For research use only. Not for therapeutic Use.
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit[1][2].
SB 218795 (3-30 nM) antagonizes the contractile responses induced by the NK3 receptor agonist senktide in a surmountable and concentration-dependent manner[2].
SB 218795 (0.3-3 μM) does not affect the contractile responses of the NK3 receptor agonist [MePhe7]-NKB in the rabbit iris sphincter muscle[2].
SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%[2].
| Catalog Number | I009314 |
| CAS Number | 174635-53-1 |
| Synonyms | methyl (2R)-2-phenyl-2-[(2-phenylquinoline-4-carbonyl)amino]acetate |
| Molecular Formula | C25H20N2O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H20N2O3/c1-30-25(29)23(18-12-6-3-7-13-18)27-24(28)20-16-22(17-10-4-2-5-11-17)26-21-15-9-8-14-19(20)21/h2-16,23H,1H3,(H,27,28)/t23-/m1/s1 |
| InChIKey | IUMQXQJZIHWLIN-HSZRJFAPSA-N |
| SMILES | COC(=O)C(C1=CC=CC=C1)NC(=O)C2=CC(=NC3=CC=CC=C32)C4=CC=CC=C4 |
| Reference | [1]. Giardina GA, et, al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J Med Chem. 1997 Jun 6;40(12):1794-807. [2]. Medhurst AD, et, al. In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br J Pharmacol. 1997 Oct;122(3):469-76. [3]. Valero MS, et, al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin. 2011 Apr;32(4):487-94. |
