Chemistry:GR-55562

From HandWiki

GR-55562 is a selective serotonin 5-HT1B and 5-HT1D receptor antagonist.[1] It is one of several selective serotonin 5-HT1B receptor antagonists used in scientific research.[2][3]

The drug is a silent antagonist of the serotonin 5-HT1B receptor, unlike the related agent GR-127935.[1][4] GR-55562 has around 10-fold selectivity for the serotonin 5-HT1B receptor over the serotonin 5-HT1D receptor and has only weak affinity for a number of other serotonin receptors.[4]

It is ineffective in attenuating MDMA-induced prosocial behavior in animals.[5][6] Conversely, the serotonin 5-HT1A receptor antagonist WAY-100635 can abolish MDMA-induced prosocial behavior.[5][6]

See also

References

  1. ↑ 1.0 1.1 "5-HT1B/1Dantagonists and depression". Expert Opinion on Therapeutic Patents (Informa Healthcare) 7 (4): 339–352. 1997. doi:10.1517/13543776.7.4.339. ISSN 1354-3776. "However, as mentioned above, it was later found that GR-127935 is not a silent antagonist at human 5- HT1B/1D sites. More recent investigations from Glaxo and others have shown that, unlike GR-127935, GR55562 could be characterised as a silent, potent and selective h5-HT1B receptor antagonist [43]. However, so far no results have been disclosed concerning the ability of this particular compound to antagonise central presynaptic 5-HT1B receptors upon systemic administration.". 
  2. ↑ "THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors". British Journal of Pharmacology 176 (Suppl 1): S21–S141. December 2019. doi:10.1111/bph.14748. PMID 31710717. 
  3. ↑ "Molecular biology of 5-HT receptors". Behavioural Brain Research 195 (1): 198–213. December 2008. doi:10.1016/j.bbr.2008.03.020. PMID 18571247. 
  4. ↑ 4.0 4.1 "GR 55562 dihydrochloride Supplier". https://www.tocris.com/products/gr-55562-dihydrochloride_1054. "GR 55562 dihydrochloride is a selective competitive 5-HT1B (5-HT1Dβ) silent antagonist with pKB values of 7.3 and 6.3 for human cloned 5-HT1B and 5-HT1D receptors respectively and only weak binding at a number of other 5-HT subtypes." 
  5. ↑ 5.0 5.1 "Effect of drugs of abuse on social behaviour: a review of animal models". Behavioural Pharmacology 26 (6): 541–570. September 2015. doi:10.1097/FBP.0000000000000162. PMID 26221831. 
  6. ↑ 6.0 6.1 "Serotonin (1A) receptor involvement in acute 3,4-methylenedioxymethamphetamine (MDMA) facilitation of social interaction in the rat". Progress in Neuro-Psychopharmacology & Biological Psychiatry 29 (5): 648–657. June 2005. doi:10.1016/j.pnpbp.2005.04.009. PMID 15908091. 



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