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Artigo Revisado por pares
BIBTEX RIS

Imetit and N-methyl derivatives. The transition from potent agonist to antagonist at histamine H3 receptors.1

1992; Elsevier BV; Volume: 2; Issue: 10 Linguagem: Inglês

10.1016/s0960-894x(00)80219-x

ISSN

1464-3405

Autores

C. Robin Ganellin, Benny Bang‐Andersen, Y. S. KHALAF, W. Tertiuk, J.M. Arrang, M. Garbarg, Xavier Ligneau, A. Rouleau, J.C. Schwartz,

Tópico(s)

Receptor Mechanisms and Signaling

Resumo

Imetit {S-[2-(imidazol-4-yl)ethyl]isothiourea} is a potent H3-agonist in vitro (on rat brain cortical slices; EC50 = 1 nM) and in vivo (ED50 ∼ 1 mg/kg per os in mice). N-Methylimetit is also an agonist (EC50 = 15 nM) but dimethyl and trimethyl derivatives are antagonists (Ki = 50 - 500 nM).

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