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ABT 239 tartrate
- Parent CAS: 460746-46-7
- Optical Purity: >98% e.e.
- Soluble in water and DMSO
- MF: C22H22N2O.C4H6O6
- MW: 480.51
Description
ABT 239 tartrate is a potent and selective histamine H3 receptor antagonist/inverse agonist used to investigate presynaptic histaminergic control of neurotransmitter release.
Histamine H3 receptors regulate histamine, acetylcholine, dopamine and other neurotransmitter systems in the CNS. ABT 239 is pharmacologically relevant for studies of cognition, wakefulness, attention and H3 receptor inverse agonism in preclinical models.
Key Features
- Potent histamine H3 receptor antagonist/inverse agonist
- Selective tool for CNS histaminergic signaling studies
- Modulates presynaptic neurotransmitter-release pathways
- Useful in behavioral and receptor pharmacology assays
Applications
- Histamine H3 receptor pharmacology
- Cognition and attention research
- Arousal and wakefulness pathway studies
- Preclinical CNS neurotransmission assays
More Information
| Parent CAS No. | 460746-46-7 |
|---|---|
| Chemical Name | 4-{2-[2-((R)-2-Methyl-pyrrolidin-1-yl)-ethyl]-benzofuran-5-yl}-benzonitrile tartrate |
| SMILES | C(C1OC2=CC=C(C3C=CC(C#N)=CC=3)C=C2C=1)CN1CCC[C@H]1C.C(O)(=O)[C@@H]([C@H](C(O)=O)O)O |&1:23,28,29,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C22H22N2O.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h4-9,13-14,16H,2-3,10-12H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t16-;1-,2-/m11/s1 |
| InChiKey | NISULOSDVFYWIH-NUFNRNBZSA-N |
| CID | 11202447 |
| Short Description | H3 antagonist |
References
- TA Esbenshade et al. 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. Ph. Exp. Ther. 2005, 313, 165.
- GB Fox et al. Pharmacological properties of ABT-239 : II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J. Ph. Exp. Ther. 2005, 313, 176–90.
- M Cowart et al. 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. J. Med. Chem. 2005, 48 (1), 38–55.
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