FG-5893
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FG-5893
FG-5893 is a chemical from the diphenylbutylpiperazine class of agents. It is a 5-HT1A agonist and a 5-HT2A antagonist. It is believed to be an anxiolytic agent with potential uses in the treatment of substance abuse disorders particularly alcoholism. There is evidence for FG-5893 behaving as a SNDRI: CNS review: See also * Amperozide * FG5865 References Alcohol abuse Alcohol and health Anxiolytics An anxiolytic (; also antipanic or anti-anxiety 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 anxie ... Anxiety disorder treatment 5-HT1A agonists Piperazines Methyl esters Pyridines 4-Fluorophenyl compounds {{anxiolytic-stub ...
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Diphenylbutylpiperazine
Diphenylbutylpiperidines are a class of typical antipsychotic drugs which were all synthesized, developed, and marketed by Janssen Pharmaceutica. They include: * Clopimozide (R-29,764) * Fluspirilene (Redeptin) * Penfluridol (Semap, Micefal, Longoperidol) * Pimozide (Orap) A closely related antipsychotic, amperozide, has an additional nitrogen atom in the heterocyclic ring and is classified as a diphenylbutylpiperazine. Other diphenylbutylpiperazines include Lidoflazine, PR-000608, FG5865, FG-5893 FG-5893 is a chemical from the diphenylbutylpiperazine class of agents. It is a 5-HT1A agonist and a 5-HT2A antagonist. It is believed to be an anxiolytic agent with potential uses in the treatment of substance abuse disorders particularly a ... and Mioflazine. References {{Chemical classes of psychoactive drugs Chemical classes of psychoactive drugs ...
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Amperozide
Amperozide is an atypical antipsychotic of the diphenylbutylpiperazine class which acts as an antagonist at the 5-HT2A receptor. It does not block dopamine receptors as with most antipsychotic drugs, but does inhibit dopamine release, and alters the firing pattern of dopaminergic neurons. It was investigated for the treatment of schizophrenia in humans, but never adopted clinically. Its main use is instead in veterinary medicine, primarily in intensively farmed pigs, for decreasing aggression and stress and thereby increasing feeding and productivity. See also *FG-5893 FG-5893 is a chemical from the diphenylbutylpiperazine class of agents. It is a 5-HT1A agonist and a 5-HT2A antagonist. It is believed to be an anxiolytic agent with potential uses in the treatment of substance abuse disorders particularly a ... References 5-HT2A antagonists Piperazines Ureas 4-Fluorophenyl compounds {{nervous-system-drug-stub ...
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FG5865
FG5865 is from the diphenylbutylpiperazine class of agents. It is a 5-HT1A agonist and a 5-HT2A antagonist. It is believed to be an anxiolytic agent with treatment in substance abuse disorders particularly alcoholism. There is evidence to suggest that FG5865 is a SNDRI. See also *Amperozide *FG-5893 References Alcohol abuse Alcohol and health Anxiolytics An anxiolytic (; also antipanic or anti-anxiety 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 anxie ... Anxiety disorder treatment 5-HT1A agonists Piperazines Disubstituted pyridines 4-Fluorophenyl compounds Amides {{Organic-compound-stub ...
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5-HT2A
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and functions as a G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades. Like all 5-HT2 receptors, the 5-HT2A receptor is coupled to the Gq/G11 signaling pathway. It is the primary excitatory receptor subtype among the serotonin-responsive GPCRs. The 5-HT2A receptor was initially noted for its central role as the primary target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. It later regained research prominence when found to mediate, at least in part, the effects of many antipsychotic drugs, particularly atypical antipsychotics. Downregulation of post-synaptic 5-HT2A receptors is an adaptive response triggered by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Elevated 5-HT2A receptor density has been observed in suicidal an ...
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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. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves
." '' GlaxoWellcome.'' Retrieved on December 6, 2007.
They are sometimes called blockers; examples include alpha blockers, beta b ...
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Anxiolytic
An anxiolytic (; also antipanic or anti-anxiety 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 response. 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. Those with anxiety disorders may have concurrent psychological disorders, such as depression. Anxiety disorders are classified using six possible clinical assessments: Different types of anxiety disorders will share some general symptoms while having their own distinctive symptoms. This explains why people with different types of anxiety disorders will respond differently to diffe ...
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Substance Abuse Disorder
Substance use disorder (SUD) is the persistent use of drugs despite substantial harm and adverse consequences to self and others. Related terms include ''substance use problems'' and ''problematic drug or alcohol use''. Along with substance-induced disorders (SID) they are encompassed in the category substance-related disorders. Substance use disorders vary with regard to the average age of onset. It is not uncommon for those who have SUD to also have other mental health disorders. Substance use disorders are characterized by an array of mental, emotional, physical, and behavioral problems such as chronic guilt; an inability to reduce or stop consuming the substance(s) despite repeated attempts; operating vehicles while intoxicated; and physiological withdrawal symptoms. Drug classes that are commonly involved in SUD include: alcohol (alcoholism); cannabis; opioids; stimulants such as nicotine (including tobacco), cocaine and amphetamines; benzodiazepines; barbiturates; and o ...
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Alcoholism
Alcoholism is the continued drinking of alcohol despite it causing problems. Some definitions require evidence of dependence and withdrawal. Problematic use of alcohol has been mentioned in the earliest historical records. The World Health Organization (WHO) estimated there were 283 million people with alcohol use disorders worldwide . The term ''alcoholism'' was first coined in 1852, but ''alcoholism'' and ''alcoholic'' are considered stigmatizing and likely to discourage seeking treatment, so diagnostic terms such as ''alcohol use disorder'' and ''alcohol dependence'' are often used instead in a clinical context. Alcohol is addictive, and heavy long-term alcohol use results in many negative health and social consequences. It can damage all the organ systems, but especially affects the brain, heart, liver, pancreas, and immune system. Heavy alcohol usage can result in trouble sleeping, and severe cognitive issues like dementia, brain damage, or Wernicke–Kors ...
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Receptor Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive."


Types of agonists

Receptors can be activated by either endogenous agonists (such as

5-HT1A
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarization and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neuromodulation 5-HT1A receptor a ...
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Alcohol Abuse
Alcohol abuse encompasses a spectrum of alcohol-related substance abuse. This spectrum can range from being mild, moderate, or severe. This can look like consumption of more than 2 drinks per day on average for men, or more than 1 drink per day on average for women, to binge drinking. Alcohol abuse was a psychiatric diagnosis in the DSM-IV, but it has been merged with alcohol dependence in the DSM-5 into alcohol use disorder. Alcohol use disorder, also known as AUD, shares similar conditions that some people refer to as alcohol abuse, alcohol dependence, alcohol addiction, and the most used term, alcoholism. Globally, excessive alcohol consumption is the seventh leading risk factor for both death and the burden of disease and injury, representing 5.1% of the total global burden of disease and injury, measured in disability-adjusted life years (DALYs). After tobacco, alcohol accounts for a higher burden of disease than any other drug. Alcohol use is a major cause of preve ...
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