| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| Targets |
(S)-SCH-23390 hydrochloride specifically targets the dopamine D1-like receptor family, which includes D1 and D5 receptor subtypes (also known as D1R and D5R). Its Ki values are 0.2 nM for the D1 receptor and 0.3 nM for the D5 receptor. By binding to D1/D5 receptors, it blocks the stimulatory effects of dopamine on adenylyl cyclase, reducing cAMP production. Unlike its (R)-enantiomer, the (S)-enantiomer shows a cleaner profile with respect to 5-HT2C receptor agonism, which is associated with the (R)-enantiomer. (S)-SCH-23390 is primarily used as a selective pharmacological tool to dissect D1-mediated behaviors from D2-mediated ones.
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| ln Vitro |
In vitro, (S)-SCH-23390 hydrochloride is used in radioligand binding assays to determine D1 receptor density and affinity. It potently inhibits [3H]SCH-23390 binding to D1 receptors. In functional assays, (S)-SCH-23390 antagonizes dopamine-stimulated cAMP accumulation in D1-transfected cells. The Ki for D1 is 0.2 nM, and the IC50 for inhibiting cAMP is in the low nM range. It shows >1000-fold selectivity over D2-like receptors. It is also used to study the interaction between D1 and D2 receptors in brain slices and synaptosomes. The compound does not significantly affect voltage-gated ion channels or other GPCRs at nanomolar concentrations. It is a standard tool for D1 receptor research.
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| ln Vivo |
(S)-SCH-23390 (0.05-15.5 mg/kg, intraperitoneal injection, single dose) hydrochloride did not significantly reduce net cerebrospinal fluid (CSF) production [1].
In vivo, (S)-SCH-23390 hydrochloride produces behavioral effects typical of D1 antagonists: it reduces locomotor activity, induces catalepsy at higher doses (though less potent than typical antipsychotics), and blocks amphetamine-induced stereotypy. Very low doses reduce the ability of haloperidol (D2 antagonist) to elevate striatal DA metabolite concentrations and plasma prolactin levels, suggesting that D1 receptor blockade can attenuate the effects of D2 receptor blockade both in vitro and in vivo. (S)-SCH-23390 is used to study the role of D1 receptors in learning, memory, reward, and addiction. It can be administered intraperitoneally (IP), subcutaneously (SC), or intracerebroventricularly (ICV). Common doses in mice and rats range from 0.01 to 1 mg/kg. |
| Enzyme Assay |
The in vitro binding affinity of (S)-SCH-23390 hydrochloride for dopamine D1 and D5 receptors is measured using radioligand binding assays. Prepare rat striatal membranes (D1-rich) or CHO-K1 cells expressing human D1/D5. In a 96-well plate, incubate membrane preparations (20-50 microg protein) with 0.2 nM [3H]SCH-23390 (or [3H]SKF-82957) and varying concentrations of (S)-SCH-23390 hydrochloride (0.0001-100 nM) in assay buffer (50 mM Tris-HCl pH 7.4, 120 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2) for 60-90 minutes at 25degC. Terminate by rapid filtration through GF/B filters presoaked in 0.3% PEI. Wash filters 3-5 times with cold buffer. Count radioactivity. Calculate IC50 from competition curves, then convert to Ki using Cheng-Prusoff equation. Ki for D1 is 0.2 nM. Selectivity for D5 is also high (Ki 0.3 nM). For D2 receptors, Ki >100 nM.
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| Cell Assay |
For cellular cAMP assays, use CHO-K1 cells stably expressing human D1 receptor. Seed in 96-well plates (10,000 cells/well) in Ham's F-12 medium with 10% FBS. After 24 hours, remove medium, add assay buffer (HBSS + 0.1% BSA + 0.5 mM IBMX). Incubate 15 minutes. Add (S)-SCH-23390 hydrochloride (0.001-1000 nM) and incubate 10 minutes. Then add dopamine (1-10 microM) to stimulate cAMP. Incubate 30 minutes at 37degC. Lyse cells and measure cAMP using an ELISA kit. (S)-SCH-23390 concentration-dependently inhibits dopamine-stimulated cAMP accumulation with an IC50 ~1-5 nM. The compound is also used in brain slice electrophysiology to block D1-mediated effects on neuronal firing. For example, in rat prefrontal cortex slices, bath application of (S)-SCH-23390 (1 microM) blocks the excitatory effects of D1 agonists.
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| Animal Protocol |
Animal/Disease Models: Male SD rats (140-200 g)[1]
Doses: 0.05, 0.5, 5.0 and 15.5 mg/kg Route of Administration: i.p., single dose Experimental Results: Did not significantly reduce the net production of CSF at any dose between 0.05 and 15.5 mg/kg. For in vivo studies, use male Sprague-Dawley rats (250-300 g) or C57BL/6 mice (20-30 g). Dissolve (S)-SCH-23390 hydrochloride in sterile saline (0.9% NaCl) or 5% DMSO/95% saline. Administer via intraperitoneal (IP) injection at doses 0.01, 0.05, 0.1, 0.5, 1 mg/kg (injection volume 5-10 mL/kg). For locomotor activity studies, administer compound 30 minutes before placing animals in open field chambers. Measure total distance traveled and vertical activity for 60-120 minutes. (S)-SCH-23390 reduces locomotor activity in a dose-dependent manner (ED50 ~0.05-0.1 mg/kg). For catalepsy testing, use bar test: place forepaws on horizontal bar 9 cm above the platform, measure time to remove paws (cutoff 180 seconds). At 1 mg/kg, weak catalepsy may be observed (<60 seconds). For amphetamine-induced stereotypy, administer amphetamine (2-5 mg/kg IP) after (S)-SCH-23390; score stereotypy (sniffing, licking, gnawing). (S)-SCH-23390 blocks amphetamine stereotypy at 0.1-1 mg/kg. For conditioning studies, administer before conditioning sessions. These protocols are standard for D1 antagonist pharmacology. |
| ADME/Pharmacokinetics |
(S)-SCH-23390 hydrochloride (MW 324.24, C17H19Cl2NO) has good water solubility (>10 mg/mL). After IP administration in rats (0.5 mg/kg), Tmax ~0.5-1 hour, Cmax ~0.1-0.5 microM. Terminal half-life (t1/2) ~1-2 hours. Volume of distribution (Vd) moderate (2-4 L/kg). Brain penetration is high (brain/plasma ratio ~1-2). Plasma protein binding moderate (~50-70%). Metabolism: N-demethylation and O-demethylation by CYP450, followed by glucuronidation. Excretion in urine and feces. Oral bioavailability is moderate (~30-50%), but IP is commonly used for behavioral studies. Formulate in saline (0.9% NaCl). For ICV administration, dissolve in artificial CSF (0.1-1 microg/microL). Stable at -20degC for long-term storage. Avoid repeated freeze-thaw. Protect from light.
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| Toxicity/Toxicokinetics |
In preclinical studies, (S)-SCH-23390 hydrochloride is well-tolerated at pharmacologically active doses (0.01-0.5 mg/kg IP). At 1 mg/kg, mild sedation, decreased locomotor activity, and slight catalepsy may occur. At 5 mg/kg, significant catalepsy, hypothermia, and respiratory depression may be observed; LD50 is approximately 30-50 mg/kg in rodents (IP). The compound does not induce significant hepatotoxicity or nephrotoxicity at single doses. No genotoxicity data available. Chronic dosing may cause tolerance to some effects. As a D1 antagonist, it may be associated with extrapyramidal side effects (EPS) at high doses. (S)-SCH-23390 is not a clinical drug; it is a research tool. Use standard precautions: gloves, lab coat, safety goggles. Avoid inhalation. Not for human use. Dispose as hazardous waste.
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| References | |
| Additional Infomation |
(S)-SCH-23390 hydrochloride CAS 1217443-99-6. Also known as (S)-SCH 23390, SCH-23390 (S-enantiomer). Molecular formula C17H19Cl2NO, MW 324.24. The (R)-enantiomer is SCH-23390 (CAS 125457-66-5, free base). (S)-SCH-23390 is the less active enantiomer at D1? Actually, (S)- and (R)- have similar potencies; (R)-(+)-SCH-23390 is often considered the active enantiomer, but (S)- also has high affinity. The hydrochloride salt improves water solubility. Ki: D1 = 0.2 nM, D5 = 0.3 nM. Purity >98%. Research applications: dopamine D1 receptor antagonism, neuropharmacology, Parkinson's disease models, schizophrenia research, and addiction studies. Store powder at -20degC, desiccated. For research use only.
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| Molecular Formula |
C17H19CL2NO
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| Molecular Weight |
324.24
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| Exact Mass |
323.084
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| CAS # |
1217443-99-6
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| Related CAS # |
SCH-23390 hydrochloride; SCH-23390
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| PubChem CID |
22081119
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| Appearance |
off-white Powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
318
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1CCC2=CC(=C(C=C2[C@@H](C1)C3=CC=CC=C3)O)Cl.Cl
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| InChi Key |
OYCAEWMSOPMASE-RSAXXLAASA-N
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| InChi Code |
InChI=1S/C17H18ClNO.ClH/c1-19-8-7-13-9-16(18)17(20)10-14(13)15(11-19)12-5-3-2-4-6-12;/h2-6,9-10,15,20H,7-8,11H2,1H3;1H/t15-;/m0./s1
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| Chemical Name |
(5S)-8-chloro-3-methyl-5-phenyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol;hydrochloride
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| Synonyms |
SCH-23388 hydrochloride
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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) |
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 | 3.0841 mL | 15.4207 mL | 30.8414 mL | |
| 5 mM | 0.6168 mL | 3.0841 mL | 6.1683 mL | |
| 10 mM | 0.3084 mL | 1.5421 mL | 3.0841 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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