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Imidazopyridine
An imidazopyridine is a nitrogen containing heterocycle that is also a class of medication, drugs that contain this same chemical substructure. In general, they are GABAA receptor, GABAA receptor receptor_agonist, agonists, however recently proton pump inhibitors, aromatase inhibitors, NSAIDs and other classes of drugs in this class have been developed as well. Despite usually being similar to them in effect, they are not chemically related to benzodiazepines. As such, GABAA-agonizing imidazopyridines, pyrazolopyrimidines, and cyclopyrrones are sometimes grouped together and referred to as "nonbenzodiazepines." Imidazopyridines include: Sedatives Anxiolytics, sedatives and hypnotics (GABAA receptor positive allosteric modulator, GABAA receptor positive allosteric modulators): * Imidazo[1,2-a]pyridines: ** Alpidem (original brand name Ananxyl)—an anxiolytic that was withdrawn from the market worldwide in 1995 due to hepatotoxicity. ** DS-1 (drug), DS-1—a GABAA receptor, GABAA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpidem
Alpidem, sold under the brand name Ananxyl, is a nonbenzodiazepine anxiolytic medication which was briefly used to treat anxiety disorders but is no longer marketed. It was previously marketed in France, but was list of withdrawn drugs, discontinued due to liver toxicity. Alpidem is taken oral administration, by mouth. Side effects of alpidem include sedation, fatigue (medical), fatigue, dizziness, and headache, among others. It has much less to no impact on cognition, memory, and Psychomotor agitation, psychomotor function relative to benzodiazepines. Similarly, no rebound effect, rebound anxiety or withdrawal symptoms have been observed with alpidem. Rarely, alpidem can cause serious liver toxicity, including liver failure and death. Alpidem is a nonbenzodiazepine of the imidazopyridine family, chemical structure, structurally related to the Z-drug zolpidem, and acts as a GABAA receptor positive allosteric modulator, GABAA receptor positive allosteric modulator of the benzodia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zolpidem
Zolpidem, sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and after behavioral changes, such as sleep hygiene, have been tried. It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer. It is taken by mouth and is available as conventional tablets, extended-release tablets, or sublingual tablets. Common side effects include daytime sleepiness, headache, nausea, and diarrhea. More severe side effects include memory problems and hallucinations. While flumazenil, a GABAA receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose. Zolpidem is a nonbenzodiazepine, or Z-drug, which acts as a sedative and hypnotic as a positive allosteric modulator at the GABAA receptor. It is an imidazopyrid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrazolopyrimidine
Pyrazolopyrimidines are a series of isomeric heterocyclic chemical compounds with the molecular formula C6H5N3. They form the central core of a variety of more complex chemical compounds including some pharmaceuticals and pesticides. Pharmaceuticals One isomer of pyrazolopyrimidines, known as pyrazolo ,5-''a''yrimidine, is the basis for a class of sedative and anxiolytic drugs related (in terms of their effect) to benzodiazepines. Most of the drugs from this class marketed to date are intended to induce sleep, and are prescribed for people suffering insomnia, however some newer compounds produce anxiolytic effects with relatively little sedation, and are being developed for use as non-sedating anti-anxiety drugs. They include: * Zaleplon - hypnotic (trade name Sonata) * Indiplon - hypnotic * Ocinaplon - anxiolytic * Lorediplon - hypnotic As they are not chemically related to the benzodiazepines despite their similar effect, such drugs—as well as the imidazopyridines and c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DS-1 (drug)
DS-1 is a drug from the imidazopyridine family, which is the first drug developed that acts as a GABAA receptor positive allosteric modulator (PAM) selective for the α4 β3 δ subtype, which is not targeted by other GABAA receptor PAMs such as the benzodiazepines or other nonbenzodiazepine drugs. Novel selective drugs such as DS-1 are useful in the study of this receptor subtype. See also * Alpidem * Saripidem * Zolpidem Zolpidem, sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and after beh ... References Benzamides 4-Chlorophenyl compounds GABAA receptor positive allosteric modulators Imidazopyridines Bromoarenes Thiophenes {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Necopidem
Necopidem is a drug in the imidazopyridine family, which is related to the better known drugs zolpidem and alpidem. It is therefore considered a nonbenzodiazepine and as such may have sedative and 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 anxie ... effects, given its structural similarity to other nonbenzodiazepine hypnotics. References Carboxamides GABAA receptor positive allosteric modulators Imidazopyridines Sedatives {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Proton Pump Inhibitors
Proton-pump inhibitors (PPIs) are a class of medications that cause a profound and prolonged reduction of gastric acid, stomach acid production. They do so by irreversibly inhibiting the stomach's H+/K+ ATPase, H+/K+ ATPase proton pump. The body eventually synthesizes new proton pumps to replace the irreversibly inhibited ones, a process driven by normal cellular turnover, which gradually restores acid production. Proton-pump inhibitors have largely superseded the H2-receptor antagonist, H2-receptor antagonists, a group of medications with similar effects but a different mode of action, and heavy use of antacids. A potassium-competitive acid blocker (PCAB) revaprazan was marketed in Korea as an alternative to a PPI. A newer PCAB vonoprazan with a faster and longer lasting action than revaprazan, and PPIs has been marketed in Japan (2013), Russia (2021), and the US (2023). PPIs are among the most widely sold medications in the world. The class of proton-pump inhibitor medication ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Saripidem
Saripidem is a sedative and anxiolytic drug in the imidazopyridine family, which is related to the better known drugs zolpidem and alpidem. Saripidem has a similar pharmacological profile to the benzodiazepine family of drugs including sedative and anxiolytic properties, but its chemical structure is quite different from that of the benzodiazepine drugs, and saripidem is described as a nonbenzodiazepine. The mechanism of action by which saripidem produces its sedative and anxiolytic effects is by modulating the benzodiazepine binding site on GABAA receptors, however unlike many older GABAA agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...s, saripidem is highly subtype selective and binds primarily to the ω1 subtype. References {{GABAAR PAMs Carboxamides 4-Chl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABRD
Gamma-aminobutyric acid receptor subunit delta is a protein that in humans is encoded by the ''GABRD'' gene. In the mammalian brain, the delta (δ) subunit forms specific GABAA receptor subtypes by co-assembly leading to δ subunit containing GABAA receptors (δ-GABAA receptors). Function The delta (δ) subunit, one of the subunits of the hetero-pentameric δ-GABAA receptors, is a determinant subunit for the specific cellular localization of δ-GABAA receptors, which are modulated by the GABA. GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts on the repertoire of GABAA receptors, the ligand-gated chloride channels. It is assembled from a diverse subunit pool, including assemblies from a family of 19 subunits (α1-α6, β1-β3, γ1-γ3, δ, ∈, θ, π and ρ1-ρ3). The GABRD gene encodes the delta (δ) subunit. Specifically, the δ-subunit is usually expressed in GABAA receptors associated with extrasynaptic activity, mediating tonic inhibition ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or Psychomotor agitation, excitement. They are central nervous system (CNS) Depressant, depressants and interact with brain activity, causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter Gamma-Aminobutyric acid, gamma-aminobutyric acid (GABA). Most sedatives produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or Anxiolytic, relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness), they are often referred to collectively as ''sedative–hypnotic'' drugs. Terminology There is some overlap ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Core Structure Of Imidazopyridines
Core or cores may refer to: Science and technology * Core (anatomy), everything except the appendages * Core (laboratory), a highly specialized shared research resource * Core (manufacturing), used in casting and molding * Core (optical fiber), the signal-carrying portion of an optical fiber * Core, the central part of a fruit * Hydrophobic core, the interior zone of a protein * Nuclear reactor core, a portion containing the fuel components * Pit (nuclear weapon) or core, the fissile material in a nuclear weapon * Semiconductor intellectual property core (IP core), is a unit of design in ASIC/FPGA electronics and IC manufacturing * Atomic core, an atom with no valence electrons * Lithic core, in archaeology, a stone artifact left over from toolmaking Geology and astrophysics * Core sample, in Earth science, a sample obtained by coring ** Ice core * Core, the central part of a galaxy; see Mass deficit * Core (anticline), the central part of an anticline or syncline * Planetary ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TP-003
TP-003 is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. TP-003 is a positive allosteric modulator at the benzodiazepine binding site of GABAA receptors. It possesses relative selectivity for benzodiazepine sites on α3-containing GABAA receptors, which are thought to contribute to the anxiolytic effects of benzodiazepines (in tandem with those containing α2 subunits). It has modest anticonvulsant activity although less than that of diazepam. See also * Imidazopyridine * L-838,417 * Alpidem Alpidem, sold under the brand name Ananxyl, is a nonbenzodiazepine anxiolytic medication which was briefly used to treat anxiety disorders but is no longer marketed. It was previously marketed in France, but was list of withdrawn drugs, disconti ... References Tertiary alcohols Anxiolytics GABAA rece ... [...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] |
