180046-99-5

180046-99-5 structure

Name: SDZ NKT 343
Chemical Name: (2S)-2-N-[(2S)-1-[benzyl(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-1-N-(2-nitrophenyl)pyrrolidine-1,2-dicarboxamide
CAS Number: 180046-99-5
Molecular Formula: C₃₃H₃₃N₅O₅
Molecular Weight: 579.64600
Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
Create Date: 2018-12-24 06:39:37
Modify Date: 2024-01-09 09:59:58
SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity[1][2].

Name	(2S)-2-N-[(2S)-1-[benzyl(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-1-N-(2-nitrophenyl)pyrrolidine-1,2-dicarboxamide
Synonyms	Lauryl-LF 11

Description	SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity[1][2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor
Target	hNK1:0.62 nM (IC50) hNK2:0.52 μM (Ki) hNK3:3.4 μM (Ki)
In Vitro	SDZ NKT 343 shows a markedly lower affinity at rat NK1 receptors in whole forebrain membranes (IC50=451+139 nM)[1]. SDZ NKT 343 shows weak affinity to human NK2 and NK3 receptors in transfected Cos-7 cells (Ki of 0.52+0.04 μM and 3.4+1.2 μM respectively)[1].
In Vivo	SDZ NKT 343 antagonized [Sar9]SP sulphone-evoked bronchoconstriction (70% reduction at 0.4 mg/kg, i.v.) in anaesthetized guinea-pigs[1].
References	[1]. Walpole CS, et al. Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br J Pharmacol. 1998 May;124(1):83-92. [2]. Walpole C, et al. 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. J Med Chem. 1998 Aug 13;41(17):3159-73.