SB 218795

Names

[ Name ]:
SB 218795

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[Target]

hNK3:13 nM (Ki)

hNK2:1220 nM (Ki)

[In Vitro]

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].

[In Vivo]

SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%[2].

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.237g/cm3

[ Boiling Point ]:
623.7ºC at 760 mmHg

[ Molecular Formula ]:
C₂₅H₂₀N₂O₃

[ Molecular Weight ]:
396.44

[ Flash Point ]:
331ºC

[ Exact Mass ]:
396.14700

[ PSA ]:
68.29000

[ LogP ]:
4.93680

[ Vapour Pressure ]:
1.78E-15mmHg at 25°C

[ Index of Refraction ]:
1.643

[ Storage condition ]:
-20°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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