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| Routes of administration | Unspecified [1] |
| Drug class | Serotonin 5-HT1B receptor antagonist |
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| Formula | C28H32FN5O4 |
| Molar mass | 521.593 g·mol−1 |
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AZD-1134 is an investigational new drug that was being evaluated for the treatment of major depressive disorder and anxiety disorder but was never marketed. [1] [2] [3] [4] It is a selective serotonin 5-HT1B receptor antagonist.
The drug 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]
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]
Pergolide, sold under the brand name Permax and Prascend (veterinary) among others, is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Parkinson's disease is associated with reduced dopamine synthesis in the substantia nigra of the brain. Pergolide acts on many of the same receptors as dopamine to increase receptor activity.
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RS-102221 is a drug developed by Hoffmann–La Roche, which was one of the first compounds discovered that acts as a potent and selective antagonist at the serotonin 5-HT2C receptor, with around 100× selectivity over the closely related 5-HT2A and 5-HT2B receptors. It has anxiolytic effects in animal studies, increases the effectiveness of SSRI antidepressants, and shows a complex interaction with cocaine, increasing some effects but decreasing others, reflecting a role for the 5-HT2C receptor in regulation of the dopamine signalling system in the brain.
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CP-93129 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist, with approximately 150x and 200x selectivity over the closely related 5-HT1D and 5-HT1A receptors. It is used in the study of 5-HT1B receptors in the brain, particularly their role in modulating the release of other neurotransmitters.
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WAY-163,909 is a drug which acts as a potent and reasonably selective agonist for the serotonin 5-HT2C receptor. It has antipsychotic-like effects in animal models, and has been used to study the role of the 5-HT2C receptor subtype in the action of addictive drugs such as nicotine and methamphetamine.
NAS-181, also known as MCOMM, is a selective rodent serotonin 5-HT1B receptor antagonist which is used in scientific research.
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