A-68930 Explained

A-68930 is a synthetic compound that acts as a selective dopamine receptor D₁ agonist.^{[1] [2]} It is orally active and has antidepressant and anorectic effects in animals, producing wakefulness and tachycardia,^{[3] [4] [5] [6]} but without stimulant effects, instead producing sedation.^{[7] [8]} The difference in effects between A-68930 and other D₁ agonists such as SKF-82958 may be due to their differing effects on the related D₅ receptor.^[9]

Notes and References

1. DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW . (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 . November 1990 . 1977907 . 10.1021/jm00173a005.
2. DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, Asin KE, Briggs C, Trugman JM, Ackerman M, Artman L, Bednarz L . A68930: a potent agonist selective for the dopamine D1 receptor . European Journal of Pharmacology . 199 . 2 . 209–19 . June 1991 . 1683288 . 10.1016/0014-2999(91)90459-4.
3. Trampus M, Ferri N, Adami M, Ongini E . 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 . April 1993 . 8100197 . 10.1016/0014-2999(93)90823-Z.
4. Christie MI, Smith GW . 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 . February 1994 . 7906731 .
5. AI-Naser HA, Cooper SJ . 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 . April 1994 . 11224270 . 10.1097/00008877-199404000-00013.
6. D'Aquila PS, Collu M, Pani L, Gessa GL, Serra G . 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 . September 1994 . 7813561 . 10.1016/0014-2999(94)90033-7.
7. Salmi P, Ahlenius S . Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior . NeuroReport . 11 . 6 . 1269–72 . April 2000 . 10817605 . 10.1097/00001756-200004270-00025. 35263421 .
8. Isacson R, Kull B, Wahlestedt C, Salmi P . 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 . 2004 . 14960337 . 10.1016/j.neuroscience.2003.11.016 . 19913930 .
9. Nergårdh R, Oerther S, Fredholm BB . Differences between A 68930 and SKF 82958 could suggest synergistic roles of D1 and D5 receptors . Pharmacology Biochemistry and Behavior . 82 . 3 . 495–505 . November 2005 . 16318870 . 10.1016/j.pbb.2005.09.017 . 23281483 .