Chemistry:AZD-3783

From HandWiki

AZD-3783 is a serotonin 5-HT1B receptor antagonist which was under development for the treatment of major depressive disorder and anxiety disorders.[1][2][3][4][5] It was being developed by AstraZeneca.[1][2] The drug reached phase 1 clinical trials prior to the discontinuation of its development.[1][2] It was discontinued following unexpected neurotoxicity findings in animals.[6]

See also

References

  1. ↑ 1.0 1.1 1.2 "AZD 3783". 18 December 2007. https://adisinsight.springer.com/drugs/800025787. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on AZD-3783 with Synapse". 23 January 2025. https://synapse.patsnap.com/drug/f9a1583574a94460a265e2edd343d1c5. 
  3. ↑ "The 5-HT1B receptor - a potential target for antidepressant treatment". Psychopharmacology 235 (5): 1317–1334. May 2018. doi:10.1007/s00213-018-4872-1. PMID 29546551. "Given the inhibitory effect of 5-HT1B receptors on serotonin release and the predominantly prevailing serotonin hypothesis of MDD, it makes sense to block 5-HT1B receptors for antidepressant effect (Slassi 2002). Thus far, most 5-HT1B receptor drug candidates for MDD treatment have been antagonists, such as SB-616234-A (Dawson et al. 2006), AZD3783 (Zhang et al. 2011), and AR-A000002 (Hudzik et al. 2003). It has been proposed that 5-HT1 receptor activation counteracts the serotonin-enhancing effects of SSRI and thereby contribute to the latency of therapeutic effect (Blier and de Montigny 1994; Nutt 2002). SSRI-induced downregulation of 5-HT1 receptors would then restore the serotonin-elevating effects of the drugs and hence enable a clinical effect, providing a rationale for blocking 5-HT1B receptors for rapid antidepressant response.". 
  4. ↑ "Preclinical pharmacology and pharmacokinetics of AZD3783, a selective 5-hydroxytryptamine 1B receptor antagonist". The Journal of Pharmacology and Experimental Therapeutics 339 (2): 567–578. November 2011. doi:10.1124/jpet.110.174433. PMID 21825000. 
  5. ↑ "Dose-dependent binding of AZD3783 to brain 5-HT1B receptors in non-human primates and human subjects: a positron emission tomography study with [11C]AZ10419369". Psychopharmacology 213 (2–3): 533–545. February 2011. doi:10.1007/s00213-011-2165-z. PMID 21234549. 
  6. ↑ "Pathology and Neurotoxicity in Dogs after Repeat Dose Exposure to a Serotonin 5-HT1B Inhibitor". Journal of Toxicologic Pathology 27 (1): 31–42. April 2014. doi:10.1293/tox.2013-0033. PMID 24791065. 



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