GR-127935

{{Short description|Drug}}

{{Drugbox

| Verifiedfields = changed

| verifiedrevid = 451223322

| IUPAC_name = N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1-1'-biphenyl-4-carboxamide

| image = GR-127,935_structure.png

| width = 250

| tradename =

| pregnancy_category =

| legal_status =

| routes_of_administration =

| bioavailability =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number_Ref = {{cascite|correct|??}}

| CAS_number = 148672-13-3

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 2LLH6CEB40

| ATC_prefix = none

| ATC_suffix =

| PubChem = 107780

| ChEMBL_Ref = {{ebicite|changed|EBI}}

| ChEMBL = 15928

| IUPHAR_ligand = 14

| ChemSpiderID = 96935

| ChEBI = 64114

| C=29 | H=31 | N=5 | O=3

| smiles = n5oc(C)nc5-c(cc2C)ccc2-c(cc3)ccc3C(=O)Nc(ccc1OC)cc1N4CCN(C)CC4

| StdInChI = 1S/C29H31N5O3/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34/h5-12,17-18H,13-16H2,1-4H3,(H,31,35)

| StdInChIKey = YDBCEBYHYKAFRX-UHFFFAOYSA-N

}}

GR-127935 is a drug which acts as a selective antagonist at the serotonin receptors 5-HT_1B and 5-HT_1D.{{cite journal |vauthors=Skingle M, Beattie DT, Scopes DI, Starkey SJ, Connor HE, Feniuk W, Tyers MB |title=GR127935: a potent and selective 5-HT1D receptor antagonist |journal=Behavioural Brain Research |volume=73 |issue=1–2 |pages=157–61 |year=1996 |pmid=8788495 |doi= 10.1016/0166-4328(96)00089-7|s2cid=34394584 }} It has little effect when given by itself but blocks the antiaggressive effect of 5-HT_1B agonists,{{cite journal |vauthors=Bannai M, Fish EW, Faccidomo S, Miczek KA |title=Anti-aggressive effects of agonists at 5-HT1B receptors in the dorsal raphe nucleus of mice |journal=Psychopharmacology |volume=193 |issue=2 |pages=295–304 |date=August 2007 |pmid=17440711 |doi=10.1007/s00213-007-0780-5 |s2cid=6766784 }} and alters release of serotonin in the brain,{{cite journal |vauthors=Rex A, Voigt JP, Wicke KM, Fink H |title=In vivo/ex vivo and behavioural study on central effects of 5-HT1B/1D and 5-HT1A antagonists in guinea pigs |journal=Pharmacology Biochemistry and Behavior |volume=88 |issue=3 |pages=196–204 |date=January 2008 |pmid=17888505 |doi=10.1016/j.pbb.2007.07.016 |s2cid=26577695 }} as well as reducing drug-seeking behaviour in cocaine addicted rats.{{cite journal |vauthors=Przegaliński E, Gołda A, Filip M |title=Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats |journal=Pharmacological Reports |volume=60 |issue=6 |pages=798–810 |year=2008 |pmid=19211971 }}