S8817
SB 218795
>98% (HPLC)
Synonym(s):
(−)-(R)-N-(α-Methoxycarbonylbenzyl)-2-phenylquinoline-4-carboxamide
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About This Item
Empirical Formula (Hill Notation):
C25H20N2O3
Molecular Weight:
396.44
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
Assay
>98% (HPLC)
form
solid
color
white
solubility
DMSO: soluble 40 mg/mL
H2O: insoluble
storage temp.
2-8°C
SMILES string
COC(=O)[C@H](NC(=O)c1cc(nc2ccccc12)-c3ccccc3)c4ccccc4
Gene Information
human ... TACR2(6865) , TACR3(6870)
Application
The pharmacodynamics profile of SB 218795 enables its use as a tool to study physiological and pathophysiological roles of NK-3 receptor in CNS-modulated behaviors.
Biochem/physiol Actions
SB 218795 is a 2-phenyl-4-quinolinecarboxamides and a selective, reversible and competitive antagonist of human NK-3 receptor that effectively crosses the blood-brain barrier. It inhibits the NK-3 receptor-induced miosis or pupil constriction in conscious rabbits.1,2
Non-peptide NK3 tachykinin receptor antagonist.
Legal Information
Sold for research purposes under agreement from GlaxoSmithKline
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Certificates of Analysis (COA)
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A D Medhurst et al.
British journal of pharmacology, 122(3), 469-476 (1997-11-14)
1. Inhibition of NK3 receptor agonist-induced contraction in the rabbit isolated iris sphincter muscle was used to assess the in vitro functional activity of three 2-phenyl-4-quinolinecarboxamides, members of a novel class of potent and selective non-peptide NK3 receptor antagonists. In
H M Sarau et al.
The Journal of pharmacology and experimental therapeutics, 295(1), 373-381 (2000-09-19)
The pharmacological and pharmacokinetic profile of SB-222200 [(S)-(-)-N-(alpha-ethylbenzyl)-3-methyl-2-phenylquinoline-4-car boxami de], a human NK-3 receptor (hNK-3R) antagonist, was determined. SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i)
Jin Zhu et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 34(3), 768-780 (2014-08-30)
Activated microglia perform many of the immune effector functions typically associated with macrophages. However, the regulators involved in microglial activation are not well defined. Because microglia play a pivotal role in immune surveillance of the CNS, we studied the effect
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