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NAS-181

Names

[ CAS No. ]:
205242-62-2

[ Name ]:
NAS-181

[Synonym ]:
nas-181

Biological Activity

[Description]:

NAS-181 is a potent and selective rat 5-hydroxytryptamine1B (r5-HT1B) antagonist with an Ki value of 47 nM. NAS-181 increases the 5-HTP accumulation in rat brain regions[1].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[In Vitro]

NAS-181 (compound (R)-25) (0-1000 nM) increases the K+-stimulated release of [3H]-5-HT from rat occipital cortical slices[1]. NAS-181 (3 mg/kg; s.c.) increases in the number of wet dog shakes in rats, and the effect is abolished by pretreatment of the rats with the tryptophan hydroxylase inhibitor p-chlorophenylalanine (pCPA) (200 mg/kg; i.p.)[1].

[In Vivo]

NAS-181 (20 mg/kg; s.c.) increases the 5-HTP accumulation in rat brain regions[1]. Animal Model: Rats[1] Dosage: 20 mg/kg Administration: S.c. Result: Significantly increased the 5-HTP accumulation in hypothalamus, hippocampus, frontal cortex, striatum, and the ratio 5-HIAA/5-HT in these brain regions was even more elevated (40−60%).

[References]

[1]. Berg S, et al. (R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist. J Med Chem. 1998 May 21;41(11):1934-42.

Chemical & Physical Properties

[ Boiling Point ]:
765ºC at 760 mmHg

[ Molecular Formula ]:
C21H34N2O10S2

[ Molecular Weight ]:
538.63200

[ Flash Point ]:
416.5ºC

[ Exact Mass ]:
538.16500

[ PSA ]:
177.69000

[ LogP ]:
2.59810

[ Vapour Pressure ]:
1.31E-24mmHg at 25°C

Related Compounds