L-DOPA cyclohexyl ester is a novel stable and potent competitive antagonist against L-DOPA, as compared to L-DOPA methyl ester.
We explore stable potent competitive antagonists against L-DOPA. In anesthetized rats, DOPA cyclohexyl ester (DOPA CHE) (30-100 ng) microinjected in depressor sites of the nucleus tractus solitarii dose-dependently shifted the dose-response-curve for L-DOPA (18-300 ng) to the right, with DOPA CHE (100 ng)-induced slight reduction of the maximum response. DOPA methyl ester (DOPA ME) at 100 ng also produced competitive antagonism. Antagonistic activity of DOPA CHE (100 ng) was similar to that of DOPA ME (300 ng). DOPA CHE is suitable for the purpose of screening.
Misu
Y
Y
Department of Pharmacology, Yokohama City University School of Medicine, Yokohama, Japan.
Goshima
Y
Y
Miyamae
T
T
Furukawa
N
N
Sugiyama
Y
Y
Okumura
Y
Y
Shimizu
M
M
Ohshima
E
E
Suzuki
F
F
D000818:Animals; D000978:Antiparkinson Agents / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D007980:Levodopa / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D008297:Male; D008845:Microinjections; D051381:Rats; D017208:Rats, Wistar; D017552:Solitary Nucleus
D000978:Antiparkinson Agents; C110321:levodopa cyclohexyl ester; D007980:Levodopa; C035420:levodopa methyl ester