Chemistry:GSK-588045

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GSK-588045 is a serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptor antagonist which was under development for the treatment of depressive and anxiety disorders but was never marketed.[1][2][3][4] It is also a serotonin reuptake inhibitor, albeit much less potently than its serotonin 5-HT1 receptor antagonism.[3][4] The drug increases brain serotonin levels in animals.[3][4] It was being developed by GlaxoSmithKline.[1][2] GSK-588045 reached phase 1 clinical trials prior to the discontinuation of its development.[1][2]

See also

References

  1. ↑ 1.0 1.1 1.2 "GSK 588045". 1 August 2023. https://adisinsight.springer.com/drugs/800026155. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on GSK-588045 with Synapse". 23 January 2025. https://synapse.patsnap.com/drug/0d8248bc87064259b484f510767f250f. 
  3. ↑ 3.0 3.1 3.2 "Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045)". J Med Chem 53 (15): 5827–5843. August 2010. doi:10.1021/jm100482n. PMID 20590088. 
  4. ↑ 4.0 4.1 4.2 "In vivo occupancy of the 5-HT1A receptor by a novel pan 5-HT1(A/B/D) receptor antagonist, GSK588045, using positron emission tomography". Neuropharmacology 92: 44–48. May 2015. doi:10.1016/j.neuropharm.2014.11.017. PMID 25476970. https://www.researchgate.net/publication/269187027. "GSK588045 is a 5-HT1A/1B/1D antagonist which has been characterised functionally in vitro using [35S]-GTPgS-SPA binding to h5- HT1A (HEK), h5-HT1B (CHO), and h5-HT1D (CHO) cell membranes. It has a high affinity for 5-HT1 autoreceptors (in vitro human 5-HT1A/ 1B/1D pKi 9.9, 9.1 and 10.0 respectively), with moderate activity at the 5-HT transporter (in vitro human 5-HTT pKi 7.5), which elevates brain 5-HT release acutely in animal models (Bromidge et al., 2010).". 





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