Dihydrexidine
Encyclopedia
Dihydrexidine is a moderately selective
full agonist at the dopamine
D1 and D5 receptors. It has approximately 10-fold selectivity for D1 and D5 over the D2 receptor. Although dihydrexidine has some affinity for the D2 receptor, it has functionally selective D2 signaling, thereby explaining why it lacks D2 agonist behavioral qualities.
Dihydrexidine has shown impressive antiparkinson effects in the MPTP-primate model, and has been investigated for the treatment
of Parkinson's disease
. In an early clinical trial
the drug was given intravenously and led to profound hypotension
so development
was halted. The drug was resurrected when it was shown that smaller subcutaneous doses were safe. This led to a pilot study in schizophrenia
and current clinical trials to assess its efficacy in improving the cognitive
and working memory deficits in schizophrenia
and schizotypal disorder.
There have been several reviews of relevance to the compound.
Binding selectivity
Binding selectivity refers to the differing affinities with which different ligands bind to a substrate forming a complex. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate...
full agonist at the dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
D1 and D5 receptors. It has approximately 10-fold selectivity for D1 and D5 over the D2 receptor. Although dihydrexidine has some affinity for the D2 receptor, it has functionally selective D2 signaling, thereby explaining why it lacks D2 agonist behavioral qualities.
Dihydrexidine has shown impressive antiparkinson effects in the MPTP-primate model, and has been investigated for the treatment
Therapy
This is a list of types of therapy .* Adventure therapy* Animal-assisted therapy* Aquatic therapy* Aromatherapy* Art and dementia* Art therapy* Authentic Movement* Behavioral therapy* Bibliotherapy* Buteyko Method* Chemotherapy...
of Parkinson's disease
Parkinson's disease
Parkinson's disease is a degenerative disorder of the central nervous system...
. In an early clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
the drug was given intravenously and led to profound hypotension
Hypotension
In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...
so development
Drug development
Drug development is a blanket term used to define the process of bringing a new drug to the market once a lead compound has been identified through the process of drug discovery...
was halted. The drug was resurrected when it was shown that smaller subcutaneous doses were safe. This led to a pilot study in schizophrenia
Schizophrenia
Schizophrenia is a mental disorder characterized by a disintegration of thought processes and of emotional responsiveness. It most commonly manifests itself as auditory hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and it is accompanied by significant social...
and current clinical trials to assess its efficacy in improving the cognitive
Cognitive deficit
Cognitive deficit, also known as cognitive impairment is an inclusive term to describe any characteristic that acts as a barrier to cognitive performance...
and working memory deficits in schizophrenia
Schizophrenia
Schizophrenia is a mental disorder characterized by a disintegration of thought processes and of emotional responsiveness. It most commonly manifests itself as auditory hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and it is accompanied by significant social...
and schizotypal disorder.
There have been several reviews of relevance to the compound.