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.
For research use only. We do not sell to patients.
- CAS No.: 478132-11-5
- Formula: C13H17N3O
- Molecular Weight:231.29
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
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) |
In Vitro
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. Further protocols information, click here.
In Vivo
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 No. 478132-11-5
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Molecular Weight 231.29
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Formula C13H17N3O
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SMILES
C[C@H](N)CN1C2=C(C=N1)C=CC3=C2CCCO3
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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.
Protocols
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AL-38022A Related Classifications
HY-182472 Related Classifications
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