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ARC-239

Names

[ CAS No. ]:
67339-62-2

[ Name ]:
ARC-239

[Synonym ]:
ARC 239 dihydrochloride,2-[2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolindionedihydrochloride

Biological Activity

[Description]:

ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM[1][2].

[Related Catalog]:

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

[Target]

human α2C-adrenoceptor:6.95 (pKi)

Alpha-2C adrenergic receptor:7.06 (pKi)

5-HT1A Receptor:63.1 nM (Ki)


[References]

[1]. K T Gavin, et al. Alpha 2C-adrenoceptors mediate contractile responses to noradrenaline in the human saphenous vein. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):406-11.  

[2]. J J Meana, et al. The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Eur J Pharmacol. 1996 Oct 3;312(3):385-8.  

Chemical & Physical Properties

[ Density]:
1.167g/cm3

[ Boiling Point ]:
595.8ºC at 760 mmHg

[ Molecular Formula ]:
C24H29N3O3

[ Molecular Weight ]:
407.51

[ Flash Point ]:
314.1ºC

[ Exact Mass ]:
479.17400

[ PSA ]:
53.09000

[ LogP ]:
4.32220

[ Index of Refraction ]:
1.576

MSDS


Related Compounds