A-317920
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade.
For research use only. We do not sell to patients.
- CAS No.: 360551-59-3
- Formula: C25H31N3O5
- Molecular Weight:453.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histamine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
rat H3 receptor 9.2 (pKi) |
human H3 receptor 7.0 (pKi) |
In Vitro
A-317920 is a potent antagonist at rat H3R in reversing R-α-methylhistamine [(R)-α-MeHA] inhibition of Forskolin-stimulated cAMP formation (pKb value of 9.1) but a weak antagonist at human H3R in cyclase (pKb value of 6.3) and calcium mobilization (pKb value of 7.3) assays in cells co-expressing Galphaqi5-protein[1].
A-317920 potently antagonizes native H3Rs by blocking histamine inhibition of potassium-evoked [3H]histamine release from rat brain cortical synaptosomes (pKb value of 9.3) and (R)-α-MeHA reversal of electric field-stimulated guinea pig ileum contractions (pA2 value of 8.3)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male spontaneously hypertensive rat (SHR) pups (postnatal day 20–24) were trained to avoid a mild footshock[1]
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Dosage:3 mg/kg,10 mg/kg
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Administration:s.c; 30 min prior to training; for a total of five trials
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Result:Significantly improved in the avoidance test when compared with saline controls.
Chemical Information
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CAS No. 360551-59-3
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Molecular Weight 453.53
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Formula C25H31N3O5
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SMILES
O=C(N[C@@H](C(N1CCN(CC1)CCCOC2=CC=C(C=C2)C(C3CC3)=O)=O)C)C4=CC=CO4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Timothy A Esbenshade, et al. Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96. [Content Brief]
[2]. G B Fox, et al. Identification of novel H3 receptor (H3R) antagonists with cognition enhancing properties in rats. Inflamm Res. 2003 Apr:52 Suppl 1:S31-2. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-317920 Related Classifications
HY-122171 Related Classifications
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