A-68930
A-68930は、ドーパミン受容体D1部分的作用薬として機能する有機合成物質である[2][3]。経口投与では動物に対し抗うつ薬と食欲抑制剤としての効果があり、覚醒状態と頻脈を生じる[4][5][6][7]。しかしながら、興奮剤としての効果は無く、むしろ鎮静剤として作用する[8][9]。A-68930とSKF-82958など他のD1作用薬の機能的相違点は、D5受容体に関連する影響の違いに起因するものと見られる[10]。
| A-68930 | |
|---|---|
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| 識別情報 | |
| CAS登録番号 | 130465-45-1  , 130465-39-3 (HCl) 
|
| PubChem | 122324 |
| ChemSpider | 109076
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| MeSH | A+68930 |
| ChEMBL | CHEMBL315468
|
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| |
| 特性 | |
| 化学式 | C16H17NO3 |
| モル質量 | 271.31 g mol−1 |
| 精密質量 | 271.120843415 g mol-1 |
| log POW | 1.175 |
| 酸解離定数 pKa | 9.491 |
| 塩基解離定数 pKb | 4.506 |
| 特記なき場合、データは常温 (25 °C)・常圧 (100 kPa) におけるものである。 | |
出典
編集- ^ CID 122324 - PubChem
- ^ 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. doi:10.1021/jm00173a005. PMID 1977907.
- ^ 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. doi:10.1016/0014-2999(91)90459-4. PMID 1683288.
- ^ 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. doi:10.1016/0014-2999(93)90823-Z. PMID 8100197.
- ^ 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.
- ^ 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.
- ^ 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. doi:10.1016/0014-2999(94)90033-7. PMID 7813561.
- ^ 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. doi:10.1097/00001756-200004270-00025. PMID 10817605.
- ^ 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.
- ^ 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. doi:10.1016/j.pbb.2005.09.017. PMID 16318870.