Idioma:

Cholinergic effects of molecular segments of apomorphine and dopaminergic effects of N,N-dialkylated dopamines

Ginos, James Z ; Cotzias, Geurge C ; Tolosa, Eduardo ; Tang, Lily C ; LoMonte, Anthony

Journal of medicinal chemistry, 1975-12, Vol.18 (12), p.1194-1200 [Periódico revisado por pares]

United States: American Chemical Society

Texto completo disponível

Citações Citado por

Enviar para

Título:
Cholinergic effects of molecular segments of apomorphine and dopaminergic effects of N,N-dialkylated dopamines
Autor: Ginos, James Z ; Cotzias, Geurge C ; Tolosa, Eduardo ; Tang, Lily C ; LoMonte, Anthony
Assuntos: Adenylyl Cyclases - metabolism ; Animals ; Apomorphine - chemical synthesis ; Apomorphine - pharmacology ; Caudate Nucleus - enzymology ; Caudate Nucleus - physiology ; Dopamine - analogs & derivatives ; Dopamine - chemical synthesis ; Dopamine - physiology ; Dopamine - toxicity ; Humans ; In Vitro Techniques ; Lethal Dose 50 ; Male ; Mice ; Motor Activity - drug effects ; Parasympathomimetics - toxicity ; Rats ; Stereotyped Behavior - drug effects ; Substantia Nigra - physiology
É parte de: Journal of medicinal chemistry, 1975-12, Vol.18 (12), p.1194-1200
Notas: ark:/67375/TPS-MWQ0N1LS-Q
istex:DE7FBE7ABB24D96DD855F43F29EE04F9D8D44045
Descrição: The hydrochlorides of molecular segments of apomorphine [2-(3',4'-dihydroxybenzyl)-1,2,3,4-tetrahydroisoquinoline, 2-(3'4'-dihydroxybenzyl)piperidine, and 1,2,3,4-tetrahydroisoquinoline with their respective N-methyl and N-n-propyl homologs] and N,N-dialkylated dopamine compounds were synthesized and studied for (1) LD50 in intact mice; (2) stereotypy in intact mice; (3) curving of the body in unilaterally caudectomized mice; (4) rotation in 6-hydroxydopamine-lesioned rats, and (5) activation of adenylate cyclase in homogenates of mouse caudate nuclei. Instead of dopaminergic effects 1-(3',4'-dihydroxybenzyl)-2-methyl-1,2,3,4-tetrahydroisoquinoline and 2-methyl-1,2,3,4-tetrahydroisoquinoline showed cholinergic ones. These effects were blocked in atropine-pretreated animals. Of the N,N-dialkylated dopamine compounds synthesized, the N-n-propyl-N-n-butyldopamine ranked in all tests as the strongest dopamine-receptor agonist and N-methyl-N-n-propyldopamine as the weakest. In contrast, N,N-dimethyldopamine and 1-(3,4-dihydroxyphenylethyl)piperidine showed no dopaminergic effects. The effectiveness of the dopaminergic agonists depended on the length of the N-alkyl substituents suggesting interactions with hydrophobic regions of the receptor site.
Editor: United States: American Chemical Society
Idioma: Inglês

Links

View this record in MEDLINE/PubMed

Voltar para lista de resultados

Resultado 1 Avançar Ir para próxima página

Realização: Logos de Redes Sociais:

Cholinergic effects of molecular segments of apomorphine and dopaminergic effects of N,N-dialkylated dopamines

Ginos, James Z ; Cotzias, Geurge C ; Tolosa, Eduardo ; Tang, Lily C ; LoMonte, Anthony

United States: American Chemical Society

Buscando em bases de dados remotas. Favor aguardar.