An α2B-adrenergic receptor antagonist
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ARC 239 (hydrochloride)

Item No. 36218

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-4,4-dimethyl-1,3(2H,4H)-isoquinolinedione, dihydrochloride
CAS Number
55974-42-0
Molecular Formula
C24H29N3O3 • 2HCl
Formula Weight
480.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Water: soluble
SMILES
O=C1C2=C(C(C)(C)C(N1CCN3CCN(CC3)C4=CC=CC=C4OC)=O)C=CC=C2.Cl.Cl
InChi Code
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
InChi Key
SAJKHRHHDGSJEZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $32

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    1 mg

    $57

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    Product Description

    ARC 239 is an antagonist of α2B-adrenergic receptors (α2B-ARs; Ki = 87.1 nM).1,2,3 It is selective for α2B-ARs over α2A-ARs (Ki = 3,548 nM) but also inhibits α2C-ARs (Ki = 112.2 nM) and the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 63.1 nM).2,3 ARC 239 also binds to α1A-, α1B-, and α1D-adrenergic receptors (Kds = 0.45, 7.08, and 1.82 nM, respectively) but only induces the release of intracellular calcium in CHO cells expressing the α1B-adrenergic receptors with an EC50 value of 100 µM.4 It has commonly been used to determine the selectivity of α2-adrenergic receptor agonists and antagonists.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gavin, K.T., Colgan, M.-P., Moore, D., et al. α2C-adrenoceptors mediate contractile responses to noradrenaline in the human saphenous vein. Naunyn Schmiedebergs Arch. Pharmacol. 355(3), 406-411 (1997).

    2. Uhlén, S., Muceniece, R., Rangel, N., et al. Comparison of the binding activities of some drugs on α2A, α2B and α2C-adrenoceptors and non-adrenergic imidazoline sites in the guinea pig. Pharmacol. Toxicol. 76(6), 353-364 (1995).

    3. Meana, J.J., Callado, L.F., Pazos, A., et al. The subtype-selective α2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Eur. J. Pharmacol. 312(3), 385-388 (1996).

    4. Proudman, R.G.W., Pupo, A.S., and Baker, J.G. The affinity and selectivity of α-adrenoceptor antagonists, antidepressants, and antipsychotics for the human α1A, α1B, and α1D-adrenoceptors. Pharmacol. Res. Perspect. 8(4), e00602 (2020).

    5. Lee, H.G., Choi, J.I., Kim, Y.O., et al. The role of alpha-2 adrenoceptor subtype in the antiallodynic effect of intraplantar dexmedetomidine in a rat spinal nerve ligation model. Neurosci. Lett. 557(Pt B), 118-122 (2013).

    6. Millan, M.J. Evidence that an α2A-adrenoceptor subtype mediates antinociception in mice. Eur. J. Pharmacol. 215(2-3), 355-356 (1992).