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Dihydrexidine
Dihydrexidine (DAR-0100) 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 (highly biased) 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 Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D1 Receptor
Dopamine receptor D1, also known as DRD1. It is one of the two types of D1-like receptor family - receptors D1 and D5. It is a protein that in humans is encoded by the DRD1 gene. Tissue distribution D1 receptors are the most abundant kind of dopamine receptor in the central nervous system. Northern blot and in situ hybridization show that the mRNA expression of DRD1 is highest in the dorsal striatum ( caudate and putamen) and ventral striatum (nucleus accumbens and olfactory tubercle). Lower levels occur in the basolateral amygdala, cerebral cortex, septum, thalamus, and hypothalamus. Function D1 receptors regulate the memory, learning, and the growth of neurons, also is used in the reward system and locomotor activity, mediating some behaviors and modulating dopamine receptor D2-mediated events. They play a role in addiction by facilitating the gene expression changes that occur in the nucleus accumbens during addiction. They are Gs/a coupled and can stimulate neuron ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D5 Receptor
Dopamine receptor D5, also known as D1BR, is a protein that in humans is encoded by the ''DRD5'' gene. It belongs to the D1-like receptor family along with the D1 receptor subtype. Function D5 receptor is a subtype of the dopamine receptor that has a 10-fold higher affinity for dopamine than the D1 subtype. The D5 subtype is a G-protein coupled receptor, which promotes synthesis of cAMP by adenylyl cyclase via activation of Gαs/olf family of G proteins. Both D5 and D1 subtypes activate adenylyl cyclase. D1 receptors were shown to stimulate monophasic dose-dependent accumulation of cAMP in response to dopamine, and the D5 receptors were able to stimulate biphasic accumulation of cAMP under the same conditions, suggesting that D5 receptors may use a different system of secondary messengers than D1 receptors. Activation of D5 receptors is shown to promote expression of brain-derived neurotrophic factor and increase phosphorylation of protein kinase B in rat and mice prefro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants ''K''AB and ''K''AC.The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. : + B AB; \mathit K_ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdrawal, decreased emotional expression, and apathy. Symptoms typically develop gradually, begin during young adulthood, and in many cases never become resolved. There is no objective diagnostic test; diagnosis is based on observed behavior, a history that includes the person's reported experiences, and reports of others familiar with the person. To be diagnosed with schizophrenia, symptoms and functional impairment need to be present for six months (DSM-5) or one month (ICD-11). Many people with schizophrenia have other mental disorders, especially substance use disorders, depressive disorders, anxiety disorders, and obsessive–compulsive disorder. About 0.3% to 0.7% of people are diagnosed with schizophrenia during their lifetime. In 2 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D5 Receptor Agonists
D5 or D05 may refer to: Arts and fiction * ''Dedication 5'', a 2013 mixtape by American rapper Lil Wayne * D5 class Klingon starships, in the ''Star Trek'' science fiction series * Dimension Delete and Deadly Destruction Day, featured in ''Digimon Xros Wars'' Other uses * Digital 5, a network of leading digital governments * D5 HD, a professional digital video format * Demand 5, a video on demand website * The fifth D: All Things Digital, conference * Nikon D5, a 20.9 megapixel DSLR camera * Trident D5 ballistic missile * Volvo D5 engine, an engine family made by Volvo Cars Transport, aviation and logistics * Citroën D5 * Albatros D.V, a German World War I fighter plane * Identification symbol for ''Nachtjagdgeschwader'' 3, a Luftwaffe night fighter-wing of World War II * Dauair (IATA code D5) * Dublin 5, an Irish postal district * Land Rover D5 - Discovery 5 Roads * D5 motorway (Czech Republic) * D5 road (Croatia), a state road * Detour for the M5 South Western Mo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
D2-receptor Agonists
D, or d, is the fourth Letter (alphabet), letter in the Latin alphabet, used in the English alphabet, modern English alphabet, the alphabets of other western European languages and others worldwide. Its name in English is English alphabet#Letter names, ''dee'' (pronounced ), plural ''dees''. History The Semitic languages, Semitic letter Daleth, Dāleth may have developed from the logogram for a fish or a door. There are many different Egyptian hieroglyphs that might have inspired this. In Semitic, Ancient Greek and Latin, the letter represented ; in the Etruscan alphabet the letter was archaic, but still retained (see letter B). The equivalent Greek letter is Delta, Delta (letter), Δ. Architecture The Lower case, minuscule (lower-case) form of 'd' consists of a lower-story left Typeface anatomy#Strokes, bowl and a Typeface anatomy#Strokes, stem ascender. It most likely developed by gradual variations on the upper case, majuscule (capital) form 'D', and today now composed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Memory Deficit
Amnesia is a deficit in memory caused by brain damage or disease,Gazzaniga, M., Ivry, R., & Mangun, G. (2009) Cognitive Neuroscience: The biology of the mind. New York: W.W. Norton & Company. but it can also be caused temporarily by the use of various sedatives and hypnotic drugs. The memory can be either wholly or partially lost due to the extent of damage that was caused. There are two main types of amnesia: retrograde amnesia and anterograde amnesia. Retrograde amnesia is the inability to retrieve information that was acquired before a particular date, usually the date of an accident or operation. In some cases the memory loss can extend back decades, while in others the person may lose only a few months of memory. Anterograde amnesia is the inability to transfer new information from the short-term store into the long-term store. People with anterograde amnesia cannot remember things for long periods of time. These two types are not mutually exclusive; both can occur simul ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cognitive Deficit
Cognitive deficit is an inclusive term to describe any characteristic that acts as a barrier to the cognition process. The term may describe * deficits in overall intelligence (as with intellectual disabilities), * specific and restricted deficits in cognitive abilities (such as in learning disorders like dyslexia), * neuropsychological deficits (such as in attention, working memory or executive function), * or it may describe drug-induced impairment in cognition and memory (such as that seen with alcohol, glucocorticoids, and the benzodiazepines.) Cause It usually refers to a durable characteristic, as opposed to altered level of consciousness, which may be acute and reversible. Cognitive deficits may be inborn or caused by environmental factors such as brain injuries, neurological disorders, or mental illness. Screening Screening for cognitive impairment in those over the age of 65 without symptoms is of unclear benefit versus harm as of 2020. In a large population-based c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypotension
Hypotension is low blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood. Blood pressure is indicated by two numbers, the systolic blood pressure (the top number) and the diastolic blood pressure (the bottom number), which are the maximum and minimum blood pressures, respectively. A systolic blood pressure of less than 90 millimeters of mercury (mmHg) or diastolic of less than 60 mmHg is generally considered to be hypotension. Different numbers apply to children. However, in practice, blood pressure is considered too low only if noticeable symptoms are present. Symptoms include dizziness or lightheadedness, confusion, feeling tired, weakness, headache, blurred vision, nausea, neck or back pain, an irregular heartbeat or feeling that the heart is skipping beats or fluttering, or fainting. Hypotension is the opposite of hypertension, which is high blood pressure. It is best understood as a physiological st ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Development
Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regulatory status, such as via the United States Food and Drug Administration for an investigational new drug to initiate clinical trials on humans, and may include the step of obtaining regulatory approval with a new drug application to market the drug. The entire process – from concept through preclinical testing in the laboratory to clinical trial development, including Phase I–III trials – to approved vaccine or drug typically takes more than a decade. New chemical entity development Broadly, the process of drug development can be divided into preclinical and clinical work. Pre-clinical New chemical entities (NCEs, also known as new molecular entities or NMEs) are compounds that emerge from the process of drug discovery. Th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Full Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
