Name | Ampalex |
Synonyms | CX516 Ampalex BDP 12 BDP-12(Ampalex) AMPAKINE CX516 1-(6-Quinoxalinylcarbonyl)piperidine 1-(quinoxalin-6-ylcarbonyl)piperidine 1-(QUINOXALIN-6-YLCARBONYL)PIPERIDINE 6-(Piperidin-1-ylcarbonyl)quinoxaline Piperidin-1-yl-quinoxalin-6-ylmethanone piperidin-1-yl(quinoxalin-6-yl)methanone Methanone, 1-piperidinyl-6-quinoxalinyl- ABT-224,piperidine, 1-(6-quinoxalinylcarbonyl)- ABT-224,PIPERIDINE, 1-(6-QUINOXALINYLCARBONYL)- |
CAS | 154235-83-3 |
EINECS | 200-256-5 |
InChI | InChI=1/C14H15N3O/c18-14(17-8-2-1-3-9-17)11-4-5-12-13(10-11)16-7-6-15-12/h4-7,10H,1-3,8-9H2 |
Molecular Formula | C14H15N3O |
Molar Mass | 241.29 |
Density | 1.236±0.06 g/cm3(Predicted) |
Melting Point | 88-90°C |
Boling Point | 433.1±25.0 °C(Predicted) |
Flash Point | 215.756°C |
Solubility | DMSO : ≥ 41 mg/mL (169.92 mM) |
Vapor Presure | 0mmHg at 25°C |
Appearance | powder |
Color | white to light brown |
pKa | -0.14±0.30(Predicted) |
Storage Condition | 2-8°C |
Refractive Index | 1.64 |
In vivo study | The specific extradimensional deficits produced by sub-chronic or early postnatal postnatal phencyclidine treatment were significantly attenuated by CX516 (10, and 20 mg/kg, s.c.). Animal Model: Male Lister Hooded rats (56-63 postnatal day) Dosage: 5, 10, 20, and 40 mg/kg Administration: Subcutaneously Result: Two doses (10 and 20 mg/kg) were highly significant in improving the extradimensional shift deficit induced by either treatment regimes. Two doses (5 and 40 mg/kg) was ineffective at reversing the extradimensional impairment induced by the sub-chronic postnatal phencyclidine treatment regime. |
RTECS | TM2785170 |
Reference Show more | 1: Gibert-Rahola J, Villena-Rodriguez A. Glutamatergic drugs for schizophrenia treatment. Actas Esp Psiquiatr. 2014 Sep;42(5):234-41. Epub 2014 Sep 1. PubMed PMID: 25179095. 2: O'Neill MJ, Witkin JM. AMPA receptor potentiators: application for depression and Parkinson's disease. Curr Drug Targets. 2007 May;8(5):603-20. Review. PubMed PMID: 17504104. 3: Olsen CK, Kreilgaard M, Didriksen M. Positive modulation of glutamatergic receptors potentiates the suppressive effects of antipsychotics on conditioned avoidance responding in rats. Pharmacol Biochem Behav. 2006 Jun;84(2):259-65. Epub 2006 Jun 19. PubMed PMID: 16782180. 4: Visser PJ, Scheltens P, Verhey FR. Do MCI criteria in drug trials accurately identify subjects with predementia Alzheimer's disease? J Neurol Neurosurg Psychiatry. 2005 Oct;76(10):1348-54. PubMed PMID: 16170074; PubMed Central PMCID: PMC1739362. 5: Danysz W. CX-516 (Cortex Pharmaceuticals Inc). IDrugs. 1999 Aug;2(8):814-22. PubMed PMID: 16127658. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.144 ml | 20.722 ml | 41.444 ml |
5 mM | 0.829 ml | 4.144 ml | 8.289 ml |
10 mM | 0.414 ml | 2.072 ml | 4.144 ml |
5 mM | 0.083 ml | 0.414 ml | 0.829 ml |
preparation | low molecular weight polyethylene glycol (PEG,HO-(CH2CH2O)n-H) is widely used as an environment-friendly solvent and phase transfer catalyst due to its advantages of high thermal stability, difficult volatilization, non-flammability, low cost and biodegradability, and is widely used in organic synthesis. The "one-pot method" does not require the separation of intermediate products. This method greatly improves the utilization rate of atoms and is a very promising organic synthesis method today. In addition, iron nitrate can be used as an excellent oxidant and catalyst in organic synthesis, and has abundant sources, low price and little environmental pollution. Our laboratory reported earlier that Fe(NO 3 ) 3 · 9H 2 O/AcOH-PEG400 can be simple, convenient and efficient to complete the synthesis of alcohol ketones, and can be further condensed with o-phenylenediamine to obtain quinoxaline. The preparation reaction formula of ampales is as follows: fig. 1 the preparation reaction formula of ampales |
biological activity | Ampalex (CX-516, Ampakine CX 516, BDP-12, SPD 420) is a forward allosteric regulator of AMPA receptor. Ampalex has potential therapeutic effects in Alzheimer's disease, schizophrenia, and mild cognitive impairment (MCI). |
target | TargetValue AMPA receptor () |
Target | Value |
in vivo study | The specific extradimensional deficits produced by sub-chronic or early postnatal postnatal phencyclidine treatment were significantly attenuated by CX516 (10, and 20 mg/kg, s.c.). Animal Model: male Lister Hooded Rats (56-63 postnatal day) Dosage: 5, 10, 20, and 40 mg/kg Administration: Subcutaneously Result: two doses (10 and 20 mg/kg) were highly significant in improving the extradimensional shift deficit induced by either treatment regimes. Two doses (5 and 40 mg/kg) was ineffective at reversing the extradimensional impairment induced by the sub-chronic postnatal phencyclidine treatment regime. |
Animal Model: | Male Lister Hooded rats (56-63 postnatal day) |
Dosage: | 5, 10, 20, and 40 mg/kg |
Administration: | Subcutaneously |
Result: | Two doses (10 and 20 mg/kg) were highly significant in improving the extradimensional shift deficit induced by either treatment regimes. Two doses (5 and 40 mg/kg) was ineffective at reversing the extradimensional impairment induced by the sub-chronic postnatal phencyclidine treatment regime. |