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Pipequaline
Pipequaline (International Nonproprietary Name, INN; development code PK-8165) is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic. Pipequaline acts as a non-selective GABAA receptor, GABAA receptor partial agonist. While its profile of anxiolytic effects without sedation would appear to have potential medical applications, pipequaline has never been developed for medical use and is currently only used in scientific research. See also * Indalpine * Viqualine References {{GABAAR PAMs Anxiolytics GABAA receptor positive allosteric modulators 4-Piperidinyl compounds Quinolines Sedatives ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonbenzodiazepine
Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive, depressant, sedative, hypnotic, anxiolytic drugs that are benzodiazepine-like in uses, such as for treating insomnia and anxiety. Nonbenzodiazepine pharmacodynamics are similar in mechanism of action to benzodiazepine drugs, acting as GABAA receptor positive allosteric modulator, GABAA receptor positive allosteric modulators of the benzodiazepine receptor, benzodiazepine site, and therefore exhibit similar benefits, side effects, and risks. However, nonbenzodiazepines have dissimilar or entirely different chemical structures, so are unrelated to benzodiazepines on a molecular level. Background Nonbenzodiazepines have demonstrated efficacy in treating sleep disorders. There is some limited evidence that suggests that drug tolerance, tolerance to nonbenzodiazepines is slower to develop than with benzodiazepines. However, data is limit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Viqualine
Viqualine (INN; developmental code PK-5078) is an antidepressant and anxiolytic drug that was never marketed. It acts as a potent and selective serotonin releasing agent (SRA) and serotonin reuptake inhibitor (SRI) similarly to ''para''-chloroamphetamine (PCA). In addition, viqualine displaces diazepam from the GABAA receptor and produces benzodiazepine-like effects, indicating that it is also a positive allosteric modulator of the benzodiazepine site of the GABAA receptor. The drug has mainly been researched as a potential treatment for alcoholism. See also * Indalpine * Pipequaline Pipequaline (International Nonproprietary Name, INN; development code PK-8165) is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar ... References Antidepressants Anxiolytics GABAA receptor positive allosteric modulators Phenol ethers Piperidines Quinolines Seroto ... [...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 (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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor Positive Allosteric Modulators
In pharmacology, GABAA receptor positive allosteric modulators, also known as GABAkines or GABAA receptor potentiators, are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor, GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it Agonist, triggers the GABAA receptor to open its GABAA receptor#Structure and function, chloride channel to allow Chloride, chloride ions into the neuron, making the cell Hyperpolarization (biology), hyperpolarized and less likely to Action potential, fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABA receptor agonist, GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-aminobutyric acid (GABA) neurotransmitter molecule: they affect the r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indalpine
Indalpine, sold under the brand name Upstène, is a selective serotonin reuptake inhibitor (SSRI) that was briefly marketed as an antidepressant for treatment of depression. It was marketed in France and a few other European countries. Indalpine is a selective serotonin reuptake inhibitor (SSRI) and antihistamine. Indalpine was invented by 1977 and was introduced for medical use in France in 1983. Two years later, in 1985, it was withdrawn from the market due to toxicity. Indalpine has sometimes been said to be the first SSRI. However, it was preceded by the SSRI zimelidine (Zelmid), which was invented in 1969 and was introduced to the market in 1981 (then similarly withdrawn due to toxicity in 1983). Pharmacology Pharmacodynamics Indalpine is a selective serotonin reuptake inhibitor (SSRI) and antihistamine. Chemistry Indalpine is an indole and is structurally similar to tryptamines but is not a tryptamine itself. Synthesis : Metalation of indole (1) using methyl magn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (biochemistry), ligands which display both agonistic and Receptor antagonist, antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anticonvulsant
Anticonvulsants (also known as antiepileptic drugs, antiseizure drugs, or anti-seizure medications (ASM)) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also used in the treatment of bipolar disorder and borderline personality disorder, since many seem to act as mood stabilizers, and for the treatment of neuropathic pain. Anticonvulsants suppress the uncontrolled and excessive firing of neurons during seizures and in doing so can also prevent the spread of the seizure within the brain. Conventional antiepileptic drugs have diverse mechanisms of action but many block sodium channels or enhance γ-aminobutyric acid ( GABA) function. Several antiepileptic drugs have multiple or uncertain mechanisms of action. Next to voltage-gated sodium channels and components of the GABA system, their targets include GABAA receptors, the GABA transporter type 1, and GABA transaminase. Additional targets include voltage-gate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
