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SDZ NKT 343

Names

[ CAS No. ]:
180046-99-5

[ Name ]:
SDZ NKT 343

[Synonym ]:
Lauryl-LF 11

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]:

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.

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

Related Compounds