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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).
ДаY verifikuj (šta je ДаYНеН ?)
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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