SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a K_i 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.

SB 218795 (3-30 nM) antagonizes the contractile responses induced by the NK3 receptor agonist senktide in a surmountable and concentration-dependent manner.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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  . 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.  [Content Brief]

  . Valero MS, et, al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin. 2011 Apr;32(4):487-94.  [Content Brief]