A-77636

A-77636
Stereo, Kekulova skeletna formula jedinjenja A-77636
IUPAC ime
Identifikacija
CAS registarski broj 778546-51-3 DaY, 145307-34-2 (HCl) DaY
PubChem[2][3] 6603703, 
9951033 (HCl)
ChemSpider[4] 5036017 DaY
ChEMBL[5] CHEMBL313530 DaY
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C20H27NO3
Molarna masa 329.43 g mol−1

 DaY (šta je ovo?)   (verifikuj)

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

Infobox references

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

[uredi | uredi kod]
  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 stuđ 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 analjsis 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.