Home
Resources
Publications
Synthesis and Structure-Activity Relationship Studies in Serotonin 5-HT(1A) Receptor Agonists Based on Fused Pyrrolidone Scaffolds

Synthesis and Structure-Activity Relationship Studies in Serotonin 5-HT(1A) Receptor Agonists Based on Fused Pyrrolidone Scaffolds

Andrea Cappelli, Monica Manini, Salvatore Valenti, Federica Castriconi, Germano Giuliani, Maurizio Anzini, Simone Brogi, Stefania Butini, Sandra Gemma, Giuseppe Campiani, Gianluca Giorgi, Laura Mennuni, etc.

Eur J Med Chem. 2013 May;63:85-94.

PMID: 23466604

Abstract:

A new class of serotonin 5-HT1A receptor ligands related to NAN-190, buspirone and aripiprazole has been designed using our potent 5-HT3 receptor ligands as templates. The designed pyrrolidone derivatives 10a-n were prepared by means of the straightforward chemistry consisting in the reaction of the appropriate γ-haloester derivatives with the suitable arylpiperazinylalkylamines. The nanomolar 5-HT1A receptor affinity and the agonist-like profile shown by fused pyrrolidone derivatives 10k,m stimulated the rationalization of the interaction with an homology model of the 5-HT1A receptor and the evaluation of their selectivity profiles and the pharmacokinetic properties. Interestingly, the results of the profiling assays suggested for close congeners 10k,m a significantly divergent binding pattern with compound 10m showing an appreciable selectivity for 5-HT1AR.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP257877444	Buspirone Related Compound N		257877-44-4	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: