Octoclothepin dimaleate
Based on 1 publication(s) in Google Scholar
Octoclothepin (Clorotepine) dimaleate is a D2 dopamine receptor antagonist and 5-HT2 serotonin receptor antagonist , with Ki values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D2, 5-HT2A, and 5-HT2C receptors, respectively. Octoclothepin dimaleate also binds to adrenergic receptors, with Ki values of 0.66 nM, 0.56 nM, and 0.77 nM for α1a, α1b, and α1d, respectively. Octoclothepin dimaleate can be used in schizophrenia research.
For research use only. We do not sell to patients.
- CAS No.: 41932-42-7
- Formula: C27H29ClN2O8S
- Molecular Weight:577.05
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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
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Octoclothepin dimaleate
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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D2 Receptor 0.67 nM (Ki) |
5-HT2A Receptor 0.57 nM (Ki) |
5-HT2C Receptor 0.19 nM (Ki) |
α1A-adrenergic receptor 0.66 nM (Ki) |
α1B-adrenergic receptor 0.56 nM (Ki) |
α1D-adrenergic receptor 0.77 nM (Ki) |
Octoclothepin (Compound 8) dimaleate binds with subnanomolar to nanomolar affinity to bovine α1a-, hamster α1b-, rat α1d-adrenoceptors, human D2, human 5-HT2A, and human 5-HT2C receptors, , with Ki values of 0.66 nM, 0.56 nM, 0.77 nM, 0.67 nM, 0.57 nM, and 0.19 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 41932-42-7
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Molecular Weight 577.05
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Formula C27H29ClN2O8S
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SMILES
CN1CCN(C2CC3=CC=CC=C3SC4=CC=C(Cl)C=C24)CC1.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
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Synonyms
Clorotepine dimaleate
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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.
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
A drug repurposing screen reveals dopamine signaling as a candidate therapeutic pathway for PIGA-CDG. [Abstract]2026 Apr 18:2026.04.17.719256. PMID: 42039650
Purity & Documentation
References
[1]. Kristensen JL, et al. Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. J Med Chem. 2010 Oct 14;53(19):7021-34. [Content Brief]
[2]. Helia CSc O, et al. Reduction of octoclothepine-N-oxide by rat liver microsomes. Eur. J. Drug Metab. Pharmacokinet. 1981 Apr;6:155-158. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Octoclothepin dimaleate Related Classifications
HY-106587B Related Classifications
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- Octoclothepin dimaleate
- 41932-42-7
- Clorotepine dimaleate
- Dopamine Receptor
- 5-HT Receptor
- Adrenergic Receptor
- serotonin 5-HT2C receptors
- α1-adrenoceptor subtypes
- dopamine D2 receptors
- rat α1d-adrenoceptors
- serotonin 5-HT2A receptors
- bovine α1a-adrenoceptors
- human H1 receptors
- human D2 receptors
- histamine H1 receptors
- hamster α1b-adrenoceptors
- Inhibitor
- inhibitor
- inhibit