Becker, Daniel P.; Flynn, Daniel L.; Moormann, Alan E.; Nosal, Roger; Villamil, Clara I.; Loeffler, Richard; Gullikson, Gary W.; Moummi, Chafiq; Yang, Dai-C. published the artcile< Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists>, Name: 5-Fluoro-1H-indole-3-carboxylic acid, the main research area is pyrrolizidine arylamide preparation 5HT4 antagonist; arylester pyrrolizidine preparation 5HT4 agonist.
A series of pyrrolizidine esters, amides, and ureas was prepared and tested for 5-HT4 and 5-HT3 receptor binding, 5-HT4 receptor agonism in the rat tunica muscularis mucosae assay (TMM), and for 5-HT3 receptor-mediated functional antagonism in the Bezold-Jarisch reflex assay. Several pyrrolizidine derivatives were identified with high affinity for the 5-HT4 receptor, including benzamide I (SC-53116), a potent and selective 5-HT4 partial agonist that exhibits efficacy in promoting antral contractions and activity in promoting gastric emptying in canine models. Also discovered were 5-HT4 receptor antagonists, including imidazopyridine amide II (SC-53606), which was a potent and selective 5-HT4 receptor antagonist with a pA2 value of 8.13 in the rat TMM assay. N-Me indole ester III was identified as a potent 5-HT4 antagonist with a pA2 value of 8.93. High selectivity was observed for these pyrrolizidine derivatives vs. other monoamine receptors, including 5-HT1, 5-HT2, D1, D2, α1, α2, and β receptors.
Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Name: 5-Fluoro-1H-indole-3-carboxylic acid.
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