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ARC 239 dihydrochloride

α2B adrenoceptor antagonist CAS# 55974-42-0

ARC 239 dihydrochloride

Catalog No. BCC6851----Order now to get a substantial discount!

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Chemical structure

ARC 239 dihydrochloride

3D structure

Chemical Properties of ARC 239 dihydrochloride

Cas No. 55974-42-0 SDF Download SDF
PubChem ID 10345075 Appearance Powder
Formula C24H31Cl2N3O3 M.Wt 480.43
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water
Chemical Name 2-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-4,4-dimethylisoquinoline-1,3-dione;dihydrochloride
SMILES CC1(C2=CC=CC=C2C(=O)N(C1=O)CCN3CCN(CC3)C4=CC=CC=C4OC)C.Cl.Cl
Standard InChIKey SAJKHRHHDGSJEZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H29N3O3.2ClH/c1-24(2)19-9-5-4-8-18(19)22(28)27(23(24)29)17-14-25-12-15-26(16-13-25)20-10-6-7-11-21(20)30-3;;/h4-11H,12-17H2,1-3H3;2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ARC 239 dihydrochloride

DescriptionSelective α2B adrenoceptor antagonist (pKD values are 8.8, 6.7 and 6.4 at α2B, α2A, and α2D receptors respectively). Also available as part of the α2-Adrenoceptor.

ARC 239 dihydrochloride Dilution Calculator

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ARC 239 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of ARC 239 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0815 mL 10.4073 mL 20.8147 mL 41.6294 mL 52.0367 mL
5 mM 0.4163 mL 2.0815 mL 4.1629 mL 8.3259 mL 10.4073 mL
10 mM 0.2081 mL 1.0407 mL 2.0815 mL 4.1629 mL 5.2037 mL
50 mM 0.0416 mL 0.2081 mL 0.4163 mL 0.8326 mL 1.0407 mL
100 mM 0.0208 mL 0.1041 mL 0.2081 mL 0.4163 mL 0.5204 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ARC 239 dihydrochloride

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.

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References on ARC 239 dihydrochloride

Characterization of sensory neurotransmission and its inhibition via alpha 2B-adrenoceptors and via non-alpha 2-receptors in rabbit iris.[Pubmed:7685502]

Naunyn Schmiedebergs Arch Pharmacol. 1993 Apr;347(4):394-401.

To find out whether, and which type of, adrenoceptors mediate prejunctional inhibition of sensory neurotransmitter release from trigeminal fibres, the modulation of twitch response to electrical field stimulation on rabbit isolated iris was investigated. Evoked iris sphincter contractions consisted of a minor fast cholinergic and a large slow component. The latter was unaffected by atropine and guanethidine, hence nonadrenergic noncholinergic in nature (NANC), but nearly completely abolished by capsaicin pretreatment and by the neurokinin receptor antagonist spantide. The response was probably not mediated by NK2 receptors as SR 48,968, an NK2 selective nonpeptide antagonist, failed to reduce the response to the release of the endogenous neurokinin(s) (and exogenous substance P), but in part due to NK1 receptor activation as shown by a reduction of response by CP 96,345, an NK1 selective non-peptide antagonist, and in part perhaps mediated by NK3 receptors. A small neurokinin receptor antagonist- and capsaicin-insensitive NANC contraction is probably not mediated by CGRP receptors. The alpha 2-adrenoceptor agonist oxymetazoline inhibited the evoked NANC response (22 nmol/l, IC20; about 40%, maximum inhibition) without affecting the cholinergic response (up to 1 mumol/l) or the postjunctional iris sensitivity to exogenous substance P. The inhibition was antagonized by rauwolscine (apparent -log KB 8.04) and by the relatively alpha 2B-adrenoceptor selective antagonist ARC-239 (-log KB 8.51). The alpha 2- and imidazoline receptor agonist aganodine inhibited the evoked NANC response (0.25 mumol/l, IC20; about 30%, maximum inhibition) without affecting the postjunctional substance P responses. Rauwolscine 0.3 mumol/l failed to antagonize this effect. It is concluded that the release of sensory neurotransmitter(s) from trigeminal fibres in the rabbit eye may be inhibited by alpha 2B-adrenoceptors and by a non-alpha 2-receptor, perhaps an imidazoline receptor.

Alpha-2A and alpha-2B adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype.[Pubmed:2835476]

J Pharmacol Exp Ther. 1988 May;245(2):600-7.

The affinities of 34 adrenergic antagonists for alpha-2 adrenergic receptors were determined from homogenate radioligand binding studies using [3H]yohimbine and [3H]rauwolscine. It has been suggested that alpha-2 adrenergic receptors can be subdivided into alpha-2A and alpha-2B subtypes. Oxymetazoline is selective for alpha-2A receptors, whereas prazosin is alpha-2B selective. Five different tissues were used, each of which has only one of the two subtypes: human platelet (alpha-2A), HT29 cell line (alpha-2A), human cerebral cortex (alpha-2A), neonatal rat lung (alpha-2B), and NG108-15 cell line (alpha-2B). The drug affinities were highly correlated when alpha-2A tissues were compared with alpha-2A tissues (r = 0.97 to 0.98) or when the two alpha-2B tissues were compared (r = 0.99). By contrast, comparison of an alpha-2A tissue with an alpha-2B tissue resulted in poor correlations (r = 0.77 to -0.87). Three new subtype selective drugs were identified among these drugs on the basis of at least a 10-fold greater affinity for one subtype. All three were selective for the alpha-2B subtype: ARC-239 (100-fold selective), chlorpromazine (18-fold selective), and 7-hydroxychlorpromazine (17-fold selective). These studies, by demonstrating distinct pharmacological profiles for the two alpha-2 adrenergic receptor subtypes in several different tissues, further support the existence and definition of these subtypes. The identification of a cell line for each subtype should be useful in the further study of alpha-2 adrenergic receptor subtypes.

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