Title : Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT2C and negative allosteric modulator of 5-HT2B receptors.

Pub. Date : 2019 Feb 15

PMID : 30622024






3 Functional Relationships(s)
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1 Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT2C and negative allosteric modulator of 5-HT2B receptors. Piperazine 5-hydroxytryptamine receptor 2C Rattus norvegicus
2 Interestingly, piperazine linked phenyl cyclopropyl methanones (58) was active as PAM of 5-HT2C (increased the Emax of 5-HT to 139%), and as negative allosteric modulator (NAM) of 5-HT2B (decreases EC50 of 5-HT 10 times without affecting Emax). Piperazine 5-hydroxytryptamine receptor 2C Rattus norvegicus
3 Therefore, these results suggest that piperazine moiety is essential for dual activity (PAM & NAM) of compounds 58, and supports the hypothesis of 5-HT2C PAM for the treatment of obesity similar to the full agonist. Piperazine 5-hydroxytryptamine receptor 2C Rattus norvegicus