N-(1-Methyl-5-indolyl)-N’-(3-pyridyl)urea hydrochloride: the first selective 5-HT1C receptor antagonist was written by Forbes, Ian T.;Kennett, Guy A.;Gadre, Angela;Ham, Peter;Hayward, Clare J.;Martin, Roger T.;Thompson, Mervyn;Wood, Martyn D.;Baxter, Gordon S.. And the article was included in Journal of Medicinal Chemistry in 1993.Related Products of 85696-95-3 This article mentions the following:
Development of specific 5-HT1C receptor antagonists has been impeded by the marked similarity between this site and the 5-HT2 receptor. A series of pyridyl indolyl ureas I (4-, 5-, 6-, 7-NHCOCNHR1; R1 = 3-pyridyl) were synthesized and shown to have affinity for the 5-HT1C receptor. One of these, I (R = 5-NHCONHR1, R1 = 3-pyridyl)(II) shows ≥48 fold selectivity in ligand binding studies for the 5-HT1C (pKI = 6.86) over the 5-HT2, 5-HT1A, 5-HT1D, 5-HT3, adrenergic α1, α2A, α2B, β1, β2, dopaminergic D1, and D2 receptors. II is a silent, competitive antagonist of 5-HT-stimulated phosphoinositide hydrolysis in the pig choroid plexus (pKB = 7.03), a model of 5-HT1C receptor functional activity and was also a surmountable antagonist of the 5-HT1C-like receptor in the rat stomach fundus (pA2 = 7.52). Thus, II represents the first reported selective 5-HT1C receptor antagonist. In the experiment, the researchers used many compounds, for example, 1-Methyl-1H-indol-4-amine (cas: 85696-95-3Related Products of 85696-95-3).
1-Methyl-1H-indol-4-amine (cas: 85696-95-3) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Related Products of 85696-95-3
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles