ABT-239

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 524114

CAS#: 460746-46-7

Description: ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia. ABT-239 is more active at the human H3 receptor than comparable agents such as thioperamide, ciproxifan, and cipralisant.


Price and Availability

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ABT-239, purity > 98%, is not in stock, may be available through custom synthesis. Minimum 1 gram order is requested. Current shipping out time is about 70 days after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 524114
Name: ABT-239
CAS#: 460746-46-7
Chemical Formula: C22H22N2O
Exact Mass: 330.17321
Molecular Weight: 330.42
Elemental Analysis: C, 79.97; H, 6.71; N, 8.48; O, 4.84


Synonym: ABT-239; ABT 239; ABT239;

IUPAC/Chemical Name: 4-(2-{2-[(2R)-2-Methylpyrrolidin-1-yl]ethyl}- benzofuran-5-yl)benzonitrile

InChi Key: KFHYZKCRXNRKRC-MRXNPFEDSA-N

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

SMILES Code: N#CC1=CC=C(C2=CC=C(OC(CCN3[C@H](C)CCC3)=C4)C4=C2)C=C1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Bhowmik M, Saini N, Vohora D. Histamine H3 receptor antagonism by ABT-239
attenuates kainic acid induced excitotoxicity in mice. Brain Res. 2014 Sep
18;1581:129-40. doi: 10.1016/j.brainres.2014.06.012. Epub 2014 Jun 18. PubMed
PMID: 24952295.

2: Kruk M, Miszkiel J, McCreary AC, Przegaliński E, Filip M, Biała G. Effects of
the histamine H₃ receptor antagonist ABT-239 on cognition and nicotine-induced
memory enhancement in mice. Pharmacol Rep. 2012;64(6):1316-25. PubMed PMID:
23406742.

3: Munari L, Provensi G, Passani MB, Blandina P. Selective brain region
activation by histamine H₃ receptor antagonist/inverse agonist ABT-239 enhances
acetylcholine and histamine release and increases c-Fos expression.
Neuropharmacology. 2013 Jul;70:131-40. doi: 10.1016/j.neuropharm.2013.01.021.
Epub 2013 Feb 1. PubMed PMID: 23380305.

4: Miszkiel J, Kruk M, McCreary AC, Przegaliński E, Biała G, Filip M. Effects of
the histamine H3 receptor antagonist ABT-239 on acute and repeated nicotine
locomotor responses in rats. Pharmacol Rep. 2011;63(6):1553-9. PubMed PMID:
22358104.

5: Varaschin RK, Akers KG, Rosenberg MJ, Hamilton DA, Savage DD. Effects of the
cognition-enhancing agent ABT-239 on fetal ethanol-induced deficits in dentate
gyrus synaptic plasticity. J Pharmacol Exp Ther. 2010 Jul;334(1):191-8. doi:
10.1124/jpet.109.165027. Epub 2010 Mar 22. PubMed PMID: 20308329; PubMed Central
PMCID: PMC2912053.

6: Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao
BB, Pan L, Wetter J, Marsh K, Bennani YL, Cowart MD, Sullivan JP, Hancock AA.
Pharmacological properties of ABT-239
[4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I.
Potent and selective histamine H3 receptor antagonist with drug-like properties.
J Pharmacol Exp Ther. 2005 Apr;313(1):165-75. Epub 2004 Dec 17. PubMed PMID:
15608078.

7: Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE,
Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner
RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan
JP, Cowart MD, Decker MW, Hancock AA. 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. 2005 Apr;313(1):176-90. Epub 2004 Dec 17. PubMed PMID:
15608077.