PMID- 7120289 OWN - NLM STAT- MEDLINE DCOM- 19821202 LR - 20190709 IS - 0022-2623 (Print) IS - 0022-2623 (Linking) VI - 25 IP - 8 DP - 1982 Aug TI - Brain levels and metabolism of the dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene after administration of various prodrugs. PG - 993-6 AB - The synthesis of four prodrug diesters (diacetyl, diisobutyryl, dipivaloyl, and dibenzoyl) of the potent dopaminergic agonist 2-amino-6,7-dihydroxytetrahydronaphthalene (6,7-ADTN) is described. The effects of prodrug structure on the levels of 6,7-ADTN in the rat corpus striatum and cerebellum, as well as the levels of the metabolite, 6-hydroxy-7-methoxy-2-aminotetralin, in the corpus striatum, have been determined after intraperitoneal administration. In addition, the striatal levels of 6,7-ADTN after administration of the dibenzoyl analogue via intraperitoneal, subcutaneous, and oral routes have been measured. These prodrugs produce a significant improvement in the penetration and accumulation of 6,7-ADTN in the brain. FAU - Horn, A S AU - Horn AS FAU - Griever-Kazemier, H AU - Griever-Kazemier H FAU - Dijkstra, D AU - Dijkstra D LA - eng PT - Journal Article PL - United States TA - J Med Chem JT - Journal of medicinal chemistry JID - 9716531 RN - 0 (Naphthalenes) RN - 0 (Tetrahydronaphthalenes) RN - 53463-78-8 (ADTN) SB - IM MH - Animals MH - Brain/*metabolism MH - Cerebellum/metabolism MH - Chemical Phenomena MH - Chemistry MH - Corpus Striatum/metabolism MH - Drug Stability MH - Female MH - Naphthalenes/*administration & dosage/*chemical synthesis MH - Rats MH - Rats, Inbred Strains MH - Tetrahydronaphthalenes/*administration & dosage/*chemical synthesis/metabolism MH - Time Factors EDAT- 1982/08/01 00:00 MHDA- 1982/08/01 00:01 CRDT- 1982/08/01 00:00 PHST- 1982/08/01 00:00 [pubmed] PHST- 1982/08/01 00:01 [medline] PHST- 1982/08/01 00:00 [entrez] AID - 10.1021/jm00350a022 [doi] PST - ppublish SO - J Med Chem. 1982 Aug;25(8):993-6. doi: 10.1021/jm00350a022.