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Hydroxydione
Hydroxydione, as hydroxydione sodium succinate (, , ) (brand names Viadril, Predion, and Presuren), also known as 21-Hydroxy-5β-pregnane-3,20-dione, is a neuroactive steroid which was formerly used as a general anesthetic, but was discontinued due to incidence of thrombophlebitis in patients. It was introduced in 1957, and was the first neuroactive steroid general anesthetic to be introduced for clinical use, an event which was shortly preceded by the observation in 1954 of the sedative properties of progesterone in mice. Chemistry Related compounds include alfadolone, alfaxolone, dihydrodeoxycorticosterone, ganaxolone, minaxolone, pregnanolone, and renanolone. References {{GABAA receptor positive modulators 5β-Pregnanes Primary alcohols Diketones GABAA receptor positive allosteric modulators General anesthetics Neurosteroids ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Renanolone
Renanolone (International Nonproprietary Name, INN), or 11-ketopregnanolone, also known as 5β-pregnan-3α-ol-11,20-dione, is a synthetic compound, synthetic neuroactive steroid which is described as a general anesthetic but was never introduced for clinical use. Its isomers, alfaxolone and alfadolone, are also general anesthetics, and are known to act as positive allosteric modulators of the GABAA receptor, GABAA receptor, a property which is likely the case for renanolone as well. Chemistry See also * Alfadolone * Alfaxolone * Ganaxolone * Hydroxydione * Minaxolone * Pregnanolone References 5β-Pregnanes General anesthetics Neurosteroids Secondary alcohols Diketones GABAA receptor positive allosteric modulators {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter Gamma-Aminobutyric acid, gamma-aminobutyric acid (GABA). Most sedatives produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or Anxiolytic, relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness), they are often referred to collectively as ''sedative–hypnotic'' drugs. Terminology There is some overlap ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alfadolone
Alfadolone ( INN), or alphadolone is a neuroactive steroid and general anesthetic. Along with alfaxolone, as alfadolone acetate, it is one of the components of the anesthetic drug mixture althesin. Chemistry See also * Ganaxolone * Hydroxydione * Minaxolone * Pregnanolone * Renanolone References General anesthetics Neurosteroids GABAA receptor positive allosteric modulators Pregnanes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dihydrodeoxycorticosterone
5α-Dihydrodeoxycorticosterone (abbreviated as DHDOC), also known as 21-hydroxy-5α-pregnan-20-one, is an endogenous progestogen and neurosteroid. It is synthesized from the adrenal hormone deoxycorticosterone (DOC) by the enzyme 5α-reductase type I. DHDOC is an agonist of the progesterone receptor, as well as a positive allosteric modulator of the GABAA receptor, and is known to have anticonvulsant effects. Chemistry See also * Tetrahydrodeoxycorticosterone (THDOC) * 5α-Dihydroprogesterone (DHP) * Hydroxydione Hydroxydione, as hydroxydione sodium succinate (, , ) (brand names Viadril, Predion, and Presuren), also known as 21-Hydroxy-5β-pregnane-3,20-dione, is a neuroactive steroid which was formerly used as a general anesthetic, but was discontinued d ... References {{GABAAR PAMs Neurosteroids Pregnanes Progestogens GABAA receptor positive allosteric modulators ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuroactive Steroid
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. The term ''neurosteroid'' was coined by the French physiologist Étienne-Émile Baulieu and refers to steroids synthesized in the brain. The term, ''neuroactive steroid'' refers to steroids that can be synthesized in the brain, or are synthesized by an endocrine gland, that then reach the brain through the bloodstream and have effects on brain function. The term neuroactive steroids was first coined in 1992 by Steven Paul and Robert Purdy. In addition to their actions on neuronal membrane receptors, some of these steroids may also exert effects on gene expression via nuclear steroid hormone receptors. Neurosteroids have a wide range of potential clinical applications from sedation to treatment of epilepsy and traumatic brain injury. Ganaxolone, a synthetic analog of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Minaxolone
Minaxolone (CCI-12923) is a neuroactive steroid which was developed as a general anesthetic but was withdrawn before registration due to toxicity seen with long-term administration in rats, and hence was never marketed. It is a positive allosteric modulator of the GABAA receptor, as well as, less potently, a positive allosteric modulator of the glycine receptor. Chemistry See also * Alfadolone * Alfaxolone * Ganaxolone * Hydroxydione * Pregnanolone * Renanolone Renanolone (International Nonproprietary Name, INN), or 11-ketopregnanolone, also known as 5β-pregnan-3α-ol-11,20-dione, is a synthetic compound, synthetic neuroactive steroid which is described as a general anesthetic but was never introduced ... References General anesthetics Neurosteroids Secondary alcohols Ethers Dimethylamino compounds Ketones GABAA receptor positive allosteric modulators Glycine receptor agonists Pregnanes Ethoxy compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diário Oficial Da União
The ''Diário Oficial da União'' (literally ''Official Diary of the Union''), abbreviated DOU, is the government gazette, official gazette of the Federal Government of Brazil, Federal Government of Brazil. It is published since 1 October 1862 and was created via the Imperial Decree 1,177 of its 9 September as the ''Official Journal of the Empire of Brazil''. Its current name was adopted after Brazil became a federal republic, and the "Union" came into being as the legal personality of the new federal government. The official journal is published by the Imprensa Nacional, Brazilian National Press. Though the journal has been published since 1862, it had many predecessors, as follows: # Gazeta do Rio de Janeiro (10/9/1808 – 29.12.1821) # Gazeta do Rio (1/1/1822 – 31/12/1822) # Diário do Governo (2/1/1823 – 28/6/1833) # Diário Fluminense (21/5/1824 – 24/4/1831) # Correio Oficial (1/7/1833 – 30/6/1836) e (2/1/1830 – 30/12/1840) # Without proper journal (31/12/1840 – ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor Positive Allosteric Modulators
In pharmacology, GABAA receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor, GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it Agonist, triggers the GABAA receptor to open its GABAA receptor#Structure and function, chloride channel to allow Chloride, chloride ions into the neuron, making the cell Hyperpolarization (biology), hyperpolarized and less likely to Action potential, fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABA receptor agonist, GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-aminobutyric acid (GABA) neurotransmitter molecule: they affect the r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diketones
In organic chemistry, a dicarbonyl is a molecule containing two carbonyl () Functional group, groups. Although this term could refer to any organic compound containing two carbonyl groups, it is used more specifically to describe molecules in which both carbonyls are in close enough proximity that their Reactivity (chemistry), reactivity is changed, such as 1,2-, 1,3-, and 1,4-dicarbonyls. Their properties often differ from those of monocarbonyls, and so they are usually considered functional groups of their own. These compounds can have symmetrical or unsymmetrical substituents on each carbonyl, and may also be functionally symmetrical (dialdehydes, diketones, diesters, ''etc.'') or unsymmetrical (keto-esters, keto-acids, ''etc.''). 1,2-Dicarbonyls 1,2-Dialdehyde The only 1,2-dialdehyde is glyoxal, . Like many alkyldialdehydes, glyoxal is encountered almost exclusively as its hydrate and oligomers thereof. These derivatives often behave equivalently to the aldehydes since hydra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Primary Alcohols
A primary alcohol is an Alcohol (chemistry), alcohol in which the hydroxy group is bonded to a primary carbon atom. It can also be defined as a molecule containing a “–CH2OH” group. In contrast, a secondary alcohol has a formula “–CHROH” and a tertiary alcohol has a formula “–CR2OH”, where “R” indicates a carbon-containing group. Examples of primary alcohols include ethanol, 1-propanol, and n-Butanol, 1-butanol. Methanol is also generally regarded as a primary alcohol, including by the 1911 edition of the Encyclopædia Britannica. See also * Alcohol (chemistry), Alcohol (especially Nomenclature section for discussion on Secondary and Tertiary alcohols.) * Oxidation of primary alcohols to carboxylic acids References Primary alcohols, {{organic-chem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ganaxolone
Ganaxolone, sold under the brand name Ztalmy, is a medication used to treat seizures in people with cyclin-dependent kinase-like 5 (CDKL5) deficiency disorder. Ganaxolone is a neuroactive steroid gamma-aminobutyric acid (GABA) A receptor positive modulator. The most common side effects of treatment with ganaxolone include somnolence (sleepiness), fever, excessive saliva or drooling, and seasonal allergy. Ganaxolone was approved for medical use in the United States in March 2022, and in the European Union in July 2023. The US Food and Drug Administration (FDA) considers it to be a first-in-class medication. Medical uses Ganaxolone is indicated for the treatment of seizures associated with cyclin-dependent kinase-like 5 (CDKL5) deficiency disorder. Pharmacology Mechanism of action The exact mechanism of action for ganaxolone is unknown; however, results from animal studies suggest that it acts by blocking seizure propagation and elevating seizure thresholds. Ganaxolone ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
