Chemistry:GR-46611

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GR-46611 is a non-selective serotonin 5-HT1 receptor agonist of the triptan group which has been used in scientific research.[1][2][3][4] It is specifically an agonist of the serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptors.[4] The drug's affinities (Ki) are 1.3 nM for the serotonin 5-HT1A receptor, 0.1 to 1.3 nM for the serotonin 5-HT1B receptor, and 0.2 to 1.0 nM for the serotonin 5-HT1D receptor.[3][4][5] Conversely, it showed very weak affinity for the serotonin 5-HT2A receptor (Ki = 1,000 nM).[4] The drug does not alter or stimulate locomotor activity when given alone in rodents, but does potentiate the hyperlocomotion induced by the serotonin 5-HT1A receptor agonists 8-OH-DPAT and buspirone.[2] The chemical synthesis of GR-46611 has been described.[3] GR-46611 was first described in the scientific literature by 1994.[6]

See also

References

  1. ↑ "Delving into the Latest Updates on GR-46611 with Synapse". 16 May 2026. https://synapse.patsnap.com/drug/139235f287ca43a18196406cb8b6b1e6. 
  2. ↑ 2.0 2.1 "GR46611 potentiates 5-HT1A receptor-mediated locomotor activity in the guinea pig". Eur J Pharmacol 370 (2): 85–92. April 1999. doi:10.1016/s0014-2999(99)00090-4. PMID 10323255. 
  3. ↑ 3.0 3.1 3.2 "5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates". J Med Chem 39 (24): 4717–4726. November 1996. doi:10.1021/jm9604890. PMID 8941384. 
  4. ↑ 4.0 4.1 4.2 4.3 "Effects of the 5-HT receptor antagonists GR127935 (5-HT1B/1D) and MDL100907 (5-HT2A) in the consolidation of learning". Behav Brain Res 89 (1-2): 217–223. December 1997. doi:10.1016/s0166-4328(97)00055-7. PMID 9475628. 
  5. ↑ "Simultaneous quantification of serotonin, dopamine and noradrenaline levels in single frontal cortex dialysates of freely-moving rats reveals a complex pattern of reciprocal auto- and heteroreceptor-mediated control of release". Neuroscience 84 (2): 413–429. May 1998. doi:10.1016/s0306-4522(97)00565-4. PMID 9539213. 
  6. ↑ "Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists". J Med Chem 37 (15): 2253–2257. July 1994. doi:10.1021/jm00041a001. PMID 8057272. 



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