1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. 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.

AL-38022A

AL-38022A Chemical Structure

CAS No. : 478132-11-5

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Description

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[1].

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.

In Vivo

AL-38022A (0.03-0.3 mg/kg; i.p.; s.c.; single dose) produces dose-dependent substitution for the DOM stimulus with ED50s of 0.05 mg/kg and 0.04 mg/kg in male Sprague-Dawley rats (250-300 g) and adult rhesus monkeys (5-8 kg), respectively[1].
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.

Animal Model: Male Sprague-Dawley rats were trained under a variable interval 15-s schedule of reinforcement to build a drug discrimination model[1].
Dosage: 0.032 mg/kg; 0.3 mg/kg
Administration: i.p.; 15 min pre-session
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.
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].
Dosage: 0.01 mg/kg; 0.1 mg/kg; 0.1 mg/kg plus MDL 100907 (0.00032-0.032 mg/kg)
Administration: s.c.; 1 min prior to testing
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.
Molecular Weight

231.29

Formula

C13H17N3O

CAS No.
SMILES

C[C@H](N)CN1C2=C(C=N1)C=CC3=C2CCCO3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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AL-38022A
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