Chemistry:A-77636
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(1R,3S)-3-(Adamantan-1-yl)-1-(aminomethyl)-1H-2-benzopyran-5,6-diol | |
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| C20H27NO3 | |
| Molar mass | 329.440 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
 verify (what is   ?)
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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]
References
- ↑ "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. doi:10.1016/0014-2999(92)90556-J. PMID 1362704.
- ↑ "Repeated D1 receptor agonist treatment blocks cocaine-induced locomotor activity and c-fos expression". Brain Research 637 (1–2): 342–4. February 1994. doi:10.1016/0006-8993(94)91258-0. PMID 7910104.
- ↑ "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. doi:10.1016/0006-8993(94)90708-0. PMID 7922577.
- ↑ "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. doi:10.1212/wnl.49.2.421. PMID 9270571.
- ↑ "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. PMID 9336323.
- ↑ "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. doi:10.1016/j.ejphar.2005.11.046. PMID 16478622.
- ↑ "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. PMID 8786531.
- ↑ "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. doi:10.1124/jpet.104.067991. PMID 15175419.
- ↑ "Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors". Neuropharmacology 52 (2): 562–75. February 2007. doi:10.1016/j.neuropharm.2006.08.028. PMID 17067639.
- ↑ "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. doi:10.1007/s00213-006-0473-5. PMID 16835769.
- ↑ "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. doi:10.1007/s002130100896. PMID 11862342. https://zenodo.org/record/1232629.
- ↑ "Nonstriatal dopamine D1 receptors regulate striatal acetylcholine release in vivo". The Journal of Pharmacology and Experimental Therapeutics 281 (1): 360–8. April 1997. PMID 9103518.
- ↑ "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. PMID 9655869.
- ↑ "Dopaminergic regulation of orexin neurons". The European Journal of Neuroscience 21 (11): 2993–3001. June 2005. doi:10.1111/j.1460-9568.2005.04121.x. PMID 15978010. https://deepblue.lib.umich.edu/bitstream/2027.42/71513/1/j.1460-9568.2005.04121.x.pdf.
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