SB-247853
Pharmaceutical compound
From Wikipedia, the free encyclopedia
SB-247853 is a highly selective serotonin 5-HT2C receptor inverse agonist which was under development for the treatment of major depressive disorder but was never marketed.[1][4][5][6][2][7]
administrationUnknown/unspecified (but orally active)[1][2][3]
- None
| |
| Clinical data | |
|---|---|
| Other names | SB247853 |
| Routes of administration | Unknown/unspecified (but orally active)[1][2][3] |
| Drug class | Serotonin 5-HT2C receptor inverse agonist |
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C22H19F3N4O2 |
| Molar mass | 428.415 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Its affinities (Ki) were found to be 0.50 nM for the serotonin 5-HT2C receptor, 60 nM for the serotonin 5-HT2B receptor, and 1,300 nM for the serotonin 5-HT2A receptor.[5][2] Hence, it shows 120-fold selectivity for the serotonin 5-HT2C receptor over the serotonin 5-HT2B receptor and 2,600-fold selectivity for the serotonin 5-HT2C receptor over the serotonin 5-HT2A receptor.[5][2] The drug reverses the hypolocomotion induced by the serotonin 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP) in rodents.[5][2] It is orally active.[2][3]
The drug produced orthostatic intolerance in healthy human volunteers during the first dose-escalation clinical study.[3] Subsequently, it was found to cause substantial hypotension (low blood pressure) and presyncope (pre-fainting symptoms) in the tilt table test.[3] It was concluded based on these findings that the serotonin 5-HT2C receptor is involved in regulating the cardiovascular system.[3]
SB-247853 was first described in the scientific literature by 2000.[2] It was developed by GlaxoSmithKline.[1][4][5] The drug reached phase 1 clinical trials prior to the discontinuation of its development in 2005.[1][4]