CPP-115 hydrochloride
CPP-115 hydrochloride is an orally active, selective GABA-AT inhibitor with a Ki value of 9.7 μM. CPP-115 hydrochloride blocks GABA degradation and increases GABA levels in the brain. CPP-115 hydrochloride does not bind to GABA transporters, does not displace GABA from GABAA/GABAB receptors, and does not act as an agonist/antagonist of GABAC receptors. CPP-115 hydrochloride reduces cocaine-induced dopamine release, blocks cocaine-induced conditioned place preference, and suppresses seizure activity in a rat model of infantile spasms. CPP-115 hydrochloride can be used in research related to infantile spasms and epilepsy.
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- CAS No.: 760947-97-5
- 화학식: C7H10ClF2NO2
- 분자량:213.61
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
CPP-115 hydrochloride potently and irreversibly inactivates GABA-AT with a kinact/KI of 52 mM·min-1, 187 times more efficiently than vigabatrin[1].
CPP-11 (6 mM) hydrochloride does not exhibit inhibitory or inactivating activity against alanine aminotransferase or aspartate aminotransferase at concentrations up to 6 mM[1].
CPP-115 (0-4.0 equiv; up to 120 h) hydrochloride time-dependently inactivates pig brain GABA-AT with a turnover number of 1.3 per active site, with greater inactivation observed at higher equivalents of the compound[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CPP-115 (1 mg/kg) hydrochloride reduces cocaine-induced dopamine release in the nucleus accumbens (NAcc) of rats to 250% of the basal level, and its potency is over 300 times higher than that of Vigabatrin[1].
CPP-115 (0.1-1 mg/kg) hydrochloride suppresses seizure episodes in the adrenocorticotropic hormone (ACTH)-resistant multi-hit infantile spasm rat model, with a potency 100-fold higher than that of Vigabatrin and better tolerability[1].
CPP-115 (20 mg/kg per day for 45 consecutive days) hydrochloride causes only 5%-30% loss of electroretinogram in rats after 45 days of administration, showing extremely low retinal toxicity compared to the effective dose of Vigabatrin[1].
CPP-115 (0.7-7 mg/kg/day; p.o.; daily; 28 days) hydrochloride is well tolerated in healthy Beagle dogs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:unspecified[1]
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Dosage:1 mg/kg
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Administration:administered with cocaine during training
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Result:Eliminated cocaine-induced conditioned place preference, with rats spending 7.8 minutes in the cocaine-paired chamber and 7.2 minutes in the unpaired chamber (comparable to saline/saline control levels).
Did not produce place preference alone.
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Animal Model:unspecified[1]
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Dosage:1 mg/kg
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Administration:administered to modulate cocaine-induced dopamine release
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Result:Reduced cocaine-induced nucleus accumbens dopamine level increase from 550% of basal levels to 250% of basal levels.
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Animal Model:unspecified[1]
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Dosage:0.5 mg/kg
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Administration:administered with cocaine
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Result:Prevented displacement of [11C]-raclopride in the nucleus accumbens, indicating insufficient dopamine release to displace the tracer.
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Animal Model:unspecified[1]
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Dosage:20 mg/kg/day
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Administration:daily; 45 days
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Result:Resulted in only 5-30% electroretinographic loss, a dose that is 20-40 times higher than the effective infantile spasms dose of 0.5-1 mg/kg/day.
Chemical Information
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CAS No. 760947-97-5
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분자량 213.61
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화학식 C7H10ClF2NO2
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SMILES
OC([C@H]1C/C([C@H](C1)N)=C(F)\F)=O.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Silverman RB. The 2011 E. B. Hershberg award for important discoveries in medicinally active substances: (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a GABA aminotransferase inactivator and new treatment for drug addiction and infantile spasms. J Med Chem. 2012 Jan 26;55(2):567-75. [Content Brief]
[2]. Lee H, et al. Mechanism of inactivation of γ-aminobutyric acid aminotransferase by (1S,3S)-3-amino-4-difluoromethylene-1-cyclopentanoic acid (CPP-115). Journal of the American Chemical Society. 2015 Feb 25;137(7):2628-40. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CPP-115 hydrochloride Related Classifications
HY-W1025152 Related Classifications
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