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GMC 15-27
- No solubility data
- MF: C27H31N5O2
- MW: 457.57
Description
GMC 15-27 is a highly potent and selective serotonin 5-HT1B/1D receptor antagonist and reported to show 1.5 times more potency than GR 127935 (Axon 1813) in functional assays. It is suited for serotonin receptor blockade in functional assays.
5-HT1B/1D receptor antagonists are used to investigate presynaptic serotonergic regulation, vascular responses and migraine-relevant signaling. GMC 15-27 can serve as a potent tool for 5-HT1B/1D receptor pharmacology.
Key Features
- Selective 5-HT1B/5-HT1D antagonist
- IC50 values of 0.5 nM, 3 nM, 23 nM for 5-HT1B, 5-HT1D and 5-HT1A
- 1.5 times more potent than GR 127935 in functional assays
- Useful for functional serotonin receptor assays
Applications
- 5-HT1B/1D receptor pharmacology
- Serotonergic signaling research
- Migraine pathway models
- GPCR antagonist potency comparison
More Information
| Parent CAS No. | 256227-71-1 |
|---|---|
| Chemical Name | 4'-Carbamimidoyl-2'-methyl-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(C(N)=N)=CC=2)CCN(C)CC1 |
| MFCD | MFCD10565904 |
| InChi | InChI=1S/C27H31N5O2/c1-18-16-21(26(28)29)8-10-23(18)19-4-6-20(7-5-19)27(33)30-22-9-11-25(34-3)24(17-22)32-14-12-31(2)13-15-32/h4-11,16-17H,12-15H2,1-3H3,(H3,28,29)(H,30,33) |
| InChiKey | LBFHWQWAWLKTEK-UHFFFAOYSA-N |
| CID | 9846928 |
| 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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