GR-46611

GR-46611
Clinical data
Other names	GR46611
Drug class	Serotonin 5-HT1 receptor agonist; Serotonin 5-HT1A receptor agonist; Serotonin 5-HT1B receptor agonist; Serotonin 5-HT1D receptor agonist
ATC code	None;
Identifiers
	IUPAC name (E)-3-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-[(4-methoxyphenyl)methyl]prop-2-enamide;
CAS Number	185259-85-2;
PubChem CID	6160690;
ChemSpider	4827659;
ChEBI	CHEBI:93195;
ChEMBL	ChEMBL344127;
Chemical and physical data
Formula	C23H27N3O2
Molar mass	377.488 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN(C)CCC1=CNC2=C1C=C(C=C2)/C=C/C(=O)NCC3=CC=C(C=C3)OC;
	InChI InChI=1S/C23H27N3O2/c1-26(2)13-12-19-16-24-22-10-6-17(14-21(19)22)7-11-23(27)25-15-18-4-8-20(28-3)9-5-18/h4-11,14,16,24H,12-13,15H2,1-3H3,(H,25,27)/b11-7+; Key:LBVZWEWTNUDWNS-YRNVUSSQSA-N;

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-HT_1A, 5-HT_1B, and 5-HT_1D receptors.^[4] The drug's affinities (K_i) are 1.3 nM for the serotonin 5-HT_1A receptor, 0.1 to 1.3 nM for the serotonin 5-HT_1B receptor, and 0.2 to 1.0 nM for the serotonin 5-HT_1D receptor.^[3]^[4]^[5] Conversely, it showed very weak affinity for the serotonin 5-HT_2A receptor (K_i = 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-HT_1A 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]