A histamine H3 receptor antagonist
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ABT-239

Item No. 45575

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-[2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl]-5-benzof uranyl]-benzonitrile
CAS Number
460746-46-7
Molecular Formula
C22H22N2O
Formula Weight
330.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
N#CC1=CC=C(C2=CC=C3OC(CCN4CCC[C@H]4C)=CC3=C2)C=C1
InChi Code
InChI=1S/C22H22N2O/c1-16-3-2-11-24(16)12-10-21-14-20-13-19(8-9-22(20)25-21)18-6-4-17(15-23)5-7-18/h4-9,13-14,16H,2-3,10-12H2,1H3/t16-/m1/s1
InChi Key
KFHYZKCRXNRKRC-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $26

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    5 mg

    $98

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    10 mg

    $169

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    25 mg

    $358

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    Product Description

    ABT-239 is a histamine H3 receptor antagonist (Kis = 0.316 and 1.258 nM, respectively, for the human and rat receptors).1 In vivo, ABT-239 (0.1-1 mg/kg) inhibits the dipsogenic response induced by (R)-(–)-α-methylhistamine (Item No. 25601) in mice. It improves social memory in adult and aged rats and attenuates methamphetamine-induced hyperactivity in mice. ABT-239 (3 mg/kg) decreases escape latency in the Morris water maze in a rat model of chronic stress.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fox, G.B., Esbenshade, T.A., Pan, J.B., et al. Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J. Pharmacol. Exp. Ther. 313(1), 176-190 (2005).

    2. Trofimiuk, E., Wielgat, P., and Car, H. Selective H3 antagonist (ABT-239) differentially modifies cognitive function under the impact of restraint stress. Front. Syst. Neurosci. 14, 614810 (2021).