Neurosteroids
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Neurosteroids
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 en ...
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Allopregnanolone
Allopregnanolone is a natural product, naturally occurring neurosteroid which is made in the body from the hormone progesterone. As a medication, allopregnanolone is referred to as brexanolone, sold under the brand name Zulresso, and used to treat postpartum depression. It is given by intravenous, injection into a vein. Side effects of brexanolone may include sedation, sleepiness, dry mouth, hot flashes, and loss of consciousness. It is a neurosteroid and acts as a positive allosteric modulator of the GABAA receptor, GABAA receptor, the major biological target of the inhibitory postsynaptic potential, inhibitory neurotransmitter γ-aminobutyric acid (GABA). Brexanolone was approved for medical use in the United States in 2019. The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. The long administration time, as well as the cost for a one-time treatment, have raised concerns about accessibility for many women. Medical uses Brexanolon ...
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GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous Ligand (biochemistry), ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Accurate regulation of GABAergic transmission through appropriate developmental processes, specificity to neural cell types, and responsiveness to activity is crucial for the proper functioning of nearly all aspects of the central nervous system (CNS). Upon opening, the GABAA receptor on the Chemical synapse, postsynaptic cell is selectively permeable to Chloride, chloride ions () and, to a lesser extent, Bicarbonate, bicarbonate ions (). GABAAR are members of the ligand-gated ion channel receptor superfamily, which is a chloride channel family with a dozen or more heterotetrametric subtypes and 19 distinct subunits. These subtypes have distinct brain regional and subcellular localization, age-dependent expression, and the ability to undergo plastic alt ...
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Étienne-Émile Baulieu
Étienne-Émile Baulieu (; 12 December 1926 – 30 May 2025) was a French biochemist and endocrinologist who was best known for his research in the field of steroid hormones and their role in reproduction and aging. He has been nicknamed the “father” of the abortion pill mainly as a result of his work on the abortion-inducing drug RU486 (Mifepristone). Baulieu also worked to determine if dehydroepiandrosterone (DHEA) was a prohormone and if it and other hormonal substitutions also increased longevity in humans. Early life and education Baulieu was born Émile Blum to Jewish parents in Strasbourg, France, on 12 December 1926. His father, who died when Baulieu was four, was Léon Blum, a physician and an early specialist in diabetes. Baulieu changed his name during World War II when his family fled to the area near Grenoble and he engaged in the French resistance. After the war, he attended the Faculté de Médecine de Paris and became a physician in 1955. He studied furt ...
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Zuranolone
Zuranolone, sold under the brand name Zurzuvae, is a medication used for the treatment of postpartum depression. It is taken by mouth. The most common side effects include drowsiness, dizziness, diarrhea, fatigue, nasopharyngitis, and urinary tract infection. An orally active inhibitory pregnane neurosteroid, zuranolone acts as a positive allosteric modulator of the GABAA receptor. Zuranolone was approved for medical use in the United States for the treatment of postpartum depression in August 2023. It was developed by Sage Therapeutics and Biogen. Medical uses Zuranolone is indicated for the treatment of postpartum depression. Adverse effects The most common side effects include drowsiness, dizziness, diarrhea, fatigue, and urinary tract infection. The US FDA label contains a boxed warning noting that zuranolone can impact a person's ability to drive and perform other potentially hazardous activities. The use of zuranolone may cause suicidal thoughts and behavi ...
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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 ...
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Steroid Hormone Receptor
Steroid hormone receptors are found in the nucleus, cytosol, and also on the plasma membrane of target cells. They are generally intracellular receptors (typically cytoplasmic or nuclear) and initiate signal transduction for steroid hormones which lead to changes in gene expression over a time period of hours to days. The best studied steroid hormone receptors are members of the nuclear receptor subfamily 3 (NR3) that include receptors for estrogen (group NR3A) and 3-ketosteroids (group NR3C). In addition to nuclear receptors, several G protein-coupled receptors and ion channels act as cell surface receptors for certain steroid hormones. A steroid hormone receptor is a protein molecule located either within the cell cytoplasm or nucleus that specifically binds to steroid hormones, such as estrogen, progesterone, and testosterone, leading to the activation or suppression of gene expression and subsequent cellular responses. This interaction is crucial for mediating the physiologic ...
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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 ...
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Physiologist
Physiology (; ) is the scientific study of functions and mechanisms in a living system. As a subdiscipline of biology, physiology focuses on how organisms, organ systems, individual organs, cells, and biomolecules carry out chemical and physical functions in a living system. According to the classes of organisms, the field can be divided into medical physiology, animal physiology, plant physiology, cell physiology, and comparative physiology. Central to physiological functioning are biophysical and biochemical processes, homeostatic control mechanisms, and communication between cells. ''Physiological state'' is the condition of normal function. In contrast, '' pathological state'' refers to abnormal conditions, including human diseases. The Nobel Prize in Physiology or Medicine is awarded by the Royal Swedish Academy of Sciences for exceptional scientific achievements in physiology related to the field of medicine. Foundations Because physiology focuses on the ...
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Positive Allosteric Modulator
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. Some of them, like benzodiazepines or alcohol, function as psychoactive drugs. The site that an allosteric modulator binds to (i.e., an ''allosteric site'') is not the same one to which an endogenous agonist of the receptor would bind (i.e., an ''orthosteric site''). Modulators and agonists can both be called receptor ligands. Allosteric modulators can be 1 of 3 types either: positive, negative or neutral. Positive types increase the response of the receptor by increasing the probability that an agonist will bind to a receptor (i.e. affinity), increasing its ability to activate the receptor (i.e. efficacy), or both. Negative types decrease the agonist affinity and/or efficacy. Neutral types don't affect agonist activity but can stop other modulators from binding to an allosteric site. Some modulators also work as allosteric agonis ...
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Aphrodisiac
An aphrodisiac is a substance that increases libido, sexual desire, sexual attraction, sexual pleasure, or sexual behavior. These substances range from a variety of plants, spices, and foods to synthetic chemicals. Natural aphrodisiacs, such as cannabis (drug), cannabis or cocaine, are classified into plant-based and non-plant-based substances. Synthetic aphrodisiacs include MDMA and methamphetamine. Aphrodisiacs can be classified by their type of effects (psychological or physiological). Aphrodisiacs that contain hallucinogenic properties, such as bufotenin, have psychological effects that can increase sexual desire and sexual pleasure. Aphrodisiacs that have smooth muscle relaxing properties, such as yohimbine, have physiological effects that can affect hormone concentrations and increase blood flow. Substances that have the opposite effects on libido are called anaphrodisiacs. Aphrodisiac effects can also be due to the Placebo, placebo effect. Both males and females can po ...
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Serenic
A serenic, or anti-aggressive drug, is a type of drug which reduces the capacity for aggression. Examples Serotonergic agents The recreational drug MDMA ("ecstasy") and a variety of related drugs have been described as '' empathogen-entactogens'', or simply as ''entactogens''. These agents possess serenic and empathy-increasing properties in addition to their euphoriant effects, and have been associated with increased sociability, friendliness, and feelings of closeness to others as well as emotional empathy and prosocial behavior. The entactogenic effects of these drugs are thought to be related to their ability to temporarily increase the levels of certain brain chemicals, including serotonin, dopamine, and, particularly, oxytocin. Certain other serotonergic drugs, such as 5-HT1A receptor agonists, also increase oxytocin levels and may possess serenic properties as well. The phenylpiperazine mixed 5-HT1A and 5-HT1B receptor agonists eltoprazine, fluprazine, and batop ...
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Prosocial Behavior
Prosocial behavior is a social behavior that "benefit other people or society as a whole", "such as helping, sharing, donating, co-operating, and volunteering". The person may or may not intend to benefit others; the behavior's prosocial benefits are often only calculable after the fact. (Consider: Someone may intend to 'do good' but the effects may be catastrophic.) Obeying the rules and conforming to socially accepted behaviors (such as stopping at a "Stop" sign or paying for groceries) are also regarded as prosocial behaviors. These actions may be motivated by culturally influenced value systems; empathy and concern about the welfare and rights of others;Santrock, John W. A Topical Approach to Life Span Development 4th Ed. New York: McGraw-Hill, 2007. Ch. 15, pp. 489–491 egoistic or practical concerns, such as one's social status or reputation, hope for direct or indirect reciprocity, or adherence to one's perceived system of fairness; or altruism, though the existence ...
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