Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Zotepine is a potent and 2nd generation antipsychotic with antidepressive and anxiolytic effects and can be used for the treatment for schizophrenia. Functioning as an antagonist for the α1-adrenergic, 5-HT2A, 5-HT2C, Histamine H1, and Dopamine D2 receptors, with corresponding Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM, and 8 nM. In individuals with acute bipolar mania, zoloftine also demonstrated effectiveness as an antimanic medication.
ln Vitro |
Zotepine exhibits multiple antagonistic profiles and strong affinities to α1-adrenergic, α2-adrenergic, Dopamine D2, Histamine H1, Muscarinic, 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors, with Kds of 7.3, 180, 8, 3.3, 330, 280, 80, 2.6, 3.2 nM, respectively[1].
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ln Vivo |
Zotepine (1-3 mg/kg; a single i.p.) dose-dependently raises noradrenaline, dopamine, glutamate release, and GABA levels without changing 5-HT levels in the medial prefrontal cortex of rats[2].
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Animal Protocol |
Male Sprague-Dawley rats (250-300 g)
1, 3 mg/kg A single i.p. |
References |
Molecular Formula |
C18H18CLNOS
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Molecular Weight |
331.86
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Exact Mass |
331.08
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Elemental Analysis |
C, 65.15; H, 5.47; Cl, 10.68; N, 4.22; O, 4.82; S, 9.66
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CAS # |
26615-21-4
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Appearance |
Solid powder
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SMILES |
CN(C)CCOC1=CC2=CC=CC=C2SC3=C1C=C(C=C3)Cl
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InChi Key |
HDOZVRUNCMBHFH-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H18ClNOS/c1-20(2)9-10-21-16-11-13-5-3-4-6-17(13)22-18-8-7-14(19)12-15(16)18/h3-8,11-12H,9-10H2,1-2H3
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Chemical Name |
2-(3-chlorobenzo[b][1]benzothiepin-5-yl)oxy-N,N-dimethylethanamine
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Synonyms |
Zotepine
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~25 mg/mL (~75.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0133 mL | 15.0666 mL | 30.1332 mL | |
5 mM | 0.6027 mL | 3.0133 mL | 6.0266 mL | |
10 mM | 0.3013 mL | 1.5067 mL | 3.0133 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00418873 | Terminated | Drug: Zotepine Drug: Risperidone |
Schizophrenia | Astellas Pharma Inc | March 2007 | Phase 4 |
NCT00622011 | Terminated | Drug: Risperidone and Zotepine for delirium |
Delirium | Changhua Christian Hospital | January 2008 | Phase 4 |
Effects of glutamate receptor antagonists (MK-801 and DNQX) and a GABAA receptor agonist (muscimol) on zotepine-induced elevation of extracellular levels of (A) GABA and (B) glutamate in the mPFC. Br J Pharmacol . 2009 Jun;157(4):656-65. td> |
Effects of glutamate receptor antagonists (MK-801 and DNQX) and a GABAA receptor agonist (muscimol) on zotepine-induced elevation of extracellular levels of (A) noradrenaline, (B) dopamine and (C) 5-HT in the mPFC. Br J Pharmacol . 2009 Jun;157(4):656-65. td> |
Typical histograms showing the effects of (A) zotepine (3 mg·kg−1 zotepine, i.p.) and (B) haloperidol (1 mg·kg−1 haloperidol, i.p.) on neuronal firing frequencies in the VTA. Br J Pharmacol . 2009 Jun;157(4):656-65. td> |