β1 Partial agonists as positive inotropic agents.

Classification of positive inotropic agents.

Although there is increasing recognition that all inotropic agents are not alike, they continue to be viewed in the generic sense because of the lack of a classification system. Analogous to the classification system proposed for the antiarrhythmic agents over 20 years ago, a classification system is proposed that categorizes inotropic agents according to their mechanisms of action. Agents are ...

Do dopamine partial agonists have partial efficacy as antipsychotics?

CNS Spectr 13:4 April 2008 279 NEW TREND IN PSYCHOPHARMACOLOGY Dopamine (D)2 partial agonists (DPAs) activate D2 receptors in a manner that is less than the full agonist dopamine yet more than full antagonists (eg, most known antipsychotics). Various DPAs span the spectrum between full agonist at one end and antagonists at the other, with the antipsychotic aripiprazole close to the antagonist e...

Partial Dopamine D2/Serotonin 5-HT1A Receptor Agonists as New Therapeutic Agents

The therapeutic efficacy of current antipsychotic or antidepressant agents still present important drawbacks such as delayed onset of action and a high percentage of non-responders. Despite significant advancements in the development of new drugs with more acceptable side-effect profiles, patients with schizophrenia or major depression experience substantial disability and burden of disease. Th...

Clinical use of inotropic agents.

Synthesis and in Vitro and in Vivo Characterization of Highly β1-Selective β-Adrenoceptor Partial Agonists

β-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human β-adrenoceptor subtype involved in these diseases, yet few truly β1-selective molecules exist. To address this clinical need, we re-evaluated LK 204-545 (1), (1) a selective β1-adrenoceptor antagonist, and discovere...