SDZ NKT 343

Modify Date: 2024-01-09 09:59:58

SDZ NKT 343 Structure
SDZ NKT 343 structure
Common Name SDZ NKT 343
CAS Number 180046-99-5 Molecular Weight 579.64600
Density 1.327g/cm3 Boiling Point 892.8ºC at 760mmHg
Molecular Formula C33H33N5O5 Melting Point N/A
MSDS N/A Flash Point 493.8ºC

 Use of SDZ NKT 343


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].

 Names

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
Synonym More Synonyms

 SDZ NKT 343 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.327g/cm3
Boiling Point 892.8ºC at 760mmHg
Molecular Formula C33H33N5O5
Molecular Weight 579.64600
Flash Point 493.8ºC
Exact Mass 579.24800
PSA 127.57000
LogP 6.05540
Vapour Pressure 0mmHg at 25°C
Index of Refraction 1.676

 Synonyms

Lauryl-LF 11