词条 | PD-128,907 |
释义 |
| Verifiedfields = changed | verifiedrevid = 451226356 | IUPAC_name = (4aR,10bR)-3,4a,4,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano-[4,3-b]-1,4-oxazin-9-ol | image = PD-128907_structure.png | width = 200 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 123594-64-9 | CAS_supplemental = 300576-59-4 (hydrochloride) | ATC_prefix = | ATC_suffix = | PubChem = 5311346 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 94015 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 23180492 | C=14 | H=19 | N=1 | O=3 | molecular_weight = 249.305 g/mol | smiles = c23cc(O)ccc3OCC1C2OCCN1CCC | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C14H19NO3/c1-2-5-15-9-17-7-12-11-6-10(16)3-4-14(11)18-8-13(12)15/h3-4,6,12-13,16H,2,5,7-9H2,1H3/t12-,13-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = ZFSOBPVEIKTNQS-CHWSQXEVSA-N }}PD-128,907 is a drug used in scientific research which acts as a potent and selective agonist for the dopamine D2 and D3 receptors.[1] It is used for studying the role of these receptors in the brain, in roles such as inhibitory autoreceptors that act to limit further dopamine release,[2] as well as release of other neurotransmitters.[3] In animal studies it has been shown to reduce toxicity from cocaine overdose.[4][5] See also
References1. ^DeWald HA, Heffner TG, Jaen JC, Lustgarten DM, McPhail AT, Meltzer LT, Pugsley TA, Wise LD. Synthesis and dopamine agonist properties of (+-)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano [4,3-b]-1,4-oxazin-9-ol and its enantiomers. Journal of Medicinal Chemistry. 1990 Jan;33(1):445-50. {{PMID|1967318}} {{Dopaminergics}}{{nervous-system-drug-stub}}2. ^Koeltzow TE, Xu M, Cooper DC, Hu XT, Tonegawa S, Wolf ME, White FJ. Alterations in dopamine release but not dopamine autoreceptor function in dopamine D3 receptor mutant mice. Journal of Neuroscience. 1998 Mar 15;18(6):2231-8. {{PMID|9482807}} 3. ^Chen G, Kittler JT, Moss SJ, Yan Z. Dopamine D3 receptors regulate GABAA receptor function through a phospho-dependent endocytosis mechanism in nucleus accumbens. Journal of Neuroscience. 2006 Mar 1;26(9):2513-21. {{PMID|16510729}} 4. ^Witkin JM, Dijkstra D, Levant B, Akunne HC, Zapata A, Peters S, Shannon HE, Gasior M. Protection against cocaine toxicity in mice by the dopamine D3/D2 agonist R-(+)-trans-3,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol [(+)-PD 128,907]. Journal of Pharmacology and Experimental Therapeutics. 2004 Mar;308(3):957-64. {{PMID|14711932}} 5. ^Witkin JM, Levant B, Zapata A, Kaminski R, Gasior M. The dopamine D3/D2 agonist (+)-PD-128,907 [(R-(+)-trans-3,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano[4,3-b]-1,4-oxazin-9-ol)] protects against acute and cocaine-kindled seizures in mice: further evidence for the involvement of D3 receptors. Journal of Pharmacology and Experimental Therapeutics. 2008 Sep;326(3):930-8. {{PMID|18566292}} 4 : Dopamine agonists|Chromenes|Phenols|Morpholines |
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