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.
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- CAS No.: 360551-59-3
- Formule: C25H31N3O5
- Masse moléculaire:453.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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rat H3 receptor 9.2 (pKi) |
human H3 receptor 7.0 (pKi) |
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.
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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Masse moléculaire 453.53
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
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