteric plexus from ileal segments. A cumulative concentration-response curve for R-alpha-methylhistamine was made; when a second curve was made 30 min afterwards, a marked decrease of pD(2), and a more modest decrease of E-max were observed without changes in tissue sensitivity to electrical stimulation or morphine inhibition. At 120 min, pD(2) and E-max were not different from those for the first curve. Receptor desensitization seems homologous and reversible and could interfere max with repetitive testing of histamine H-3 receptor ligands. (C) 1998 Elsevier Science B.V.

引用

页码：253 / 256

页数：4

共 18 条

[1] EFFECT OF MORPHINE AND ACETYLCHOLINE ON CONTRACTILE ACTIVITY AND CYCLIC-AMP IN GUINEA-PIG ILEUM [J].

ALGUACIL, LF ;

LOPEZRUIZ, MP ;

PRIETO, JC ;

ALAMO, C ;

CUENCA, E .

BIOSCIENCE REPORTS, 1990, 10 (01) :113-119

[2] AUTO-INHIBITION OF BRAIN HISTAMINE-RELEASE MEDIATED BY A NOVEL CLASS (H-3) OF HISTAMINE-RECEPTOR [J].

ARRANG, JM ;

GARBARG, M ;

SCHWARTZ, JC .

NATURE, 1983, 302 (5911) :832-837

[3] HISTAMINE H-3 RECEPTOR-BINDING SITES IN RAT-BRAIN MEMBRANES - MODULATIONS BY GUANINE-NUCLEOTIDES AND DIVALENT-CATIONS [J].

ARRANG, JM ;

ROY, J ;

MORGAT, JL ;

SCHUNACK, W ;

SCHWARTZ, JC .

EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION, 1990, 188 (4-5) :219-227

[4] HIGHLY POTENT AND SELECTIVE LIGANDS FOR HISTAMINE RECEPTORS-H-3 [J].

ARRANG, JM ;

GARBARG, M ;

LANCELOT, JC ;

LECOMTE, JM ;

POLLARD, H ;

ROBBA, M ;

SCHUNACK, W ;

SCHWARTZ, JC .

NATURE, 1987, 327 (6118) :117-123

[5] BETA-ADRENERGIC-RECEPTOR KINASE - PRIMARY STRUCTURE DELINEATES A MULTIGENE FAMILY [J].

BENOVIC, JL ;

DEBLASI, A ;

STONE, WC ;

CARON, MG ;

LEFKOWITZ, RJ .

SCIENCE, 1989, 246 (4927) :235-240

[6]

CORUZZI G, 1991, J PHARMACOL EXP THER, V258, P325

[7]

FINK K, 1990, N-S ARCH PHARMACOL, V342, P513

[8] CHARACTERIZATION OF HISTAMINE H-3 RECEPTORS IN GUINEA-PIG ILEUM WITH H-3 SELECTIVE LIGANDS [J].

HEW, RWS ;

HODGKINSON, CR ;

HILL, SJ .

BRITISH JOURNAL OF PHARMACOLOGY, 1990, 101 (03) :621-624

[9] EVALUATION OF THE RECEPTOR SELECTIVITY OF THE H-3 RECEPTOR ANTAGONISTS, IODOPHENPROPIT AND THIOPERAMIDE - AN INTERACTION WITH THE 5-HT3 RECEPTOR REVEALED [J].

LEURS, R ;

TULP, MTM ;

MENGE, WMBP ;

ADOLFS, MJP ;

ZUIDERVELD, OP ;

TIMMERMAN, H .

BRITISH JOURNAL OF PHARMACOLOGY, 1995, 116 (04) :2315-2321

[10] EFFECTS OF THIOPERAMIDE, A HISTAMINE H-3 RECEPTOR ANTAGONIST, ON A SCOPOLAMINE-INDUCED LEARNING DEFICIT USING AN ELEVATED PLUS-MAZE TEST IN MICE [J].

MIYAZAKI, S ;

IMAIZUMI, M ;

ONODERA, K .

LIFE SCIENCES, 1995, 57 (23) :2137-2144

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