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ARC 239 dihydrochloride Sale

(Synonyms: ARC?239二盐酸盐) 目录号 : GC10965

An α2B-adrenergic receptor antagonist

ARC 239 dihydrochloride Chemical Structure

Cas No.:55974-42-0

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5mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Description

ARC 239 dihydrochloride is a selective antagonist of α2B adrenoceptor with pKD value of 8.8 [1].

α2B adrenoceptor is a G-protein coupled receptor. α2-adrenergic receptors include three subtypes: α2A, α2B and α2C, which play an important role in regulating neurotransmitter release from adrenergic neurons in the central nervous system and from sympathetic nerves.

ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist. In rat brain, ARC 239 inhibited the binding of 5-HTIA receptor radioligands 8-OH-DPAT and RX 821002 to cortical membranes with Ki values of 63.1 and 136 nM respectively, which suggested that ARC 239 recognized 5-HT1A receptor [2]. Treatment human platelets with ARC 239 significantly inhibited platelet aggregation induced by adenosine diphosphate (ADP), epinephrine and arachidonic acid and increased collagen/epinephrine closure time, which suggested that α2B adrenoceptor play a critical role in platelet aggregation [3]. In cervical samples isolated from pregnant rats, ARC 239 effectively inhibited noradrenaline-stimulated contractions [4].

In C57BL/6 mice with gastric mucosal damage induced by acidified ethanol, ARC 239 (10.4 nM) antagonized gastroprotective effect induced by α2-adrenoceptor agonists [5].

References:
[1].  Bylund DB, Ray-Prenger C, Murphy TJ. Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. J Pharmacol Exp Ther, 1988, 245(2): 600-607.
[2].  Meana JJ, Callado LF, Pazos A, 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, 312(3): 385-388.
[3].  Marketou ME, Kintsurashvili E, Androulakis NE, et al. Blockade of platelet alpha2B-adrenergic receptors: a novel antiaggregant mechanism. Int J Cardiol, 2013, 168(3): 2561-2566.
[4].  Gál A, Kolarovszki-Sipiczki Z, et al. The effect of the ARC 239 on the myometrial and cervical action in the rat, in vitro. Acta Pharm Hung, 2009, 79(2): 75-80.
[5].  Zádori ZS, Shujaa N, Brancati SB, et al. Both α2B- and α2C-adrenoceptor subtypes are involved in the mediation of centrally induced gastroprotection in mice. Eur J Pharmacol, 2011, 669(1-3): 115-120.

化学性质

Cas No. 55974-42-0 SDF
别名 ARC?239二盐酸盐
化学名 2-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-4,4-dimethylisoquinoline-1,3(2H,4H)-dione dihydrochloride
Canonical SMILES CC(C1=CC=CC=C1C(N2CCN3CCN(C4=CC=CC=C4OC)CC3)=O)(C2=O)C.Cl.Cl
分子式 C24H29N3O3.2HCl 分子量 480.43
溶解度 <48.04mg/ml in Water 储存条件 Store at RT
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1 mM 2.0815 mL 10.4073 mL 20.8147 mL
5 mM 0.4163 mL 2.0815 mL 4.1629 mL
10 mM 0.2081 mL 1.0407 mL 2.0815 mL
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