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Azapirones are a class of drugs used as anxiolytics and antipsychotics. [1]

70 relations: Absorption (pharmacokinetics), Agonist, Alnespirone, Antidepressant, Antipsychotic, Anxiolytic, Augmentation (pharmacology), Azaspirodecanedione, Benzodiazepine, Binding selectivity, Binospirone, Buspirone, Chemical structure, Clinical trial, Cognitive deficit, Diarrhea, Dizziness, Dopamine receptor D2, Dopamine receptor D4, Drug, Drug tolerance, Enilospirone, Eptapirone, Excretion, Feces, Functional group, Generalized anxiety disorder, Gepirone, Half-life, Headache, Imipramine, Intrinsic activity, Inverse agonist, Ipsapirone, Japan, Liver, Major depressive disorder, Metabolism, Metabolite, Nausea, Onset of action, Paroxetine, Partial agonist, Perospirone, Pharmacology, Physical dependence, Pre-clinical development, Psychomotor agitation, Pyrimidinylpiperazine, Receptor (biochemistry), ..., Receptor antagonist, Revospirone, Schizophrenia, Sedation, Selective serotonin reuptake inhibitor, Side effect, Sigma receptor, Substance abuse, Substance use disorder, Tandospirone, Time release technology, Tiospirone, Umespirone, United States, Urine, Zalospirone, 5-HT1A receptor, 5-HT2A receptor, 5-HT2C receptor, 5-HT7 receptor. Expand index (20 more) »

Absorption (pharmacokinetics)

In pharmacology (and more specifically pharmacokinetics), absorption is the movement of a drug into the bloodstream.

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An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.

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Alnespirone (S-20,499) is a selective 5-HT1A receptor full agonist of the azapirone chemical class.

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Antidepressants are drugs used for the treatment of major depressive disorder and other conditions, including dysthymia, anxiety disorders, obsessive compulsive disorder, eating disorders, chronic pain, neuropathic pain and, in some cases, dysmenorrhoea, snoring, migraine, attention-deficit hyperactivity disorder (ADHD), addiction, dependence, and sleep disorders.

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Antipsychotics (also known as neuroleptics or major tranquilizers) are a class of psychiatric medication primarily used to manage psychosis (including delusions, hallucinations, or disordered thought), in particular in schizophrenia and bipolar disorder, and are increasingly being used in the management of non-psychotic disorders (ATC code N05A).

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An anxiolytic (also antipanic or antianxiety agent) is a medication or other intervention that inhibits anxiety.

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Augmentation (pharmacology)

Augmentation, in the context of the pharmacological management of Psychiatry, refers to the combination of two or more drugs to achieve better treatment results.

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Azaspirodecanedione is a chemical compound.

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Benzodiazepines (BZD), sometimes called "benzos", are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring.

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Binding selectivity

Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex.

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Binospirone (MDL-73,005-EF) is a drug which acts as a partial agonist at 5-HT1A somatodendritic autoreceptors but as an antagonist at postsynaptic 5-HT1A receptors.

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Buspirone, trade name Buspar, is an anxiolytic psychotropic drug of the azapirone chemical class.

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Chemical structure

A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid.

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Clinical trial

Clinical trials are experiments done in clinical research.

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Cognitive deficit

Cognitive deficit or cognitive impairment is an inclusive term to describe any characteristic that acts as a barrier to the cognition process.

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Diarrhea, also spelled diarrhoea, is the condition of having at least three loose or liquid bowel movements each day.

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Dizziness is an impairment in spatial perception and stability.

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Dopamine receptor D2

Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the DRD2 gene.

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Dopamine receptor D4

The dopamine receptor D4 is a G protein-coupled receptor encoded by the gene.

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A drug is, in the broadest of terms, a chemical substance that has known biological effects on humans or other animals.

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Drug tolerance

Drug tolerance is a pharmacology concept where a subject's reaction to a specific drug and concentration of the drug is reduced followed repeated use, requiring an increase in concentration to achieve the desired effect.

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Enilospirone (CERM-3,726) is a selective 5-HT1A receptor agonist of the azapirone class.

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Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family.

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Excretion is the process by which waste products of metabolism and other non-useful materials are eliminated from an organism.

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Feces (US) or faeces (UK), also known by many other names, is a solid waste product from an animal digestive tract, discharged through the anus or cloaca during a process called defecation.

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Functional group

In organic chemistry, functional groups are specific groups (moieties) of atoms or bonds within molecules that are responsible for the characteristic chemical reactions of those molecules.

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Generalized anxiety disorder

Generalized anxiety disorder (GAD) is an anxiety disorder characterized by excessive, uncontrollable and often irrational worry, that is, apprehensive expectation about events or activities.

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Gepirone (Ariza, Variza; BMY-13,805, ORG-13,011) is an antidepressant and anxiolytic of the azapirone class.

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Half-life (t1⁄2) is the amount of time required for the amount of something to fall to half its initial value.

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A headache or cephalalgia is pain anywhere in the region of the head or neck.

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Imipramine (G 22355), sold as Tofranil and also known as melipramine, is a tricyclic antidepressant (TCA) of the dibenzazepine group.

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Intrinsic activity

Intrinsic activity (IA) or efficacy refers to the relative ability of a drug-receptor complex to produce a maximum functional response.

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Inverse agonist

In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.

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Ipsapirone is a selective 5-HT1A receptor partial agonist of the piperazine and azapirone chemical classes.

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Japan (日本 Nippon or Nihon; formally or Nihon-koku, "State of Japan") is an island country in East Asia.

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The liver is a vital organ of vertebrates and some other animals.

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Major depressive disorder

Major depressive disorder (MDD) (also known as clinical depression, major depression, unipolar depression, or unipolar disorder; or as recurrent depression in the case of repeated episodes) is a mental disorder characterized by a pervasive and persistent low mood that is accompanied by low self-esteem and by a loss of interest or pleasure in normally enjoyable activities.

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Metabolism (from μεταβολή metabolē, "change") is the set of life-sustaining chemical transformations within the cells of living organisms.

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Metabolites are the intermediates and products of metabolism.

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Nausea (Latin nausea, from Greek ναυσία - nausia, "ναυτία" - nautia, motion sickness", "feeling sick or queasy") is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit.

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Onset of action

Onset of action is the duration of time it takes for a drug's effects to come to prominence upon administration.

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Paroxetine (also known by the trade name Paxil among others) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) type. Paroxetine is used to treat major depression, obsessive-compulsive disorder, panic disorder, social anxiety, posttraumatic stress disorder, generalized anxiety disorder and vasomotor symptoms (e.g. hot flashes and night sweats) associated with menopause in adult outpatients. Differences between newer antidepressants are usually fairly subtle and mostly confined to side effects. It shares the common side effects and contraindications of other SSRIs, with higher rates of nausea, sleepiness, sexual side effects, and weight gain. Discontinuing paroxetine is associated with a high risk of withdrawal syndrome. Paroxetine may be associated with a slightly increased risk of birth defects. Marketing of the drug began in 1992 by the pharmaceutical company SmithKline Beecham, now GlaxoSmithKline. Generic formulations have been available since 2003 when the patent expired.

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Partial agonist

In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist.

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Perospirone (Lullan) is an atypical antipsychotic of the azapirone family.

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Pharmacology (from Greek φάρμακον, pharmakon, "poison" in classic Greek; "drug" in modern Greek; and -λογία, -logia "study of", "knowledge of") is the branch of medicine and biology concerned with the study of drug action, where a drug can be broadly defined as any man-made, natural, or endogenous (from within body) molecule which exerts a biochemical and/or physiological effect on the cell, tissue, organ, or organism (sometimes the word pharmacon is used as a term to encompass these endogenous and exogenous bioactive species).

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Physical dependence

Physical dependence refers to a state resulting from chronic use of a drug that has produced tolerance and where negative physical symptoms of withdrawal result from abrupt discontinuation or dosage reduction.

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Pre-clinical development

In drug development, pre-clinical development, also named preclinical studies and nonclinical studies, is a stage of research that begins before clinical trials (testing in humans) can begin, and during which important feasibility, iterative testing and drug safety data is collected.

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Psychomotor agitation

Psychomotor agitation is a series of unintentional and purposeless motions that stem from mental tension and anxiety of an individual.

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1-(2-Pyrimidinyl)piperazine (1-PP, 1-PmP) is a chemical compound and piperazine derivative.

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Receptor (biochemistry)

In biochemistry and pharmacology, a receptor is a protein molecule usually found embedded within the plasma membrane surface of a cell that receives chemical signals from outside the cell.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens agonist-mediated responses rather than provoking a biological response itself upon binding to a receptor.

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Revospirone (Bay Vq 7813) is an azapirone drug which was patented as a veterinary tranquilizer but was never marketed.

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Schizophrenia is a mental disorder often characterized by abnormal social behavior and failure to recognize what is real.

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Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure.

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Selective serotonin reuptake inhibitor

Selective serotonin re-uptake inhibitors or serotonin-specific reuptake inhibitors (SSRIs) are a class of compounds typically used as antidepressants in the treatment of major depressive disorder and anxiety disorders.

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Side effect

In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug.

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Sigma receptor

Schematic σ receptor The sigma receptors σ1 and σ2 bind to ligands such as 4-PPBP, SA 4503, ditolylguanidine, dimethyltryptamine and siramesine.

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Substance abuse

Substance abuse, also known as drug abuse and substance use disorder, is a patterned use of a drug in which the user consumes the substance in amounts or with methods which are harmful to themselves or others, and is a form of substance-related disorder.

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Substance use disorder

Substance use disorder, also known as drug use disorder, is a condition in which the use of one or more substances leads to a clinically significant impairment or distress.

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Tandospirone (Sediel), also known as metanopirone, is an anxiolytic and antidepressant used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma.

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Time release technology

Time release technology (also known as sustained-release, extended-release, controlled-release, and other synonyms) is a mechanism used in pill tablets or capsules to dissolve a drug over time in order to be released slower and steadier into the bloodstream while having the advantage of being taken at less frequent intervals than immediate-release (IR) formulations of the same drug.

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Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an atypical antipsychotic of the azapirone class.

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Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties.

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United States

The United States of America (USA), commonly referred to as the United States (U.S.) or America, is a federal republic composed of 50 states, a federal district, five major territories and various possessions.

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Urine (from Latin Urina, ae, f.) is a liquid by-product of the body secreted by the kidneys through a process called urination (or micturition) and excreted through the urethra.

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Zalospirone (WY-47,846) is a selective 5-HT1A partial agonist of the azapirone chemical class.

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5-HT1A receptor

The 5-HT1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).

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5-HT2A receptor

The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR).

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5-HT2C receptor

The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).

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5-HT7 receptor

The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels.

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[1] https://en.wikipedia.org/wiki/Azapirone

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