ABSTRACT
The design and synthesis of some hybrid-structures comprising the dopamine framework on one hand and an N-(1-substituted-cycloalkyl) moiety on the other have been elaborated. Selective members of the new series were biochemically assayed to determine their effects on the levels of dopamine and its metabolite norepinephrine in brains of Albino-rats. The brain MAO activity was also estimated. The results were compared with those displayed by apomorphine, metoclopramide and PCP.
Subject(s)
Dopamine Agents/chemistry , Phenethylamines/chemistry , Dopamine Agents/pharmacology , Drug Design , Molecular Structure , Phenethylamines/pharmacologyABSTRACT
The bilateral diamino analogs namely N,N'-dialkyl-N,N'-diaralkyl- and N,N,N',N'-tetraalkyl-2-(3,4-dimethoxyphenyl)-1,3-propanediamine s were synthesized. The biochemical determination of the brain levels of dopamine and norepinephrine as well as of brain monoamine oxidase (MAO) activity was performed.
Subject(s)
Diamines/chemical synthesis , Dopamine Agents/chemical synthesis , Animals , Apomorphine/pharmacology , Brain Chemistry/drug effects , Chemical Phenomena , Chemistry , Diamines/pharmacology , Dopamine/metabolism , Membranes/drug effects , Membranes/metabolism , Metoclopramide/pharmacology , Mitochondria/drug effects , Mitochondria/metabolism , Monoamine Oxidase/metabolism , Norepinephrine/metabolism , RatsABSTRACT
The synthesis of some N-methyl, N-alkyl derivatives of (+/-)alpha-phenyl-beta-(3,4-dimethoxy)- and (+/-)alpha-phenyl-beta-(3,4-dihydroxy)-phenethylamines was achieved. These compounds were shown to bear certain structural features of acetylcholine (ACh), as well as phencyclidine (PCP). The latter was reported to act as a specific probe for the nicotinic ACh receptor-ion channel molecule from Torpedo electric organ. Biochemical binding studies revealed that for the nicotinic ACh receptor, the 3,4-dimethoxy derivatives behaved as blockers for the binding interaction of [3H]ACh, whereas the 3,4-dihydroxy analogues stimulated such binding. On the other hand, all of the tested phenethylamines exhibited potent blockade towards [3H]PCP binding interactions. The results indicated that the tested compounds might be applied as potential probes for the ACh receptor-ion channel molecule.
