A-68930

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A-68930
Stereo, Kekulé skeletal formula of A-68930
IUPAC ime
Identifikacija
CAS registarski broj 130465-45-1DaY,130465-39-3(HCl)DaY
PubChem[1][2] 122324
ChemSpider[3] 109076DaY
MeSH A+68930
ChEMBL[4] CHEMBL315468DaY
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

DaY(šta je ovo?) (verifikuj)

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

Infobox references

A-68930je sintetičko jedinjenje koje deluje kao selektivniparcijalni agonistD1.[5][6]On je oralno aktivan i imaantidepresivnoianoreksičnodejstvo na životinje, proizvodi budnost itahikardiju,[7][8][9][10]ali bezstimulansnihefekata, umesto toga uzrokujesedaciju.[11][12]Moguće je da je razlika u dejstvu između A-68930 i drugih D1agonista kao što jeSKF-82958posledica različitih efekata na srodniD5receptor.[13]

Reference

[uredi|uredi kod]
  1. Li Q, Cheng T, Wang Y, Bryant SH (2010).„PubChem as a public resource for drug discovery.”.Drug Discov Today15(23-24): 1052-7.DOI:10.1016/j.drudis.2010.10.003.PMID20970519.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 Chemistry4:217-241.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 Cheminform2(1): 3.DOI:10.1186/1758-2946-2-3.PMID20331846.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 Res40(Database issue): D1100-7.DOI:10.1093/nar/gkr777.PMID21948594.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 Chemistry33(11): 2948–50.DOI:10.1021/jm00173a005.PMID1977907.
  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 Pharmacology199(2): 209–19.DOI:10.1016/0014-2999(91)90459-4.PMID1683288.
  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 Pharmacology235(1): 83–7.DOI:10.1016/0014-2999(93)90823-Z.PMID8100197.
  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 Therapeutics268(2): 565–70.PMID7906731.
  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 Pharmacology5(2): 210–218.PMID11224270.
  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 Pharmacology262(1–2): 107–11.DOI:10.1016/0014-2999(94)90033-7.PMID7813561.
  11. Salmi P, Ahlenius S (April 2000). „Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior”.Neuroreport11(6): 1269–72.DOI:10.1097/00001756-200004270-00025.PMID10817605.
  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?”.Neuroscience124(1): 33–42.DOI:10.1016/j.neuroscience.2003.11.016.PMID14960337.
  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 Behavior82(3): 495–505.DOI:10.1016/j.pbb.2005.09.017.PMID16318870.