DR/5-HT7AR Ligand-1
DR/5-HT7AR Ligand-1 is a ligand with a Ki value of 1.24 nM against human D2R, 5.78 nM against human D3R, 0.67 nM against human 5-HT1AR, and 19.9 nM against human 5-HT7AR. DR/5-HT7AR Ligand-1 can be used for the research of schizophrenia.
For research use only. We do not sell to patients.
- Formula: C27H30F2N2O2
- Molecular Weight:452.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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D2 Receptor 1.24 nM (Ki) |
D3 Receptor 5.78 nM (Ki) |
5-HT1A Receptor 0.67 nM (Ki) |
5-HT7A Receptor 19.9 nM (Ki) |
DR/5-HT7AR Ligand-1 (compound 36) (0.1 nM-10 μM; 90 min) binds to human D2 (Ki = 1.24 nM), D3 (Ki = 5.78 nM), D4 (Ki = 39.4 nM), 5-HT1A (Ki = 0.67 nM), 5-HT2A (Ki = 144.2 nM), and 5-HT7A (Ki = 19.9 nM) receptors, with highest affinity for the 5-HT1A and D2 receptors[1].
DR/5-HT7AR Ligand-1 exhibits antagonist-like binding interactions at human D2 and 5-HT2A receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DR/5-HT7AR Ligand-1 (0.632-1.896 mg/kg; i.p.) does not induce catalepsy in rats even at a dose 3× its antipsychotic ED50, suggesting minimal extrapyramidal side effect liability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss-Webster (male, 5-6 weeks old, 21-34 g)[1]
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Dosage:0.632 mg/kg (ED50)
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Administration:i.p.
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Result:Produced a dose-dependent inhibition of apomorphine-induced climbing behavior.
Achieved an ED50 value of 0.632 mg/kg (1.39 μmol/kg).
Demonstrated an ED50 more than 8-fold lower than that of SYA16263 (ED50 = 3.88 mg/kg) and 2-fold lower than that of lurasidone (ED50 = 1.59 mg/kg).
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Animal Model:Sprague-Dawley (male, ~6 weeks old, 133-153 g)[1]
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Dosage:0.632 mg/kg (ED50); 1.896 mg/kg (3× ED50)
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Administration:i.p.
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Result:Showed no significant cataleptic response in either the bar or crossed-legs position tests compared with vehicle controls.
Enabled all animals to successfully right themselves during the righting reflex test, indicating no marked impairment.
Chemical Information
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Molecular Weight 452.54
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Formula C27H30F2N2O2
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SMILES
OC(C1=CC=C(F)C=C1)(CCCN2CCN(C3=C(OC)C=CC=C3)CC2)C4=CC=C(F)C=C4
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DR/5-HT7AR Ligand-1 Related Classifications
HY-187538 Related Classifications
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