879208-43-2

Upstream product

• 141197-04-8 (1S,7aS)-hexahydro-1H-pyrrolizin-1-ylmethylamine 
• 526-64-7 laburnine 
• 111975-23-6 (S)-5-[(R)-3-Chloro-1-((S)-4-isopropyl-2-thioxo-thiazolidine-3-carbonyl)-propyl]-pyrrolidin-2-one 
• 24201-13-6 4-(acetylamino)-5-chloro-2-methoxybenzoic acid 
• 141119-76-8 2-[(1S,7aS)-hexahydro-1H-pyrrolizin-1-ylmethyl]-1H-isoindole-1,3(2H)-dione 

Relevant academic research and scientific papers

Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists

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 (TMM) assay, 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 12a (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 12h (SC-53606), which is a potent and selective 5-HT4 receptor antagonist with a pA2 value of 8.13 in the rat TMM assay. N-Methyl indole ester 13d was identified as a potent 5-HT 4 antagonist with a pA2 value of 8.93. High selectivity was observed for these pyrrolizidine derivatives versus other monoamine receptors, including 5-HT1, 5-HT2, D1, D 2, α1, α2, and β receptors. 2006 American Chemical Society.