A-68930

Из Википедије, слободне енциклопедије
A-68930
IUPAC ime
Identifikacija
CAS registarski broj 130465-45-1 ДаY, 130465-39-3 (HCl) ДаY
PubChem[1][2] 122324
ChemSpider[3] 109076 ДаY
MeSH A+68930
ChEMBL[4] CHEMBL315468 ДаY
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C16H17NO3
Molarna masa 271.31 g mol−1
Tačna masa 271,12 g mol-1
log P 1,175
pKa 9,491
Baznost (pKb) 4,506

 ДаY (šta je ovo?)   (verifikuj)

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

A-68930 je sintetičko jedinjenje koje deluje kao selektivni parcijalni agonist D1.[5][6] On je oralno aktivan i ima antidepresivno i anoreksično dejstvo na životinje, proizvodi budnost i tahikardiju,[7][8][9][10] ali bez stimulansnih efekata, umesto toga uzrokuje sedaciju.[11][12] Moguće je da je razlika u dejstvu između A-68930 i drugih D1 agonista kao što je SKF-82958 posledica različitih efekata na srodni D5 receptor.[13]

Reference[уреди]

  1. 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
  2. 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. 
  3. 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
  4. 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
  5. DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW (1990). „(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist”. Journal of Medicinal Chemistry. 33 (11): 2948—50. doi:10.1021/jm00173a005. PMID 1977907. 
  6. DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, Asin KE, Briggs C, Trugman JM, Ackerman M, Artman L, Bednarz L (1991). „A68930: a potent agonist selective for the dopamine D1 receptor”. European Journal of Pharmacology. 199 (2): 209—19. doi:10.1016/0014-2999(91)90459-4. PMID 1683288. 
  7. Trampus M, Ferri N, Adami M, Ongini E (1993). „The dopamine D1 receptor agonists, A68930 and SKF 38393, induce arousal and suppress REM sleep in the rat”. European Journal of Pharmacology. 235 (1): 83—7. doi:10.1016/0014-2999(93)90823-Z. PMID 8100197. 
  8. Christie MI, Smith GW (1994). „Cardiovascular and renal hemodynamic effects of A-68930 in the conscious dog: a comparison with fenoldopam”. The Journal of Pharmacology and Experimental Therapeutics. 268 (2): 565—70. PMID 7906731. 
  9. AI-Naser HA, Cooper SJ (1994). „A-68930, a novel, potent dopamine D1 receptor agonist: a microstructural analysis of its effects on feeding and other behaviour in the rat”. Behavioural Pharmacology. 5 (2): 210—218. PMID 11224270. 
  10. D'Aquila PS, Collu M, Pani L, Gessa GL, Serra G (1994). „Antidepressant-like effect of selective dopamine D1 receptor agonists in the behavioural despair animal model of depression”. European Journal of Pharmacology. 262 (1–2): 107—11. doi:10.1016/0014-2999(94)90033-7. PMID 7813561. 
  11. Salmi P, Ahlenius S (2000). „Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior”. Neuroreport. 11 (6): 1269—72. doi:10.1097/00001756-200004270-00025. PMID 10817605. 
  12. Isacson R, Kull B, Wahlestedt C, Salmi P (2004). „A 68930 and dihydrexidine inhibit locomotor activity and d-amphetamine-induced hyperactivity in rats: a role of inhibitory dopamine D(1/5) receptors in the prefrontal cortex?”. Neuroscience. 124 (1): 33—42. doi:10.1016/j.neuroscience.2003.11.016. PMID 14960337. 
  13. Nergårdh R, Oerther S, Fredholm BB (2005). „Differences between A 68930 and SKF 82958 could suggest synergistic roles of D1 and D5 receptors”. Pharmacology, Biochemistry, and Behavior. 82 (3): 495—505. doi:10.1016/j.pbb.2005.09.017. PMID 16318870. 
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