AL-38022A
AL-38022A is a potent and selective 5-HT2 receptor agonist (Ki ≤2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. AL-38022A potently stimulates functional responses via 5-HT2 receptor subtypes including [Ca2+]i mobilization and tissue contractions with apparently similar potencies and intrinsic activities. AL-38022A fully generalizes to the (±)-1-(2,5-dimethoxy 4-methylphenyl)-2-aminopropane hydrochloride (DOM) stimulus in drug discrimination paradigms. AL-38022A can be used for the glaucoma research.
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- CAS. Nr.: 478132-11-5
- Formel: C13H17N3O
- Molecular Weight:231.29
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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Human 5-HT2A Receptor 2.2 nM (Ki) |
human 5-HT2B Receptor 2.0 nM (Ki) |
Human 5-HT2C Receptor 0.51 nM (Ki) |
Human 5-HT2A Receptor 1.68 nM (EC50) |
human 5-HT2B Receptor 3.98 nM (EC50) |
Human 5-HT2C Receptor 0.3 nM (EC50) |
Rat 5-HT2A 0.13 nM (Ki) |
Rat 5-HT2A 22.5 nM (EC50) |
AL-38022A exhibits Kis of 0.13 nM, 2.2 nM, 2.0 nM and 0.51 nM at rat 5-HT2A/C, human 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively[1].
AL-38022A exhibits EC50s of 22.5 nM, 1.9 nM, 15.7 nM, 1.68 nM, 3.98 nM and 0.3 nM at rat 5-HT2A, 5-HT2B, 5-HT2C, human 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively[1].
AL-38022A shows very low affinity (>1 µM) for other 5-HT receptors with the exception of 5-HT1A where it shows modest affinity (Ki = 294 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AL-38022A (0.03-0.3 mg/kg; s.c.; single dose) induces response rate-decreasing effects that were dose-dependently reversed by MDL 100907 (HY-14940) (0.00032-0.032 mg/kg) in adult rhesus monkeys (5-8 kg) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats were trained under a variable interval 15-s schedule of reinforcement to build a drug discrimination model[1].
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Dosage:0.032 mg/kg; 0.3 mg/kg
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Administration:i.p.; 15 min pre-session
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Result:Produced a maximum of 99% DOM-appropriate responding (at 0.3 mg/kg).
Did not produce response rates substantially different from those observed following administration of DOM or saline at doses that engendered ≥80% DOM-appropriate responding.
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Animal Model:Two males and two females adult rhesus monkeys were trained under a stimulus-shock termination schedule to build a drug discrimination model[1].
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Dosage:0.01 mg/kg; 0.1 mg/kg; 0.1 mg/kg plus MDL 100907 (0.00032-0.032 mg/kg)
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Administration:s.c.; 1 min prior to testing
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Result:Occasioned responding on the DOM-associated lever up to a maximum of 100% at a dose of 0.1 mg/kg.
Induced response rate-decreasing effects that were dose-dependently reversed by MDL 100907.
Chemical Information
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CAS. Nr. 478132-11-5
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Molecular Weight 231.29
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Formel C13H17N3O
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SMILES
C[C@H](N)CN1C2=C(C=N1)C=CC3=C2CCCO3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AL-38022A Related Classifications
HY-182472 Related Classifications
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