Synthesis, in vitro binding profile, and CNS penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole

Autor:	Chalabi Pm, Karen J. Guarino, J. S. Furman, J. L. Ives, Arthur Adam Nagel, Stafford McLean, Dianne K. Bryce, Rosen T, Seeger Thomas Francis, Roth Rw
Rok vydání:	1990
Předmět:	Stereochemistry Antagonist Biological activity In vitro chemistry.chemical_compound 5-HT3 Receptor Antagonist Biochemistry chemistry In vivo Drug Discovery Radioligand Molecular Medicine Thiazole Receptor
Zdroj:	Journal of Medicinal Chemistry. 33:3020-3023
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm00173a017
Popis:	4-(2-Methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole (5) is a highly potent member of a structurally novel series of selective serotonin-3 receptor antagonists. The synthesis of tritiated 5 and its binding profile in neuroblastoma-glioma 108-15 cells are described. Furthermore, in vivo studies in rat with this radioligand indicate that it effectively penetrates the blood-brain barrier upon peripheral administration. Thus, 5 should be a useful pharmacological tool for both in vitro and in vivo studies of this class of compounds.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::668cf26978093954793dbef0156d5595 https://doi.org/10.1021/jm00173a017 Zobrazit plný text záznamu