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A-77636
A-77636 is a synthetic drug which acts as a selective D1 receptor full agonist. It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies, but its high potency and long duration of action causes D1 receptor downregulation and tachyphylaxis, and unlike other D1 full agonists such as SKF-82,958, it does not produce place preference in animals. A-77636 partially substituted for cocaine Cocaine (from , from , ultimately from Quechuan languages, Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly recreational drug use, used recreationally for its euphoria, euphoric effects. It is primarily obtained from t ... in animal studies, and has been suggested for use as a possible substitute drug in treating addiction, but it is better known for its use in studying the role of D1 receptors in the brain. References D1-receptor agonists Adamantanes Isochromenes Catechols {{Organic-compound-stub ... [...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] |
Hydrochloride
In chemistry, a hydrochloride is an acid salt resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (e.g. an amine). An alternative name is chlorhydrate, which comes from French. An archaic alternative name is muriate, derived from hydrochloric acid's ancient name: muriatic acid. Uses Converting amines into their hydrochlorides is a common way to improve their water solubility, which can be desirable for substances used in medications. The European Pharmacopoeia lists more than 200 hydrochlorides as active ingredients in medications. These hydrochlorides, compared to free bases, may more readily dissolve in the gastrointestinal tract and be absorbed into the bloodstream more quickly. Additionally, many hydrochlorides of amines have a longer shelf-life than their respective free bases. Amine hydrochlorides represent latent forms of a more reactive free base. In this regard, formation of an amine hydrochloride confers protection. This eff ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Synthesis
As a topic of chemistry, chemical synthesis (or combination) is the artificial execution of chemical reactions to obtain one or several products. This occurs by physical and chemical manipulations usually involving one or more reactions. In modern laboratory uses, the process is reproducible and reliable. A chemical synthesis involves one or more compounds (known as '' reagents'' or ''reactants'') that will experience a transformation when subjected to certain conditions. Various reaction types can be applied to formulate a desired product. This requires mixing the compounds in a reaction vessel, such as a chemical reactor or a simple round-bottom flask. Many reactions require some form of processing (" work-up") or purification procedure to isolate the final product. The amount produced by chemical synthesis is known as the ''reaction yield''. Typically, yields are expressed as a mass in grams (in a laboratory setting) or as a percentage of the total theoretical quantity that ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ... [...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] |
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 |
Nootropic
Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic supplements or drugs and other substances that are claimed to improve cognitive function or to promote relaxation, particularly boosting mood, executive functions, attention, memory, creativity, or motivation in healthy individuals. The use of cognition-enhancing supplements by healthy individuals in the absence of a medical indication spans numerous controversial issues, including the ethics and fairness of their use, concerns over adverse effects, and the diversion of prescription drugs for non-medical uses. Nonetheless, the international sales of cognitive- or mood-enhancing supplements have continued to grow over time and in 2012 reached 0.69 billion. With sales supported by global health trends, the market is expected to reach US$33.85 billion by the year 2030, at a CAGR of 14.8%. While most nootropics are not regulated, there are ot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anorectic
An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek ''ἀν-'' (an-) = "without" and ''ὄρεξις'' (órexis) = "appetite"), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term basis clinically to treat obesity, some appetite suppressants are also available over-the-counter. Most common natural appetite suppressants are based on ''Hoodia'', a genus of 13 species in the flowering plant family Apocynaceae, under the subfamily Asclepiadoideae. Several appetite suppressants are based on a mix of natural ingredients, mostly using green tea as its basis, in combination with other plant extracts such as fucoxanthin, found naturally in seaweed. Drugs of this class are frequently stimulants of the phenethylamine family, related to amphetamine. The German and Fi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Management Of Parkinson's Disease
In the management of Parkinson's disease, due to the chronic nature of Parkinson's disease (PD), a broad-based program is needed that includes patient and family education, support-group services, general wellness maintenance, exercise, and nutrition. At present, no cure for the disease is known, but medications or surgery can provide relief from the symptoms. While many medications treat Parkinson's, none actually reverses the effects of the disease. Furthermore, the gold-standard treatment varies with the disease state. People with Parkinson's, therefore, often must take a variety of medications to manage the disease's symptoms. Several medications currently in development seek to better address motor fluctuations and nonmotor symptoms of PD. However, none is yet on the market with specific approval to treat Parkinson's. Medication The main families of drugs useful for treating motor symptoms are levodopa, dopamine agonists, and MAO-B inhibitors. The most commonly used treatm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachyphylaxis
Tachyphylaxis (Greek ταχύς, ''tachys'', "rapid", and φύλαξις, ''phylaxis'', "protection") is a medical term describing an acute, sudden decrease in response to a drug after its administration; i.e. a rapid and short-term onset of drug tolerance. It can occur after an initial dose or after a series of small doses. Increasing the dose of the drug may be able to restore the original response. Characteristics Tachyphylaxis is characterized by the rate sensitivity: the response of the system depends on the rate with which a stimulus is presented. To be specific, a high-intensity prolonged stimulus or often-repeated stimulus may bring about a diminished response also known as desensitization. Molecular interaction In biological sciences, molecular interactions are the physical bases of the operation of the system. The control of the operation, in general, involves interaction of a stimulus molecule with a receptor/enzyme subsystem by, typically, binding to the macromolecule A a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SKF-82,958
SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/ D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine. SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen Estrogen or oestrogen is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal acti .... References 1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Synthetic estrogens GSK plc brands D1-receptor agonists D5 receptor agonists Phenols Chloroarenes Allyl compounds {{gastrointestinal-drug-st ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cocaine
Cocaine (from , from , ultimately from Quechuan languages, Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly recreational drug use, used recreationally for its euphoria, euphoric effects. It is primarily obtained from the leaves of two Coca species native to South America, ''Erythroxylum coca'' and ''Erythroxylum novogranatense''. After extraction from coca leaves and further processing into cocaine hydrochloride (powdered cocaine), the drug is often Insufflation (medicine), snorted, applied topical administration, topically to the mouth, or dissolved and injection (medicine), injected into a vein. It can also then be turned into free base form (crack cocaine), in which it can be heated until sublimated and then the vapours can be smoking, inhaled. Cocaine stimulates the mesolimbic pathway, reward pathway in the brain. Mental effects may include an euphoria, intense feeling of happiness, sexual arousal, psychosis, loss of contact with reality, or psychomo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
