A-68930

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

 YesY (šta je ovo?)   (verifikuj)

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

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[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. PMID 20331846. doi:10.1186/1758-2946-2-3.  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. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  5. ↑ DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW (November 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. PMID 1977907. doi:10.1021/jm00173a005. 
  6. ↑ DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, Asin KE, Briggs C, Trugman JM, Ackerman M, Artman L, Bednarz L (June 1991). "A68930: a potent agonist selective for the dopamine D1 receptor". European Journal of Pharmacology 199 (2): 209–19. PMID 1683288. doi:10.1016/0014-2999(91)90459-4. 
  7. ↑ Trampus M, Ferri N, Adami M, Ongini E (April 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. PMID 8100197. doi:10.1016/0014-2999(93)90823-Z. 
  8. ↑ Christie MI, Smith GW (February 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 (April 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 (September 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. PMID 7813561. doi:10.1016/0014-2999(94)90033-7. 
  11. ↑ Salmi P, Ahlenius S (April 2000). "Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior". Neuroreport 11 (6): 1269–72. PMID 10817605. doi:10.1097/00001756-200004270-00025. 
  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. PMID 14960337. doi:10.1016/j.neuroscience.2003.11.016. 
  13. ↑ Nergårdh R, Oerther S, Fredholm BB (November 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. PMID 16318870. doi:10.1016/j.pbb.2005.09.017. 


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