ABSTRACT
(+/-)-1-Amino-6,7,8,8a-tetrahydroacenaphthene was synthesized and evaluated as a novel drug acting on the dopaminergic system. It was shown that the new compound displays activity as MAO inhibitor.
Subject(s)
Acenaphthenes/chemical synthesis , Cerebral Cortex/enzymology , Liver/enzymology , Monoamine Oxidase Inhibitors/chemical synthesis , Acenaphthenes/pharmacology , Animals , Cerebral Cortex/drug effects , Dopamine/physiology , Liver/drug effects , Male , Monoamine Oxidase Inhibitors/pharmacology , Rats , Rats, Sprague-Dawley , Spectrophotometry, Infrared , StereoisomerismABSTRACT
Compound 2 considered as a rigid non-hydroxylated 2-amino tetralin was synthesized and biologically evaluated. Central administration of compound 2 (50 microg or 100 microg/10 microl) induced a reduction in urinary sodium and potassium excretion at 3 and 6 h of urine collection. We speculate that compound 2 may be acting as a dopamine receptor antagonist.
Subject(s)
Amines/pharmacology , Dopamine Antagonists/pharmacology , Dopamine D2 Receptor Antagonists , Heterocyclic Compounds/pharmacology , Phenalenes , Polycyclic Compounds/pharmacology , Receptors, Dopamine D1/antagonists & inhibitors , Amines/chemical synthesis , Amines/chemistry , Animals , Diuresis/drug effects , Dopamine Antagonists/chemical synthesis , Dopamine Antagonists/chemistry , Heterocyclic Compounds/chemical synthesis , Heterocyclic Compounds/chemistry , Male , Molecular Structure , Natriuresis/drug effects , Polycyclic Compounds/chemical synthesis , Polycyclic Compounds/chemistry , Potassium/urine , Rats , Rats, Sprague-Dawley , Sodium/urineABSTRACT
Amino substitution of rigid forms of dopamine 4,5-dihydroxy-2-aminoindan and 5,6-dihydroxy-2-aminoindan with aralkyl functionalities were carried out to investigate the role of such structural modifications upon cardiac inotropic-chronotropic activity. Compounds synthesized demonstrated a modest inotropic selectivity, while one of them, described as 5,6-dihydroxy-N-[2-(4-hydroxyphenyl)-1-methylethyl]-2-aminoindan hydrobromide 17, showed a marked inotropic action on isolated heart tissue.
