Abstract: Trans-hexahydrobenzoaphenanthridines of the formula (I) wherein X, Y, R1, R2, R3, R4, R5, R6, and R7 are as defined herein, are disclosed. Pharmaceutical formulations including such compounds, and methods of using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system are also disclosed.

Abstract: Trans-hexahydrobenzoaphenanthridines of the formula (I) wherein X, Y, R1, R2, R3, R4, R5, R6, and R7 are as defined herein, are disclosed. Pharmaceutical formulations including such compounds, and methods of using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system are also disclosed.

Abstract: Novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.

Abstract: The present invention relates to the treatment of dopamine-related dysfunction using full D1 dopamine receptor agonists in an intermittent dosing protocol with a short, but essential, “off-period.” The D1 agonist concentration is reduced during the “off-period” to obtain a plasma concentration of agonist that suboptimally activates D1 dopamine receptors for a period of time to prevent induction of tolerance. Specifically, the method comprises the steps of periodically administering to a patient a full D1 agonist with a half-life of up to about 6 hours at a dose resulting in a first plasma concentration of agonist capable of activating D1 dopamine receptors to produce a therapeutic effect. The dose is reduced at least once every 24 hours to obtain a second lower plasma concentration of agonist that results in suboptimal activation of D1 dopamine receptors for a period of time sufficient to prevent induction of tolerance.

Abstract: The present invention relates to the treatment of dopamine-related dysfunction using full D1 dopamine receptor agonists in an intermittent dosing protocol with a short, but essential, “off-period.” The D1 agonist concentration is reduced during the “off-period” to obtain a plasma concentration of agonist that suboptimally activates D1 dopamine receptors for a period of time to prevent induction of tolerance. Specifically, the method comprises the steps of periodically administering to a patient a full D1 agonist with a half-life of up to about 6 hours at a dose resulting in a first plasma concentration of agonist capable of activating D1 dopamine receptors to produce a therapeutic effect. The dose is reduced at least once every 24 hours to obtain a second lower plasma concentration of agonist that results in suboptimal activation of D1 dopamine receptors for a period of time sufficient to prevent induction of tolerance.

Abstract: Novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.

Abstract: Trans-hexahydrobenzo[a]phenanthridine of the formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 is hydrogen or a phenoxy protecting group, X is fluoro, chloro, bromo, iodo or a group of the formula--OR.sub.5, and R.sub.2, R.sub.3, and R.sub.4 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, fluoro, chloro, bromo, iodo, or a group --OR.sub.1 provided that at least one of R.sub.2, R.sub.3, and R.sub.4 are other than hydrogen, are novel ligands for dopamine receptors.