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A-77636

С Википедије, слободне енциклопедије
A-77636
Stereo, Kekulova skeletna formula jedinjenja A-77636
Nazivi
IUPAC naziv
(1R,3S)-3-(1-Adamantil)-1-(aminometil)-3,4-dihidro-1H-izohromen-5,6-diol[1]
Identifikacija
3D model (Jmol)
ChemSpider
  • Oc1ccc2c(c1O)C[C@H](O[C@H]2CN)C35CC4CC(C3)CC(C4)C5
Svojstva
C20H27NO3
Molarna masa 329,44 g·mol−1
Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa).
Зелена квачицаДа verifikuj (šta je Зелена квачицаДаRed КрстићНе ?)
Reference infokutije

A-77636 je sintetički lek koji deluje kao selektivni agonist D1 receptora.[4] On ispoljava nootropne, anestetičke, i antiparkinsonske efekte u životinjskim studijama,[5][6][7][8][9] ali njegova visoka potentnost i dugotrajno dejstvo uzrokuju umanjenje senzitivnosti D1 receptora i tahifilaksu.[10][11][12] Za razliku od drugih D1 punih agonista kao što je SKF-82,958, on ne proizvodi preferenciju mesta kod životinja.[13] A-77636 parcijalno zamenjuje kokain u životinjskim studijama, te se pretpostavlja da može da nađe primenu kao zamena za drogu u lečenju adikcije.[14] On je bolje poznat po primeni u studijama za ispitivanje uloge D1 receptora u mozgu.[15][16][17]

Reference

[уреди | уреди извор]
  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  уреди
  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. ^ Kebabian JW, Britton DR, DeNinno MP, Perner R, Smith L, Jenner P, Schoenleber R, Williams M (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. PMID 1362704. doi:10.1016/0014-2999(92)90556-J. 
  5. ^ Asin KE, Nikkel AL, Wirtshafter D (1994). . „Repeated D1 receptor agonist treatment blocks cocaine-induced locomotor activity and c-fos expression”. Brain Research. 637 (1-2): 342—4. PMID 7910104. doi:10.1016/0006-8993(94)91258-0. 
  6. ^ Ranaldi R, Beninger RJ (1994). . „The effects of systemic and intracerebral injections of D1 and D2 agonists on brain stimulation reward”. Brain Research. 651 (1-2): 283—92. PMID 7922577. doi:10.1016/0006-8993(94)90708-0. 
  7. ^ Grondin R, Bédard PJ, Britton DR, Shiosaki K (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. 
  8. ^ Cai JX, Arnsten AF (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. 
  9. ^ Cooper SJ, Al-Naser HA, Clifton PG (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. PMID 16478622. doi:10.1016/j.ejphar.2005.11.046. 
  10. ^ Lin CW, Bianchi BR, Miller TR, Stashko MA, Wang SS, Curzon P, Bednarz L, Asin KE, Britton DR (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. 
  11. ^ Saklayen SS, Mabrouk OS, Pehek EA (2004). . „Negative feedback regulation of nigrostriatal dopamine release: mediation by striatal D1 receptors”. The Journal of Pharmacology and Experimental Therapeutics. 311 (1): 342—8. PMID 15175419. doi:10.1124/jpet.104.067991. 
  12. ^ Ryman-Rasmussen JP, Griffith A, Oloff S, Vaidehi N, Brown JT, Goddard WA, Mailman RB (2007). . „Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors”. Neuropharmacology. 52 (2): 562—75. PMC 1855220 Слободан приступ. PMID 17067639. doi:10.1016/j.neuropharm.2006.08.028. 
  13. ^ Graham DL, Hoppenot R, Hendryx A, Self DW (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. PMID 16835769. doi:10.1007/s00213-006-0473-5. 
  14. ^ Chausmer AL, Katz JL (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. PMID 11862342. doi:10.1007/s002130100896. 
  15. ^ Acquas E, Wilson C, Fibiger HC (1997). . „Nonstriatal dopamine D1 receptors regulate striatal acetylcholine release in vivo”. The Journal of Pharmacology and Experimental Therapeutics. 281 (1): 360—8. PMID 9103518. 
  16. ^ Ruskin DN, Rawji SS, Walters JR (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. 
  17. ^ Bubser M, Fadel JR, Jackson LL, Meador-Woodruff JH, Jing D, Deutch AY (2005). . „Dopaminergic regulation of orexin neurons”. The European Journal of Neuroscience. 21 (11): 2993—3001. PMID 15978010. doi:10.1111/j.1460-9568.2005.04121.x. 


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