| 词条 | A-77636 |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 477363088 | ImageFile = A-77636.svg | ImageFile_Ref = {{chemboximage|correct|??}} | ImageName = Stereo, Kekulé skeletal formula of A-77636 | IUPACName = (1R,3S)-3-(1-Adamantyl)-1-(aminomethyl)-3,4-dihydro-1H-isochromene-5,6-diol[1] | Section1 = {{Chembox Identifiers | CASNo = 778546-51-3 | CASNo_Ref = {{cascite|changed|??}} | CASNo1 = 145307-34-2 | CASNo1_Ref = {{cascite|correct|}} | CASNo1_Comment= (HCl) | PubChem = 6603703 | PubChem1 = 9951033 | PubChem1_Comment = (HCl) | SMILES = Oc1ccc2c(c1O)C[C@H](O[C@H]2CN)C35CC4CC(C3)CC(C4)C5 | InChI = 1/C20H27NO3/c21-10-17-14-1-2-16(22)19(23)15(14)6-18(24-17)20-7-11-3-12(8-20)5-13(4-11)9-20/h1-2,11-13,17-18,22-23H,3-10,21H2/t11?,12?,13?,17-,18-,20?/m0/s1 | InChIKey = QLJOSZATCBCBDR-DFKUFRTHBM | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C20H27NO3/c21-10-17-14-1-2-16(22)19(23)15(14)6-18(24-17)20-7-11-3-12(8-20)5-13(4-11)9-20/h1-2,11-13,17-18,22-23H,3-10,21H2/t11?,12?,13?,17-,18-,20?/m0/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = QLJOSZATCBCBDR-DFKUFRTHSA-N | ChemSpiderID = 5036017 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChEMBL = 313530 | ChEMBL_Ref = {{ebicite|changed|EBI}} }} | Section2 = {{Chembox Properties | C=20|H=27|N=1|O=3 }} }}A-77636 is a synthetic drug which acts as a selective D1 receptor full agonist.[2] It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies,[3][4][5][6][7] but its high potency and long duration of action causes D1 receptor downregulation and tachyphylaxis,[8][9][10] and unlike other D1 full agonists such as SKF-82,958, it does not produce place preference in animals.[11] A-77636 partially substituted for cocaine in animal studies, and has been suggested for use as a possible substitute drug in treating addiction,[12] but it is better known for its use in studying the role of D1 receptors in the brain.[13][14][15] References1. ^{{PubChem|6603703}} {{Stimulants}}{{Anorectics}}{{Nootropics}}{{Dopaminergics}}{{gastrointestinal-drug-stub}}{{nervous-system-drug-stub}}{{Organic-compound-stub}}2. ^{{cite journal |vauthors =Kebabian JW, Britton DR, DeNinno MP, Perner R, Smith L, Jenner P, Schoenleber R, Williams M |title=A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets |journal=European Journal of Pharmacology |volume=229 |issue=2-3 |pages=203–9 |date=December 1992 |pmid=1362704 |doi= 10.1016/0014-2999(92)90556-J|url=}} 3. ^{{cite journal |vauthors =Asin KE, Nikkel AL, Wirtshafter D |title=Repeated D1 receptor agonist treatment blocks cocaine-induced locomotor activity and c-fos expression |journal=Brain Research |volume=637 |issue=1-2 |pages=342–4 |date=February 1994 |pmid=7910104 |doi= 10.1016/0006-8993(94)91258-0|url=}} 4. ^{{cite journal |vauthors =Ranaldi R, Beninger RJ |title=The effects of systemic and intracerebral injections of D1 and D2 agonists on brain stimulation reward |journal=Brain Research |volume=651 |issue=1-2 |pages=283–92 |date=July 1994 |pmid=7922577 |doi= 10.1016/0006-8993(94)90708-0|url=}} 5. ^{{cite journal |vauthors =Grondin R, Bédard PJ, Britton DR, Shiosaki K |title=Potential therapeutic use of the selective dopamine D1 receptor agonist, A-86929: an acute study in parkinsonian levodopa-primed monkeys |journal=Neurology |volume=49 |issue=2 |pages=421–6 |date=August 1997 |pmid=9270571 |doi= 10.1212/wnl.49.2.421|url=}} 6. ^{{cite journal |vauthors =Cai JX, Arnsten AF |title=Dose-dependent effects of the dopamine D1 receptor agonists A77636 or SKF81297 on spatial working memory in aged monkeys |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=283 |issue=1 |pages=183–9 |date=October 1997 |pmid=9336323 |doi= |url=}} 7. ^{{cite journal |vauthors =Cooper SJ, Al-Naser HA, Clifton PG |title=The anorectic effect of the selective dopamine D1-receptor agonist A-77636 determined by meal pattern analysis in free-feeding rats |journal=European Journal of Pharmacology |volume=532 |issue=3 |pages=253–7 |date=February 2006 |pmid=16478622 |doi=10.1016/j.ejphar.2005.11.046 |url=}} 8. ^{{cite journal |vauthors =Lin CW, Bianchi BR, Miller TR, Stashko MA, Wang SS, Curzon P, Bednarz L, Asin KE, Britton DR |title=Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=276 |issue=3 |pages=1022–9 |date=March 1996 |pmid=8786531 |doi= |url=}} 9. ^{{cite journal |vauthors =Saklayen SS, Mabrouk OS, Pehek EA |title=Negative feedback regulation of nigrostriatal dopamine release: mediation by striatal D1 receptors |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=311 |issue=1 |pages=342–8 |date=October 2004 |pmid=15175419 |doi=10.1124/jpet.104.067991 |url=}} 10. ^{{cite journal |vauthors =Ryman-Rasmussen JP, Griffith A, Oloff S, Vaidehi N, Brown JT, Goddard WA, Mailman RB |title=Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors |journal=Neuropharmacology |volume=52 |issue=2 |pages=562–75 |date=February 2007 |pmid=17067639 |pmc=1855220 |doi=10.1016/j.neuropharm.2006.08.028 |url=}} 11. ^{{cite journal |vauthors =Graham DL, Hoppenot R, Hendryx A, Self DW |title=Differential ability of D1 and D2 dopamine receptor agonists to induce and modulate expression and reinstatement of cocaine place preference in rats |journal=Psychopharmacology |volume=191 |issue=3 |pages=719–30 |date=April 2007 |pmid=16835769 |doi=10.1007/s00213-006-0473-5 |url=}} 12. ^{{cite journal |vauthors =Chausmer AL, Katz JL |title=Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents |journal=Psychopharmacology |volume=159 |issue=2 |pages=145–53 |date=January 2002 |pmid=11862342 |doi=10.1007/s002130100896 }} 13. ^{{cite journal |vauthors =Acquas E, Wilson C, Fibiger HC |title=Nonstriatal dopamine D1 receptors regulate striatal acetylcholine release in vivo |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=281 |issue=1 |pages=360–8 |date=April 1997 |pmid=9103518 |doi= |url=}} 14. ^{{cite journal |vauthors =Ruskin DN, Rawji SS, Walters JR |title=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 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=286 |issue=1 |pages=272–81 |date=July 1998 |pmid=9655869 |doi= |url=}} 15. ^{{cite journal |vauthors =Bubser M, Fadel JR, Jackson LL, Meador-Woodruff JH, Jing D, Deutch AY |title=Dopaminergic regulation of orexin neurons |journal=The European Journal of Neuroscience |volume=21 |issue=11 |pages=2993–3001 |date=June 2005 |pmid=15978010 |doi=10.1111/j.1460-9568.2005.04121.x |url=}} 4 : Dopamine agonists|Adamantanes|Isochromenes|Catechols |
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