AZD-1134
Pharmaceutical compound
From Wikipedia, the free encyclopedia
AZD-1134 is an investigational new drug that was being evaluated for the treatment of major depressive disorder and anxiety disorders but was never marketed.[1][2][3][4]
administrationUnspecified[1]
| |
| Clinical data | |
|---|---|
| Routes of administration | Unspecified[1] |
| Drug class | Serotonin 5-HT1B receptor antagonist |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C28H32FN5O4 |
| Molar mass | 521.593 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Pharmacology
AZD-1134 is a selective serotonin 5-HT1B receptor antagonist. It has been found to increase serotonin levels in the dorsal hippocampus in animals and to increase serotonin turnover (as measured by 5-HIAA/serotonin ratio) in the cerebral cortex, hypothalamus, hippocampus, and striatum.[3] Alone, AZD-1134 increased hippocampal serotonin levels to 179% of baseline, and in combination with the selective serotonin reuptake inhibitor (SSRI) citalopram, it increased levels to 950% of baseline.[3] The increases in serotonin levels and turnover with AZD-1134 are presumably due to blockade of inhibitory presynaptic 5-HT1B autoreceptors.[3] AZD-1134 administered alone produced antidepressant-like effects in animals.[2]
History
AZD-1134 reached preclinical research prior to the discontinuation of its development.[1] It was under development by AstraZeneca.[1] Another selective serotonin 5-HT1B receptor antagonist, AZD-3783, was also subsequently developed and studied by AstraZeneca.[5][6] However, this drug was later found to produce unexpected neurotoxicity.[7]