CDPPB
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(IUPAC) ime | |||
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3-ciano-N-(1,3-difenil-1H-pirazol-5-il)benzamid | |||
Klinički podaci | |||
Identifikatori | |||
CAS broj | 781652-57-1 | ||
ATC kod | nije dodeljen | ||
PubChem[1][2] | 11245456 | ||
Hemijski podaci | |||
Formula | C23H18N4O | ||
Mol. masa | 366,414 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
CDPPB je lek koji se koristi u naučnim istraživanjima. On deluje kao pozitivni alosterni modulator koji je selektivan za metabotropni glutamatni receptor mGluR5.[3][4][5] On ima antipsihotičke efekte u životinjskim modelima.[6] and mGluR5 Modulatori se istražuju kao potencijalni lekovi za tretman šizofrenije,[7] i drugih bolesti.[8][9]
Reference
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR (November 2004). „Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo”. Journal of Medicinal Chemistry 47 (24): 5825–8. DOI:10.1021/jm049400d. PMID 15537338.
- ↑ de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, Baldwin RM, Tamagnan GD, Conn PJ (June 2006). „Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes”. Journal of Medicinal Chemistry 49 (11): 3332–44. DOI:10.1021/jm051252j. PMID 16722652.
- ↑ Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, Conn PJ (May 2007). „Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses”. Molecular Pharmacology 71 (5): 1389–98. DOI:10.1124/mol.106.032425. PMID 17303702.
- ↑ Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL (April 2005). „A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models”. The Journal of Pharmacology and Experimental Therapeutics 313 (1): 199–206. DOI:10.1124/jpet.104.079244. PMID 15608073.
- ↑ Lindsley CW, Shipe WD, Wolkenberg SE, Theberge CR, Williams DL, Sur C, Kinney GG (2006). „Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia”. Current Topics in Medicinal Chemistry 6 (8): 771–85. DOI:10.2174/156802606777057599. PMID 16719816.
- ↑ Lecourtier L, Homayoun H, Tamagnan G, Moghaddam B (October 2007). „Positive allosteric modulation of metabotropic glutamate 5 (mGlu5) receptors reverses N-Methyl-D-aspartate antagonist-induced alteration of neuronal firing in prefrontal cortex”. Biological Psychiatry 62 (7): 739–46. DOI:10.1016/j.biopsych.2006.12.003. PMC 2910402. PMID 17511968.
- ↑ Gass JT, Olive MF (April 2009). „Positive allosteric modulation of mGluR5 receptors facilitates extinction of a cocaine contextual memory”. Biological Psychiatry 65 (8): 717–20. DOI:10.1016/j.biopsych.2008.11.001. PMC 2870714. PMID 19100966.
Spoljašnje veze
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Agonisti: Neselektivni: ACPD • DHPG • Kuiskualinska kiselina; mGlu1-selektivni: Ro01-6128 • Ro67-4853 • Ro67-7476 • VU-71; mGlu5-selektivni: ADX-47273 • CDPPB • CHPG • DFB • VU-1545 Antagonisti: Neselektivni: MCPG • NPS-2390; mGlu1-selektivni: BAY 36-7620 • CPCCOEt • LY-367,385 • LY-456,236; mGlu5-selektivni: DMeOB • Fenobam • LY-344,545 • MPEP • MTEP • SIB-1757 • SIB-1893 | |
Agonisti: Neselektivni: CBiPES • DCG-IV • Eglumegad • LY-379,268 • LY-404,039 • LY-487,379 • MGS-0028; mGlu2-selektivni: BINA • LY-566,332 Antagonisti: Neselektivni: APICA • EGLU • HYDIA • LY-307,452 • LY-341,495 • MCPG • MGS-0039; mGlu2-selektivni: PCCG-4; mGlu3-selektivni: CECXG; Negativni alosterni modulatori: RO4491533 | |
transporta
DHKA • PDC • WAY-213,613 | |