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Fasedienol
Fasedienol (; developmental code names PH94B and Aloradine), also known as 4-androstadienol or as 4,16-androstadien-3β-ol, is a pherine which is under development by VistaGen Therapeutics in a nasal spray formulation ( ''PRN'') for the acute treatment of social anxiety disorder. It is also being investigated by VistaGen Therapeutics for the treatment of generalized anxiety disorder (GAD) and post-traumatic stress disorder (PTSD). The pherine is a positional isomer of the endogenous pheromone androstadienol (5-androstadienol or 5,16-androstadien-3β-ol). As of 2020, it is in phase III clinical trials for social anxiety disorder. Fasedienol lacks affinity for steroid hormone receptors and has instead been found to directly activate isolated human vomeronasal receptor cells at nanomolar concentrations ( EC50 = 200nM). The pheromone androstenol has been found to act as a potent positive allosteric modulator of the GABAA receptor, and it has been proposed that this action may medi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pherine
Pherines, also known as vomeropherines, are odorless synthetic neuroactive steroids that engage nasal chemosensory receptors and induce dose-dependent and reversible pharmacological and behavioral effects. Pherines target human chemosensory receptors and possibly other receptors such as the GABAA receptor and influence central nervous system activity. Currently known pherine molecules are being developed for the treatment of various medical conditions. Pherines specifically target nasal chemosensory cells and mediate selective modulation of brain areas like the limbic amygdala, hypothalamus, hippocampus, and prefrontal cortex. In clinical trials, pherines formulated for intranasal administration in ultra low doses (nanogram to low microgram quantities) showed rapid onset of efficacy (10–15 minutes) and an excellent safety and tolerability profile. Pherines are also minimally invasive (do not require systemic absorption) to exert their pharmacological effects and can be used ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Anxiolytics
This is a list of investigational anxiolytics, or anxiolytics that are currently under development for clinical use but are not yet approved. Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses. Generalized anxiety disorder * Agomelatine (AGO-178; Valdoxan) – melatonin MT1 and MT2 receptor agonist, 5-HT2C receptor antagonist* Riluzole sublingual (BHV-0223) – undefined mechanism of action * TGFK08AA – 5-HT ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Neurosteroids
This is a list of neurosteroids, or natural and synthetic steroids that are active on the mammalian nervous system through receptors other than steroid hormone receptors. It includes inhibitory, excitatory, and neurotrophic neurosteroids as well as pheromones and vomeropherines. In contrast to steroid hormones, neurosteroids have rapid, non- genomic effects through interactions with membrane steroid receptors and can quickly influence central nervous system function. Inhibitory Natural Cholestanes * 25-Hydroxycholesterol: cholest-5-en-3β,25-diol – NMDA receptor negative allosteric modulator Androstanes * 3α,5α-Androstanediol (3α-androstanediol): 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator * 3α,5β-Androstanediol (etiocholanediol): 5β-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator * 3α-Androstenol: 5α-androst-16-en-3α-ol – GABAA receptor positive allosteric modulator * Androsterone: 5α-androsta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intranasal
Nasal administration, popularly known as snorting, is a route of administration in which drugs are insufflated through the nose. It can be a form of either topical administration or systemic administration, as the drugs thus locally delivered can go on to have either purely local or systemic effects. Nasal sprays are locally acting drugs such as decongestants for cold and allergy treatment, whose systemic effects are usually minimal. Examples of systemically active drugs available as nasal sprays are migraine drugs, rescue medications for overdose and seizure emergencies, nicotine replacement, and hormone treatments. Advantages with nasal systemic drug delivery The nasal cavity is covered by a thin mucosa which is well vascularised. Therefore, a drug molecule can be transferred quickly across the single epithelial cell layer directly to the systemic blood circulation without first-pass hepatic and intestinal metabolism. The effect is often reached within 5 min for smaller ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androstanes
An androgen (from Greek ''andr-'', the stem of the word meaning "man") is any natural or synthetic steroid hormone that regulates the development and maintenance of male characteristics in vertebrates by binding to androgen receptors. This includes the embryological development of the primary male sex organs, and the development of male secondary sex characteristics at puberty. Androgens are synthesized in the testes, the ovaries, and the adrenal glands. Androgens increase in both males and females during puberty. The major androgen in males is testosterone. Dihydrotestosterone (DHT) and androstenedione are of equal importance in male development. DHT ''in utero'' causes differentiation of the penis, scrotum and prostate. In adulthood, DHT contributes to balding, prostate growth, and sebaceous gland activity. Although androgens are commonly thought of only as male sex hormones, females also have them, but at lower levels: they function in libido and sexual arousal. Also, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androstenone
Androstenone (5α-androst-16-en-3-one) is a 16-androstene class steroidal pheromone. It is found in boar's saliva, celery cytoplasm, and truffle fungus. Androstenone was the first mammalian pheromone to be identified. It is found in high concentrations in the saliva of male pigs, and, when inhaled by a female pig that is in heat, results in the female assuming the mating stance. Androstenone is the active ingredient in 'Boarmate', a commercial product made by DuPont sold to pig farmers to test sows for timing of artificial insemination. Biosynthesis Androstenone is synthesized from androstadienone by 5α-reductase, and can be converted into 3α-androstenol or 3β-androstenol by 3-ketosteroid reductase. Properties Depending upon the subject, it is reported to be an unpleasant, sweaty, urinous smell, a woody smell, or even a pleasant floral smell. There are two different genotypes that allow an individual to smell androstenone. The first genotype, which consists of two ful ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androstadienone
Androstadienone, or androsta-4,16-dien-3-one, is a 16-androstene class endogenous steroid that has been described as having potent pheromone-like activities in humans. The compound is synthesized from androstadienol by 3β-hydroxysteroid dehydrogenase, and can be converted into androstenone (a more potent and odorous pheromone) by 5α-reductase, which can subsequently be converted into 3α-androstenol or 3β-androstenol (also more potent and odorous pheromones) by 3-ketosteroid reductase. Androstadienone is related to the androgen sex hormones; however, androstadienone does not exhibit any androgenic or anabolic effects. Though it has been reported to significantly affect the mood of heterosexual women and homosexual men Gay men are male homosexuals. Some bisexual men, bisexual and homoromantic men may also dually identify as gay, and a number of young gay men also identify as queer. Historically, gay men have been referred to by a number of different terms, ..., it d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androstadienol
Androstadienol, or androsta-5,16-dien-3β-ol, is a 16-Androstene, 16-androstene class endogenous steroid, pheromone, and chemical intermediate to several other pheromones that is found in the sweat of both men and women. Androstadienol and androstadienone are odorless compounds secreted by the apocrine glands, and via conversion into the more powerfully-odorous androstenone and androstenol (catalyzed by Aerobic organism, aerobic corynebacteria, particularly ''Corynebacterium xerosis'', in men, and ''Micrococcaceae, Micrococcaceae spp.'' in women), are considered to be mainly responsible for the "musky" component of axillary (underarm) body odor, odor. Androstadienol is biosynthesis, synthesized from pregnenolone by the 16-ene-synthetase activity of CYP17A1, and is converted into androstadienone by 3β-hydroxysteroid dehydrogenase. Male sweat contains approximately five times as much androstenone as does female sweat, which can be explained by sexual dimorphism, sex differences in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiety disorders and their related psychological and physical symptoms. Nature of anxiety Anxiety is a naturally-occurring emotion and an innate response of the body to the environmental stimuli. Mild to moderate anxiety would increase level of performance. However, when anxiety levels exceed the tolerability of a person, anxiety disorders may occur. People with anxiety disorders can exhibit fear responses such as defensive behaviors, high levels of alertness and negative emotions, without external stimuli which induce anxiety within an individual. Those with anxiety disorders are also often found to have concurrent psychological disorders, most commonly depression. Anxiety disorders are divided into 6 types in clinical recognition. They are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV). T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 stimulus. Some of them, like benzodiazepines, are 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 agonists. The term "allosteric" derive ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Androstenol
Androstenol, also known as 5α-androst-16-en-3α-ol (shortened to 3α,5α-androstenol or 3α-androstenol), is a 16-androstene class steroidal pheromone and neurosteroid in humans and other mammals, notably pigs. It possesses a characteristic musk-like odor. Androstenol, or a derivative, is found in black truffles. This was offered as an explanation for how pigs locate them deep in the ground: Androstenol is produced in the saliva of male pigs. However, experiments in France using pigs to scent truffles, truffle scent extract, and purified androstenol showed that pigs responded to the first two (actually trying to eat dirt containing the truffle extract), but ignored the androstenol. A positional isomer of androstenol, 3β-androstenol (5α-androst-16-en-3β-ol), is also endogenous to humans (as well as to pigs), behaving as a pheromone and contributing to axillary odor. Biosynthesis In humans and boars, androstenol is biosynthesized in the testes. Pregnenolone is metabolized int ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
