A-68930
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| Nazivi | |
|---|---|
| IUPAC naziv
(1R,3S)-1-(Aminometil)-3-fenil-3,4-dihidro-1H-izohromen-5,6-diol
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| Identifikacija | |
3D model (Jmol)
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| ChemSpider | |
| MeSH | A+68930 |
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| Svojstva | |
| C16H17NO3 | |
| Molarna masa | 271,32 g·mol−1 |
| log P | 1,175 |
| Kiselost (pKa) | 9,491 |
| Baznost (pKb) | 4,506 |
Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa). | |
 verifikuj (šta je   ?)
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| Reference infokutije | |
A-68930 je sintetičko jedinjenje koje deluje kao selektivni parcijalni agonist D1.[3][4] On je oralno aktivan i ima antidepresivno i anoreksično dejstvo na životinje, proizvodi budnost i tahikardiju,[5][6][7][8] ali bez stimulansnih efekata, umesto toga uzrokuje sedaciju.[9][10] 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.[11]
Reference
[уреди | уреди извор]- ^ 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.
- ^ 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.
- ^ 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. PMID 1977907. doi:10.1021/jm00173a005.
- ^ 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. PMID 1683288. doi:10.1016/0014-2999(91)90459-4.
- ^ 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. PMID 8100197. doi:10.1016/0014-2999(93)90823-Z.
- ^ 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.
- ^ 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.
- ^ 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. PMID 7813561. doi:10.1016/0014-2999(94)90033-7.
- ^ 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. PMID 10817605. doi:10.1097/00001756-200004270-00025.
- ^ 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.
- ^ 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. PMID 16318870. doi:10.1016/j.pbb.2005.09.017.
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