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Eur J Med Chem. 2000 Jan;35(1):5-20.

Selective ligands as tools to study histamine receptors.

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Leiden/Amsterdam Center for Drug Research, Department of Pharmacochemistry, Vrije Universiteit, De Boelelaan 1083, NL 1081 HV, Amsterdam, The Netherlands.


In this review the histaminergic ligands for the histamine H(1), H(2) and H(3) receptors, which are currently used as tools in pharmacological studies, are described. To study interactions with the histamine H(1) receptor, the H(1) agonist 2-aminoethylthiazole has long since been used. However, during the last decade, 2-phenylhistamine derivatives emerged with interesting binding features. So far no radiolabelled selective H(1) agonist has been commonly used. As H(1) antagonists mepyramine, triprolidine and chlorpheniramine are described together with radiolabelled H(1) antagonists [3H]mepyramine and [3H]doxepin. Special attention has been paid to the PET ligands [11C]doxepin and [11C]mepyramine and the [125I] labelled antagonists [125I]iodobolpyramine and [125I]iodoazidophenpyramine. Concerning H(2) agonists, especially dimaprit, amthamine and impromidine are discussed. There are several H(2) antagonists; amongst them cimetidine, tiotidine and ranitidine are used most frequently. Many of these antagonists behave as inverse agonists. As radiolabelled H(2) antagonists, [3H]cimetidine, [3H]tiotidine, [125I]iodoaminopotentidine and [125I]iodoazidopotentidine are included. Commonly used histamine H(3) agonists are N(alpha)-methylhistamine, (R)alpha-methylhistamine, imetit and immepip. Both methylhistamines are also available as [3H] labelled ligands. As reference compounds, often used H(3) antagonists are thioperamide, clobenpropit, iodophenpropit and impentamine. Most important radiolabelled H(3) antagonists are S-[3H]methylthioperamide, [3H]thioperamide, [125I]iodophenpropit and [125I]iodoproxyfan. The use of all these compounds as a tool in pharmacology is also discussed.

[Indexed for MEDLINE]

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