A-77636 Explained

A-77636 is a synthetic drug which acts as a selective D1 receptor full agonist.[1] It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies,[2] [3] [4] [5] [6] but its high potency and long duration of action causes D1 receptor downregulation and tachyphylaxis,[7] [8] [9] and unlike other D1 full agonists such as SKF-82,958, it does not produce place preference in animals.[10] A-77636 partially substituted for cocaine in animal studies, and has been suggested for use as a possible substitute drug in treating addiction,[11] but it is better known for its use in studying the role of D1 receptors in the brain.[12] [13] [14]

Notes and References

  1. Kebabian JW, Britton DR, DeNinno MP, Perner R, Smith L, Jenner P, Schoenleber R, Williams M . A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets . European Journal of Pharmacology . 229 . 2–3 . 203–9 . December 1992 . 1362704 . 10.1016/0014-2999(92)90556-J.
  2. Asin KE, Nikkel AL, Wirtshafter D . Repeated D1 receptor agonist treatment blocks cocaine-induced locomotor activity and c-fos expression . Brain Research . 637 . 1–2 . 342–4 . February 1994 . 7910104 . 10.1016/0006-8993(94)91258-0. 20197207 .
  3. Ranaldi R, Beninger RJ . The effects of systemic and intracerebral injections of D1 and D2 agonists on brain stimulation reward . Brain Research . 651 . 1–2 . 283–92 . July 1994 . 7922577 . 10.1016/0006-8993(94)90708-0. 18241791 .
  4. Grondin R, Bédard PJ, Britton DR, Shiosaki K . Potential therapeutic use of the selective dopamine D1 receptor agonist, A-86929: an acute study in parkinsonian levodopa-primed monkeys . Neurology . 49 . 2 . 421–6 . August 1997 . 9270571 . 10.1212/wnl.49.2.421. 541898 .
  5. Cai JX, Arnsten AF . Dose-dependent effects of the dopamine D1 receptor agonists A77636 or SKF81297 on spatial working memory in aged monkeys . The Journal of Pharmacology and Experimental Therapeutics . 283 . 1 . 183–9 . October 1997 . 9336323 .
  6. Cooper SJ, Al-Naser HA, Clifton PG . The anorectic effect of the selective dopamine D1-receptor agonist A-77636 determined by meal pattern analysis in free-feeding rats . European Journal of Pharmacology . 532 . 3 . 253–7 . February 2006 . 16478622 . 10.1016/j.ejphar.2005.11.046 .
  7. Lin CW, Bianchi BR, Miller TR, Stashko MA, Wang SS, Curzon P, Bednarz L, Asin KE, Britton DR . Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636 . The Journal of Pharmacology and Experimental Therapeutics . 276 . 3 . 1022–9 . March 1996 . 8786531 .
  8. Saklayen SS, Mabrouk OS, Pehek EA . Negative feedback regulation of nigrostriatal dopamine release: mediation by striatal D1 receptors . The Journal of Pharmacology and Experimental Therapeutics . 311 . 1 . 342–8 . October 2004 . 15175419 . 10.1124/jpet.104.067991 . 36903868 .
  9. Ryman-Rasmussen JP, Griffith A, Oloff S, Vaidehi N, Brown JT, Goddard WA, Mailman RB . Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors . Neuropharmacology . 52 . 2 . 562–75 . February 2007 . 17067639 . 1855220 . 10.1016/j.neuropharm.2006.08.028 .
  10. Graham DL, Hoppenot R, Hendryx A, Self DW . Differential ability of D1 and D2 dopamine receptor agonists to induce and modulate expression and reinstatement of cocaine place preference in rats . Psychopharmacology . 191 . 3 . 719–30 . April 2007 . 16835769 . 10.1007/s00213-006-0473-5 . 21192319 .
  11. Chausmer AL, Katz JL . Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents . Psychopharmacology . 159 . 2 . 145–53 . January 2002 . 11862342 . 10.1007/s002130100896 . 6788631 .
  12. Acquas E, Wilson C, Fibiger HC . Nonstriatal dopamine D1 receptors regulate striatal acetylcholine release in vivo . The Journal of Pharmacology and Experimental Therapeutics . 281 . 1 . 360–8 . April 1997 . 9103518 .
  13. Ruskin DN, Rawji SS, Walters JR . Effects of full D1 dopamine receptor agonists on firing rates in the globus pallidus and substantia nigra pars compacta in vivo: tests for D1 receptor selectivity and comparisons to the partial agonist SKF 38393 . The Journal of Pharmacology and Experimental Therapeutics . 286 . 1 . 272–81 . July 1998 . 9655869 .
  14. Bubser M, Fadel JR, Jackson LL, Meador-Woodruff JH, Jing D, Deutch AY . Dopaminergic regulation of orexin neurons . The European Journal of Neuroscience . 21 . 11 . 2993–3001 . June 2005 . 15978010 . 10.1111/j.1460-9568.2005.04121.x . 2027.42/71513 . 11527186 . free .

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