Ciproxifan and chemically related compounds are highly potent and selective histamine H3-receptor antagonists

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 358, Issue 6, 1998, Pages 623-627

  Kathmann, M ^a   Schlicker, E ^a   Marr, I ^a   Werthwein, S ^a   Stark, H ^b   Schunack, W ^b  

^a UNIVERSITY OF BONN   (Germany)

^b FREIE UNIVERSITÄT BERLIN   (Germany)

Author keywords

Ciproxifan; Iodoproxyfan; Noradrenaline release; Rat brain cortex membranes Mouse brain cortex slices Histamine H3 receptors; 3H N( ) methylhistamine binding

Indexed keywords

CIPROXIFAN; FUB 360; FUB 372; FUB 404; FUB 451; HISTAMINE; HISTAMINE DERIVATIVE; HISTAMINE H1 RECEPTOR; HISTAMINE H2 RECEPTOR; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; IODOPROXYFAN; NORADRENALIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING SITE; BRAIN CORTEX; BRAIN SLICE; CONCENTRATION RESPONSE; DRUG STRUCTURE; GUINEA PIG; HEART ATRIUM; MOUSE; NONHUMAN; NORADRENALIN RELEASE; RECEPTOR AFFINITY; RECEPTOR BINDING;

EID: 0031698466     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/PL00005303     Document Type: Article

References (27)

1. 3) of histamine receptor. Nature 302:832-837
2. 2 receptors. Nature 236:385-390
3. Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254
4. De Lean A, Hancock AA, Lefkowitz RJ (1982) Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. Mol Pharmacol 21:5-16
5. Furchgott RF (1972) The classification of adrenoceptors (adrenergic receptors). An evaluation from the standpoint of receptor theory. In: Blaschko H, Muscholl E (eds) Handbook of experimental pharmacology, vol 33. Springer, Berlin Heidelberg New York, pp 283-335
6. Hill SJ, Ganellin CR, Timmerman H, Schwartz J-C, Skankley NP, Young JM, Schunack W, Levi R, Haas HL (1997) International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 49:253-278
7. 3 receptor model. Naunyn Schmiedebergs Arch Pharmacol 348:498-503
8. 3 receptors. Psychopharmacology 116:464-468
9. 3 receptors in guinea pigs by Nα-methylhistamine. Biochem Biophys Res Commun 168: 979-986
10. Lemoine H, Kaumann AJ (1982) A novel analysis of concentration-dependence of partial agonism. Ring-demethylation of bupranolol results in a high affinity partial agonist (K105) for myocardial and tracheal beta-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol 320:130-144
11. 3-receptor: a target for developing new drugs. Prog Drug Res 39:127-165
12. Leurs R, Smit MJ, Timmerman H (1995) Molecular pharmacological aspects of histamine receptors. Pharmacol Ther 66:413-463
13. 3 receptor heterogeneity? J Pharmacol Exp Ther 276:1009-1015
14. 3 receptors. J Pharmacol Exp Ther 271:452-459
15. 3-receptor antagonist. J Pharmacol Exp Ther (in press)
16. 2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat. J Pharm Pharmacol 47:310-316
17. 3A receptor-mediated inhibition of noradrenaline release in the mouse brain cortex. Naunyn Schmiedebergs Arch Pharmacol 345:489-493
18. 3 receptor models. Br J Pharmacol 112:1043-1048 and 113:657 (erratum)
19. 3 heteroreceptors. Fundam Clin Pharmacol 8:128-137
20. 3 receptors. Inflamm Res 44:296-300
21. 3 receptor heterogeneity? Naunyn Schmiedebergs Arch Pharmacol 353:482-488
22. 3-receptor antagonist of high in vitro and in vivo potency and high selectivity. 27th meeting of the European Histamine Research Society, Lodz, 20-23 May (Abstr 42)
23. Schwartz J-C, Arrang J-M, Garbarg M, Pollard H, Ruat M (1991) Histaminergic transmission in the mammalian brain. Physiol Rev 71:1-51
24. 3 (ant)agonists. PCT WO96/29315 (26.9.1996)
25. 3-receptor antagonists. Drugs Future 21:507-520
26. Van Rossum JM (1963) Cumulative dose-response curves. - II. Technique for the making of dose-response curves in isolated organs and the evaluation of drug parameters. Arch Int Pharmacodyn 143:299-330
27. 3-histamine receptor subtypes. Mol Pharmacol 38:610-613