| Size | Price | Stock | Qty |
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| 1mg |
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| 1g | |||
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| Targets |
α-2C adrenergic receptor. ORM-10921 is a novel and potent selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. α-2C adrenergic receptors are G protein-coupled receptors that mediate the effects of norepinephrine and epinephrine in the central nervous system. They are involved in the regulation of neurotransmitter release, particularly dopamine and norepinephrine, and play a role in mood, cognition, and behavior. By antagonizing α-2C receptors, ORM-10921 increases extracellular dopamine levels in the prefrontal cortex. This mechanism is thought to underlie its antidepressant and antipsychotic-like effects. ORM-10921 has shown antipsychotic and antidepressant activity in animal studies and is being investigated for the treatment of schizophrenia.
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| ln Vitro |
ORM-10921 is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. The compound displays potent antidepressant and antipsychotic-like effects. In pharmacodynamic microdialysis studies, ORM-10921 was found to increase extracellular dopamine levels in the prefrontal cortex under baseline conditions. The compound's activity has been characterized in receptor binding assays measuring α-2C receptor affinity and selectivity over other adrenergic receptor subtypes. ORM-10921 has shown antipsychotic and antidepressant activity in animal studies. The compound is being investigated for the potential treatment of schizophrenia.
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| ln Vivo |
ORM-10921 has been studied in vivo in animal models of psychiatric disorders. The compound has shown antipsychotic and antidepressant activity in animal studies. In pharmacodynamic microdialysis studies, ORM-10921 was found to increase extracellular dopamine levels in the prefrontal cortex under baseline conditions. The compound is being investigated for the potential treatment of schizophrenia. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical studies. ORM-10921 is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
α-2C adrenergic receptor binding assays are performed using membranes prepared from cells expressing recombinant α-2C receptors or from brain tissue. Radioligand binding studies use [³H]-rauwolscine or [³H]-RX821002 as labeled ligands. Membrane preparations are incubated with varying concentrations of ORM-10921 and a fixed concentration of radioligand in binding buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl₂, 1 mM EDTA) for 60-120 minutes at room temperature. Non-specific binding is determined using excess unlabeled rauwolscine or yohimbine. Bound radioactivity is measured by scintillation counting after filtration through GF/B filters. IC50 and Ki values are calculated by non-linear regression. The Ki for ORM-10921 is 1.4 nM.
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| Cell Assay |
Cellular α-2C receptor antagonism is evaluated in cell lines expressing recombinant α-2C receptors (e.g., HEK-293 cells). Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with ORM-10921 at various concentrations. Functional assays measure receptor-mediated inhibition of cAMP accumulation (Gi-coupled receptor) in response to agonist (e.g., UK-14304) stimulation. The compound's antagonist activity is assessed by its ability to reverse agonist-induced inhibition of cAMP. Cell viability is assessed using MTT or LDH assays. Each experiment includes known α-2 adrenergic antagonists (e.g., yohimbine, rauwolscine) as positive controls and vehicle controls.
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| Animal Protocol |
In vivo efficacy of ORM-10921 is evaluated in animal models of schizophrenia and depression. The compound is administered orally or intraperitoneally at doses determined by preclinical studies. Behavioral assessments include tests of antipsychotic-like activity (e.g., prepulse inhibition, amphetamine-induced hyperactivity) and antidepressant-like activity (e.g., forced swim test, tail suspension). Extracellular dopamine levels in the prefrontal cortex are measured by microdialysis. Sample sizes typically range from 8-12 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 285.39. Formula: C18H23NO2. CAS No.: 610782-82-6. Chemical Name: 2H-Benzofuro[2,3-a]quinolizine, 1,3,4,6,7,12b-hexahydro-1-(methoxymethyl)-1-methyl-, (1S,12bS)-. Synonyms: ORM-10921 free base. Appearance: Solid. Purity: Typically >98%. Solubility: Soluble in DMSO. Storage: Typically at -20°C. ORM-10921 is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for ORM-10921. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As an α-2C adrenergic receptor antagonist, potential adverse effects may include cardiovascular effects (e.g., hypertension, tachycardia) and central nervous system effects. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
ORM-12741 has been used in trials investigating the basic science and treatment of Alzheimer's disease.
ORM-10921 is also known as ORM-10921 free base. Its chemical name is 2H-Benzofuro[2,3-a]quinolizine, 1,3,4,6,7,12b-hexahydro-1-(methoxymethyl)-1-methyl-, (1S,12bS)-. ORM-10921 is a novel and potent selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. The compound displays potent antidepressant and antipsychotic-like effects and has shown antipsychotic and antidepressant activity in animal studies. ORM-10921 increases extracellular dopamine levels in the prefrontal cortex and is being investigated for the treatment of schizophrenia. No clinical trials have been reported for this compound. ORM-10921 is for research use only. |
| Molecular Formula |
C18H23NO2
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|---|---|
| Molecular Weight |
285.3807
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| Exact Mass |
285.172
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| CAS # |
610782-82-6
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| Related CAS # |
1308264-47-2 (HCl);610782-82-6;1308264-48-3 (hydrate);
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| PubChem CID |
71301276
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| Appearance |
Light yellow to yellow solid
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
384.0±32.0 °C at 760 mmHg
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| Flash Point |
186.1±25.1 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
3.76
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
387
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O1C2C=CC=CC=2C2CCN3CCC[C@](C)(COC)[C@H]3C1=2
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| InChi Key |
OCUKPFWNSAAHRP-QZTJIDSGSA-N
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| InChi Code |
InChI=1S/C18H23NO2/c1-18(12-20-2)9-5-10-19-11-8-14-13-6-3-4-7-15(13)21-16(14)17(18)19/h3-4,6-7,17H,5,8-12H2,1-2H3/t17-,18-/m1/s1
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| Chemical Name |
(1S,12bS)-1-(methoxymethyl)-1-methyl-2,3,4,6,7,12b-hexahydro-[1]benzofuro[2,3-a]quinolizine
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5041 mL | 17.5205 mL | 35.0410 mL | |
| 5 mM | 0.7008 mL | 3.5041 mL | 7.0082 mL | |
| 10 mM | 0.3504 mL | 1.7520 mL | 3.5041 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.
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