A-77636

Из Википедије, слободне енциклопедије
A-77636
IUPAC ime
Identifikacija
CAS registarski broj 778546-51-3 ДаY, 145307-34-2 (HCl) ДаY
PubChem[2][3] 6603703
9951033 (HCl)
ChemSpider[4] 5036017 ДаY
ChEMBL[5] CHEMBL313530 ДаY
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C20H27NO3
Molarna masa 329.43 g mol−1
Tačna masa 329,199093735 g mol-1

 ДаY (šta je ovo?)   (verifikuj)

Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala

A-77636 je sintetički lek koji deluje kao selektivni agonist D1 receptora.[6] On ispoljava nootropne, anestetičke, i antiparkinsonske efekte u životinjskim studijama,[7][8][9][10][11] ali njegova visoka potentnost i dugotrajno dejstvo uzrokuju umanjenje senzitivnosti D1 receptora i tahifilaksu.[12][13][14] Za razliku od drugih D1 punih agonista kao što je SKF-82,958, on ne proizvodi preferenciju mesta kod životinja.[15] A-77636 parcijalno zamenjuje kokain u životinjskim studijama, te se pretpostavlja da može da nađe primenu kao zamena za drogu u lečenju adikcije.[16] On je bolje poznat po primeni u studijama za ispitivanje uloge D1 receptora u mozgu.[17][18][19]

Reference[уреди]

  1. PubChem 6603703
  2. 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
  3. 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 
  4. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. doi:10.1186/1758-2946-2-3. PMID 20331846  edit
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. doi:10.1093/nar/gkr777. PMID 21948594  edit
  6. Kebabian JW, Britton DR, DeNinno MP, Perner R, Smith L, Jenner P, Schoenleber R, Williams M (December 1992). „A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets”. European Journal of Pharmacology 229 (2-3): 203–9. doi:10.1016/0014-2999(92)90556-J. PMID 1362704 
  7. Asin KE, Nikkel AL, Wirtshafter D (February 1994). „Repeated D1 receptor agonist treatment blocks cocaine-induced locomotor activity and c-fos expression”. Brain Research 637 (1-2): 342–4. doi:10.1016/0006-8993(94)91258-0. PMID 7910104 
  8. Ranaldi R, Beninger RJ (July 1994). „The effects of systemic and intracerebral injections of D1 and D2 agonists on brain stimulation reward”. Brain Research 651 (1-2): 283–92. doi:10.1016/0006-8993(94)90708-0. PMID 7922577 
  9. Grondin R, Bédard PJ, Britton DR, Shiosaki K (August 1997). „Potential therapeutic use of the selective dopamine D1 receptor agonist, A-86929: an acute study in parkinsonian levodopa-primed monkeys”. Neurology 49 (2): 421–6. PMID 9270571 
  10. Cai JX, Arnsten AF (October 1997). „Dose-dependent effects of the dopamine D1 receptor agonists A77636 or SKF81297 on spatial working memory in aged monkeys”. The Journal of Pharmacology and Experimental Therapeutics 283 (1): 183–9. PMID 9336323 
  11. Cooper SJ, Al-Naser HA, Clifton PG (February 2006). „The anorectic effect of the selective dopamine D1-receptor agonist A-77636 determined by meal pattern analysis in free-feeding rats”. European Journal of Pharmacology 532 (3): 253–7. doi:10.1016/j.ejphar.2005.11.046. PMID 16478622 
  12. Lin CW, Bianchi BR, Miller TR, Stashko MA, Wang SS, Curzon P, Bednarz L, Asin KE, Britton DR (March 1996). „Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636”. The Journal of Pharmacology and Experimental Therapeutics 276 (3): 1022–9. PMID 8786531 
  13. Saklayen SS, Mabrouk OS, Pehek EA (October 2004). „Negative feedback regulation of nigrostriatal dopamine release: mediation by striatal D1 receptors”. The Journal of Pharmacology and Experimental Therapeutics 311 (1): 342–8. doi:10.1124/jpet.104.067991. PMID 15175419 
  14. Ryman-Rasmussen JP, Griffith A, Oloff S, Vaidehi N, Brown JT, Goddard WA, Mailman RB (February 2007). „Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors”. Neuropharmacology 52 (2): 562–75. doi:10.1016/j.neuropharm.2006.08.028. PMC 1855220. PMID 17067639 
  15. Graham DL, Hoppenot R, Hendryx A, Self DW (April 2007). „Differential ability of D1 and D2 dopamine receptor agonists to induce and modulate expression and reinstatement of cocaine place preference in rats”. Psychopharmacology 191 (3): 719–30. doi:10.1007/s00213-006-0473-5. PMID 16835769 
  16. Chausmer AL, Katz JL (January 2002). „Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents”. Psychopharmacology 159 (2): 145–53. doi:10.1007/s002130100896. PMID 11862342 
  17. Acquas E, Wilson C, Fibiger HC (April 1997). „Nonstriatal dopamine D1 receptors regulate striatal acetylcholine release in vivo”. The Journal of Pharmacology and Experimental Therapeutics 281 (1): 360–8. PMID 9103518 
  18. Ruskin DN, Rawji SS, Walters JR (July 1998). „Effects of full D1 dopamine receptor agonists on firing rates in the globus pallidus and substantia nigra pars compacta in vivo: tests for D1 receptor selectivity and comparisons to the partial agonist SKF 38393”. The Journal of Pharmacology and Experimental Therapeutics 286 (1): 272–81. PMID 9655869 
  19. Bubser M, Fadel JR, Jackson LL, Meador-Woodruff JH, Jing D, Deutch AY (June 2005). „Dopaminergic regulation of orexin neurons”. The European Journal of Neuroscience 21 (11): 2993–3001. doi:10.1111/j.1460-9568.2005.04121.x. PMID 15978010 


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