Pub. Date : 2019 Feb 15
PMID : 30622024
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
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 |