{{Short description|5-HT1B and 5-HT1D antagonist}} {{cs1 config|name-list-style=vanc|display-authors=6}} {{Infobox drug | drug_name = | image = GR-55562.svg | image_class = skin-invert-image | width = | caption =
<!-- Clinical data --> | pronounce = | tradename = | Drugs.com = | MedlinePlus = | licence_CA = | licence_EU = | DailyMedID = | licence_US = | pregnancy_AU = | pregnancy_category = | dependency_liability = | addiction_liability = | routes_of_administration = | class = Serotonin 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptor antagonist; Selective serotonin 5-HT<sub>1B</sub> antagonist | ATC_prefix = | ATC_suffix =
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<!-- Identifiers --> | CAS_number = 159533-26-3 | CAS_supplemental = | PubChem = 128018 | PubChemSubstance = | IUPHAR_ligand = 113 | DrugBank = | ChemSpiderID = 113523 | UNII = QPY74DMU5M | KEGG = | ChEBI = 92813 | ChEMBL = 119264 | NIAID_ChemDB = | PDB_ligand = | synonyms = GR55562; GR-55,562; GR55,562
<!-- Chemical data --> | IUPAC_name = 3-[3-(dimethylamino)propyl]-4-hydroxy-''N''-(4-pyridin-4-ylphenyl)benzamide | C=23 | H=25 | N=3 | O=2 | SMILES = CN(C)CCCC1=C(C=CC(=C1)C(=O)NC2=CC=C(C=C2)C3=CC=NC=C3)O | StdInChI = 1S/C23H25N3O2/c1-26(2)15-3-4-19-16-20(7-10-22(19)27)23(28)25-21-8-5-17(6-9-21)18-11-13-24-14-12-18/h5-14,16,27H,3-4,15H2,1-2H3,(H,25,28) | StdInChIKey = ZAGAUUVCYGSPBP-UHFFFAOYSA-N }}
'''GR-55562''' is a selective serotonin 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptor antagonist.<ref name="HalazyLamotheJorand-Lebrun1997">{{cite journal | vauthors = Halazy S, Lamothe M, Jorand-Lebrun C | title=5-HT<sub>1B/1D</sub>antagonists and depression | journal=Expert Opinion on Therapeutic Patents | publisher=Informa Healthcare | volume=7 | issue=4 | year=1997 | issn=1354-3776 | doi=10.1517/13543776.7.4.339 | pages=339–352 | quote = 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.}}</ref> It is one of several selective serotonin 5-HT<sub>1B</sub> receptor antagonists used in scientific research.<ref name="AlexanderChristopoulosDavenport2019">{{cite journal | vauthors = Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA | title = THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors | journal = British Journal of Pharmacology | volume = 176 | issue = Suppl 1 | pages = S21–S141 | date = December 2019 | pmid = 31710717 | pmc = 6844580 | doi = 10.1111/bph.14748 }}</ref><ref name="HannonHoyer2008">{{cite journal | vauthors = Hannon J, Hoyer D | title = Molecular biology of 5-HT receptors | journal = Behavioural Brain Research | volume = 195 | issue = 1 | pages = 198–213 | date = December 2008 | pmid = 18571247 | doi = 10.1016/j.bbr.2008.03.020 }}</ref>
The drug is a silent antagonist of the serotonin 5-HT<sub>1B</sub> receptor, unlike the related agent GR-127935.<ref name="HalazyLamotheJorand-Lebrun1997" /><ref name="Tocris" /> GR-55562 has around 10-fold selectivity for the serotonin 5-HT<sub>1B</sub> receptor over the serotonin 5-HT<sub>1D</sub> receptor and has only weak affinity for a number of other serotonin receptors.<ref name="Tocris">{{cite web | title=GR 55562 dihydrochloride Supplier | website=Tocris Bioscience | url=https://www.tocris.com/products/gr-55562-dihydrochloride_1054 | access-date=27 October 2024 | quote = 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.}}</ref>
It is ineffective in attenuating MDMA-induced prosocial behavior in animals.<ref name="Blanco-GandíaMateos-GarcíaGarcía-Pardo2015">{{cite journal | vauthors = Blanco-Gandía MC, Mateos-García A, García-Pardo MP, Montagud-Romero S, Rodríguez-Arias M, Miñarro J, Aguilar MA | title = Effect of drugs of abuse on social behaviour: a review of animal models | journal = Behavioural Pharmacology | volume = 26 | issue = 6 | pages = 541–570 | date = September 2015 | pmid = 26221831 | doi = 10.1097/FBP.0000000000000162 }}</ref><ref name="MorleyArnoldMcGregor2005">{{cite journal | vauthors = Morley KC, Arnold JC, McGregor IS | title = Serotonin (1A) receptor involvement in acute 3,4-methylenedioxymethamphetamine (MDMA) facilitation of social interaction in the rat | journal = Progress in Neuro-Psychopharmacology & Biological Psychiatry | volume = 29 | issue = 5 | pages = 648–657 | date = June 2005 | pmid = 15908091 | doi = 10.1016/j.pnpbp.2005.04.009 }}</ref> Conversely, the serotonin 5-HT<sub>1A</sub> receptor antagonist WAY-100635 can abolish MDMA-induced prosocial behavior.<ref name="Blanco-GandíaMateos-GarcíaGarcía-Pardo2015" /><ref name="MorleyArnoldMcGregor2005" />
== See also == * AR-A000002 * GR-127935 * SB-216641 * SB-236057
== References == {{Reflist}}
{{Serotonin receptor modulators}}
Category:5-HT1B antagonists Category:5-HT1D antagonists Category:Alcohols Category:Benzamides Category:Dimethylamino compounds Category:Experimental drugs Category:4-Pyridyl compounds Category:Anilides Category:Phenols Category:Biaryls