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Azapirone

Index Azapirone

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

80 relations: Absorption (pharmacology), Adrenergic receptor, Agonist, Alnespirone, Alpha-1 adrenergic receptor, Alpha-2 adrenergic receptor, Animal testing on rodents, Antidepressant, Antipsychotic, Anxiolytic, Augmentation (pharmacology), Azaspirodecanedione, Benzodiazepine, Binding selectivity, Binding site, Binospirone, Buspirone, Chemical structure, Clinical trial, Cognitive deficit, Diarrhea, Dizziness, Dopamine receptor D1, Dopamine receptor D2, Dopamine receptor D4, Drug, Drug tolerance, Enilospirone, Eptapirone, Excretion, Feces, Functional gastrointestinal disorder, Functional group, Generalized anxiety disorder, Gepirone, Half-life, Headache, Imipramine, Intrinsic activity, Inverse agonist, Ipsapirone, Japan, Liver, Major depressive disorder, Metabolism, Metabolite, Modified-release dosage, Nausea, Onset of action, Panic disorder, ..., 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, Tiospirone, Umespirone, United States, Urine, Zalospirone, 5-HT1A receptor, 5-HT1B receptor, 5-HT1D receptor, 5-HT2A receptor, 5-HT2C receptor, 5-HT7 receptor. Expand index (30 more) »

Absorption (pharmacology)

In pharmacology (and more specifically pharmacokinetics), absorption is the movement of a drug from the site of administration to bloodstream.

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Adrenergic receptor

The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine (noradrenaline) and epinephrine (adrenaline).

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Agonist

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

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Alnespirone

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

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Alpha-1 adrenergic receptor

The alpha-1 (α1) adrenergic receptor is a G protein-coupled receptor (GPCR) associated with the Gq heterotrimeric G-protein.

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Alpha-2 adrenergic receptor

The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein.

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Animal testing on rodents

Rodents are commonly used in animal testing, particularly mice and rats, but also guinea pigs, hamsters, gerbils and others.

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Antidepressant

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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Antipsychotic

Antipsychotics, also known as neuroleptics or major tranquilizers, are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder.

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Anxiolytic

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

Azaspirodecanedione is a chemical compound.

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Benzodiazepine

Benzodiazepines (BZD, BZs), 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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Binding site

In biochemistry, a binding site is a region on a protein or piece of DNA or RNA to which ligands (specific molecules and/or ions) may form a chemical bond.

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Binospirone

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

Buspirone, sold under the brand name Buspar, is an anxiolytic drug that is primarily used to treat generalized anxiety disorder (GAD).

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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 or observations 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

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

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Dizziness

Dizziness is an impairment in spatial perception and stability.

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Dopamine receptor D1

Dopamine receptor D1, also known as DRD1, is a protein that in humans is encoded by the DRD1 gene.

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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 dopamine D2-like G protein-coupled receptor encoded by the gene on chromosome 11 at 11p15.5.

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Drug

A drug is any substance (other than food that provides nutritional support) that, when inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue causes a temporary physiological (and often psychological) change in the body.

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Drug tolerance

Drug tolerance is a pharmacological concept describing subjects' reduced reaction to a drug following its repeated use.

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Enilospirone

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

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Eptapirone

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

Excretion is the process by which metabolic waste is eliminated from an organism.

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Feces

Feces (or faeces) are the solid or semisolid remains of the food that could not be digested in the small intestine.

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Functional gastrointestinal disorder

Functional gastrointestinal disorders (FGID), also known as disorders of gut-brain interaction include a number of separate idiopathic disorders which affect different parts of the gastrointestinal tract and involve visceral hypersensitivity and impaired gastrointestinal motility.

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Functional group

In organic chemistry, functional groups are specific substituents or moieties 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

Gepirone is an antidepressant and anxiolytic drug of the azapirone group that was synthesized by Bristol-Myers Squibb in 1986 and has been under development for the treatment of depression but has yet to be marketed.

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Half-life

Half-life (symbol t1⁄2) is the time required for a quantity to reduce to half its initial value.

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Headache

Headache is the symptom of pain anywhere in the region of the head or neck.

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Imipramine

Imipramine, sold under the brand name Tofranil among others, is a tricyclic antidepressant (TCA) which is used mainly in the treatment of depression.

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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

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

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Japan

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

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Liver

The liver, an organ only found in vertebrates, detoxifies various metabolites, synthesizes proteins, and produces biochemicals necessary for digestion.

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Major depressive disorder

Major depressive disorder (MDD), also known simply as depression, is a mental disorder characterized by at least two weeks of low mood that is present across most situations.

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Metabolism

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

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Metabolite

A metabolite is the intermediate end product of metabolism.

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Modified-release dosage

Modified-release dosage is a mechanism that (in contrast to immediate-release dosage) delivers a drug with a delay after its administration (delayed-release dosage) or for a prolonged period of time (extended-release dosage) or to a specific target in the body (targeted-release dosage).

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Nausea

Nausea or queasiness is an unpleasant sense of unease, discomfort, and revulsion towards food.

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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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Panic disorder

Panic disorder is an anxiety disorder characterized by reoccurring unexpected panic attacks.

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Paroxetine

Paroxetine, also known by trade names including Paxil and Seroxat among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat major depressive disorder, obsessive-compulsive disorder, social anxiety disorder, panic disorder, posttraumatic stress disorder, generalized anxiety disorder and premenstrual dysphoric disorder. It has also been used in the treatment of hot flashes and night sweats associated with menopause. It has a similar tolerability profile to other SSRIs. The common side effects include drowsiness, dry mouth, loss of appetite, sweating, trouble sleeping and delayed ejaculation. It may also be associated with a slightly increased risk of birth defects. The rate of withdrawal symptoms in young people may be higher with paroxetine and venlafaxine than other SSRIs and SNRIs. Several studies have associated paroxetine with suicidal thinking and behavior in children and adolescents. Marketing of the drug began in 1992 by the pharmaceutical company SmithKline Beecham, known since 2000 as GlaxoSmithKline. Generic formulations have been available since 2003 when the patent expired. The United States Department of Justice fined GlaxoSmithKline $3 billion in 2012, including a sum for withholding data on paroxetine, unlawfully promoting it for under-18s and preparing an article, following one of its clinical trials, study 329, that misleadingly reported the drug was effective in treating adolescent depression.

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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

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

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Pharmacology

Pharmacology is the branch of 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 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 is a physical condition caused by chronic use of a tolerance forming drug, in which abrupt or gradual drug withdrawal causes unpleasant physical symptoms.

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Pre-clinical development

In drug development, preclinical 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 are collected.

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Psychomotor agitation

Psychomotor agitation is a set of signs and symptoms that stem from mental tension and anxiety.

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Pyrimidinylpiperazine

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 that receives chemical signals from outside a cell.

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Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist.

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Revospirone

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

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Schizophrenia

Schizophrenia is a mental disorder characterized by abnormal social behavior and failure to understand reality.

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Sedation

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 reuptake inhibitors (SSRIs) are a class of drugs that are 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 (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine.

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Substance abuse

Substance abuse, also known as drug abuse, 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

A substance use disorder (SUD), also known as a 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

Tandospirone (brand name Sediel) is an anxiolytic and antidepressant drug used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma.

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Tiospirone

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

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Umespirone

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 known as the United States (U.S.) or America, is a federal republic composed of 50 states, a federal district, five major self-governing territories, and various possessions.

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Urine

Urine is a liquid by-product of metabolism in humans and in many animals.

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Zalospirone

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

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5-HT1A receptor

The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor (5-HT receptor) that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT).

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5-HT1B receptor

5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the HTR1B gene.

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5-HT1D receptor

5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it.

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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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Azaspirones.

References

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

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