Bulk Inquiry
GMC 2-29
- Soluble in DMSO
- MF: C29H31N5O3
- MW: 497.59
Description
GMC 2-29 is a highly potent and selective 5-HT1B/1D receptor antagonist with IC50 of 0.93 nM. It was reported to show even greater potency than GR 127935 (Axon 1813) in functional assays. It is useful for blocking serotonin 5-HT1B/1D receptor-mediated responses.
5-HT1B and 5-HT1D receptors are Gi/o-coupled serotonin receptors involved in vascular, neuronal and migraine-related pathways. GMC 2-29 enables functional studies of these receptor subtypes and comparison with established antagonists such as GR 127935.
Key Features
- Highly potent and selective 5-HT1B/5-HT1D antagonist
- IC50 values of 0.93 nM (5-HT1B), 37 nM (5-HT1D) and >1000 nM (5-HT1A)
- Reportedly higher potency than GR 127935 in functional assays
- Useful for serotonin receptor blockade studies
Applications
- Serotonin receptor pharmacology
- Serotonergic GPCR antagonist assays
- Migraine and vascular signaling models
More Information
| Parent CAS No. | 148672-15-5 |
|---|---|
| Chemical Name | 2'-Methyl-4'-(5-methyl-[1,3,4]oxadiazol-2-yl)-biphenyl-4-carboxylic acid [4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide |
| SMILES | N1(C2=CC(=CC=C2OC)NC(=O)C2C=CC(=CC=2)C2C(C)=CC(C3OC(C)=NN=3)=CC=2)CCN(C)CC1 |
| MFCD | MFCD00919101 |
| InChi | InChI=1S/C29H31N5O3/c1-19-17-23(29-32-31-20(2)37-29)9-11-25(19)21-5-7-22(8-6-21)28(35)30-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34/h5-12,17-18H,13-16H2,1-4H3,(H,30,35) |
| InChiKey | QXLNAYIFEMXTDZ-UHFFFAOYSA-N |
| CID | 10323598 |
| Short Description | 5-HT1B/1D antagonist |
References
- Y Liao et al. New selective and potent 5-HT1B/1D or 5-HT1B antagonists: chemistry and pharmacological evaluation of GR127935-like compounds. J. Med. Chem. 2000, 43, 517-525.
- JW Clitherow et al. Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J. Med. Chem. 1994, 37, 2253.
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