2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. SCH 50911

SCH 50911 is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B Receptor) antagonist with an IC50 of 1.1 μM in rats. SCH 50911 blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder.

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SCH 50911

SCH 50911 Chemical Structure

CAS No. : 733717-87-8

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10 mM * 1 mL in Water
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Based on 1 publication(s) in Google Scholar

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SCH 50911 Related Antibodies

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Description

SCH 50911 is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B Receptor) antagonist with an IC50 of 1.1 μM in rats. SCH 50911 blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder[1][2][3][4].

IC50 & Target

GABA(B)

1.1 μM (IC50)

In Vitro

SCH 50911 (1.1-2.2 μM) potently inhibits GABA binding to GABA-B receptors in rat brain with an IC50 of 1.1 μM, and shows no binding affinity for most tested non-GABA-B receptors aside from weak activity in a nonspecific muscarinic binding assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SCH 50911 Related Antibodies
In Vivo

SCH 50911 (100-300 mg/kg; i.p.; single acute dose) produces a significant, dose-dependent proconvulsive effect in rats undergoing ethanol withdrawal syndrome, with the 300 mg/kg dose inducing tonic-clonic seizures in 44% of treated rats[2].
Sch 50911 suppresses multiple forms of absence seizures in lethargic (lh/lh) mutant mice[3].
Sch 50911 (systemic) crosses the blood-brain barrier and blocks Baclofen (HY-B0007)-induced central antitussive and respiratory depressant effects in Felis catus and Cavia porcellus[3].
SCH 50911 (25-100 mg/kg; i.p.; single dose; 30 minutes before test session) reduces operant alcohol self-administration in male sP rats, with statistically significant ~35% and ~65% reductions in alcohol lever-responses at 50 and 100 mg/kg, respectively, and marked interindividual response variability[4].
SCH 50911 (100 mg/kg; i.p.; single dose; 30 minutes before test session) produces a statistically significant ~70% reduction in operant sucrose self-administration in male sP rats, with marked interindividual response variability[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (male, 275-300g, ethanol-dependent via Majchrowicz method)[2]
Dosage: 100 mg/kg; 170 mg/kg; 300 mg/kg
Administration: i.p.; single acute dose
Result: Produced seizure scores significantly higher than saline-treated controls.
Induced repeated tonic-clonic seizures (score 6) in 4 out of 9 rats at 300 mg/kg.
Caused a significant, dose-dependent increase in seizure score.
Animal Model: Sardinian alcohol-preferring (sP) rats (male, 55 days old, 95th to 97th generations, trained to lever-respond for oral alcohol under fixed ratio 4 schedule)[4]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: i.p.; single dose; 30 minutes before 30-minute test session
Result: Produced a statistically significant ~35% reduction in alcohol lever-responses at 50 mg/kg.
Produced a statistically significant ~65% reduction in alcohol lever-responses at 100 mg/kg.
Produced a statistically significant reduction in the amount of self-administered alcohol at 100 mg/kg.
Induced virtually complete suppression of alcohol lever-responses in 1/16, 3/16, and 10/16 rats at 25, 50, and 100 mg/kg, respectively.
Produced a statistically significant ~45% reduction in alcohol lever-responses at 100 mg/kg (replication experiment).
Induced virtually complete suppression of alcohol lever-responses in 0/16, 5/16, and 8/16 rats at 25, 50, and 100 mg/kg, respectively.
Revealed four response variability subgroups in combined data (n=32 rats): 10/32 rats showed dose-related reduction with multiple doses; 6/32 rats showed reduction only at 100 mg/kg; 10/32 rats showed V-shaped response pattern; 6/32 rats showed no effect from any dose.
Animal Model: Sardinian alcohol-preferring (sP) rats (male, 55 days old, 95th to 97th generations, trained to lever-respond for sucrose solution under fixed ratio 4 schedule)[4]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: i.p.; single dose; 30 minutes before 30-minute test session
Result: Produced a statistically significant ~70% reduction in sucrose lever-responses at 100 mg/kg.
Produced a statistically significant reduction in the amount of self-administered sucrose solution at 100 mg/kg.
Induced virtually complete suppression of sucrose lever-responses in 0/16, 1/16, and 10/16 rats at 25, 50, and 100 mg/kg, respectively.
Revealed four response variability subgroups (n=16 rats): 6/16 rats showed dose-related reduction with multiple doses; 4/16 rats showed reduction only at 100 mg/kg; 4/16 rats showed V-shaped response pattern; 2/16 rats showed no effect from any dose.
Molecular Weight

173.21

Formula

C8H15NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C[C@H]1CNC(C)(C)CO1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 12.5 mg/mL (72.17 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.7733 mL 28.8667 mL 57.7334 mL
5 mM 1.1547 mL 5.7733 mL 11.5467 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
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The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 5.7733 mL 28.8667 mL 57.7334 mL 144.3335 mL
5 mM 1.1547 mL 5.7733 mL 11.5467 mL 28.8667 mL
10 mM 0.5773 mL 2.8867 mL 5.7733 mL 14.4333 mL
15 mM 0.3849 mL 1.9244 mL 3.8489 mL 9.6222 mL
20 mM 0.2887 mL 1.4433 mL 2.8867 mL 7.2167 mL
25 mM 0.2309 mL 1.1547 mL 2.3093 mL 5.7733 mL
30 mM 0.1924 mL 0.9622 mL 1.9244 mL 4.8111 mL
40 mM 0.1443 mL 0.7217 mL 1.4433 mL 3.6083 mL
50 mM 0.1155 mL 0.5773 mL 1.1547 mL 2.8867 mL
60 mM 0.0962 mL 0.4811 mL 0.9622 mL 2.4056 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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SCH 50911 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SCH 50911733717-87-8SCH50911SCH-50911GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorhistamine H1 receptorGABA-A receptordopamine D2 receptorhistamine H3 receptormuscarinic m1 receptorratSardinian alcohol-preferring ratsGABA-B receptorserotonin 5-HT2 receptordopamine D1 receptorInhibitorinhibitorinhibit

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