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Halaman 1 / 2Alcohol use disorder is responsible for a large worldwide burden of morbidity, premature mortality, and economic consequences resulting from accidents, violence, incarceration, decreased productivity, and increased healthcare spending.[A229073] Acamprosate…
Amfecloral is a stimulant drug of the phenethylamine and amphetamine chemical classes. For a short period of time, it was available under the brand Acutran and indicated as an appetite suppressant, but this product no longer exists. It acts as a prodrug which…
Atagabalin has been used in trials studying the treatment of Insomnia, Primary Insomnia, and Nonrestorative Sleep.
AZD7325 is a high affinity, selective modulator of the GABAA receptor system. [L2936]
Baclofen is a gamma-aminobutyric acid (GABA) agonist used as a skeletal muscle relaxant. Although originally designed in 1962 to treat epilepsy, baclofen was not effective in treating this condition but instead was shown to reduce spasticity in selected patie…
Bicuculline is a light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.
Cannabidiol, or CBD, is one of at least 85 active cannabinoids identified within the Cannabis plant. It is a major phytocannabinoid, accounting for up to 40% of the Cannabis plant's extract, that binds to a wide variety of physiological targets of the endocan…
Cenobamate, or YKP-3089, is an antiepileptic drug developed by SK Pharmaceuticals and used to treat partial onset seizures.[A188442,L10653] The exact mechanism of action has not been described in the literature, though it positively modulates GABA<sub>A</sub>…
Citalopram is an antidepressant belonging to the class of selective _serotonin-reuptake inhibitors_ (SSRIs) widely used to treat the symptoms of depression. It is a racemic bicyclic phthalate derivate and is the only compound with a tertiary amine and 2 nitro…
Clobazam belongs to the 1,5-benzodiazepine class of drugs and is marketed under different names, Onfi, Frisium, Urbanyl, and others.[A256868]. Clobazam was first synthesized in 1966 and first published in 1969, following the incidental synthesis and discovery…
Clomethiazole is a well-established ?-aminobutyric acid (GABAA)-mimetic drug. It is a sedative and hypnotic that is widely used in treating and preventing symptoms of acute alcohol withdrawal. It is a drug which is structurally related to thiamine (vitamin B1…
Clorazepic acid (clorazepate) is a water-soluble benzodiazepine with muscle-relaxant and anticonvulsant actions effective in the treatment of anxiety.[A957,L44788] Following administration, clorazepate is rapidly converted to nordiazepam (N-desmethyldiazepam)…
Crisugabalin is under investigation in clinical trial NCT06490484 (Efficacy and Safety of HSK16149 Capsule in Chinese Patients With Diabetic Peripheral Neuropathic Pain Who Had an Inadequate Response to Pregabalin).
Daridorexant, formerly known as nemorexant, is a selective dual orexin receptor antagonist used to treat insomnia. Insomnia is characterized by difficulties with sleep onset and/or sleep maintenance and impairment of daytime functioning. It chronically affect…
Darigabat is under investigation in clinical trial NCT05941442 (A Study to Evaluate Efficacy, Safety, and Tolerability of Darigabat in Participants With Panic Disorder).
Deramciclane (EGIS-3886) is used for the treatment of a number of anxiety disorders. Deramciclane differs from other anti anxiety medications in that it is not a benzodiazepine and so has a different structure and target. It antagonizes 5-HT2A receptors, agon…
Difelikefalin (CR845) is an agonist of kappa opioid receptors (KORs) useful in the treatment of pruritus secondary to chronic kidney disease. KORs were first associated with itching in 1984.[A237610] Further investigations revealed that dynorphins, endogenous…
Etizolam is a thienodiazepine which is chemically related to benzodiazepine (BDZ) drug class; it differs from BDZs in having a benzene ring replaced with a thiophene ring. It is an agonist at GABA-A receptors and possesses amnesic, anxiolytic, anticonvulsant,…
EVT 201 is a novel partial positive allosteric modulator of the GABAA receptor complex which is being developed as a treatment for insomnia. It is being developed by Evotec Inc.
Felbamate is an anticonvulsant drug used in the treatment of epilepsy. In particular, in the adult patient population, it can be employed to treat partial seizures (with and without generalization). Alternatively, it is used to treat partial and generalized s…
Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benz…
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Gabapentin is a structural analogue of the inhibitory neurotransmitter gamma-aminobutyric acid ([GABA]) that was first approved for use in the United States in 1993.[L8717] It was originally developed as a novel anti-epileptic for the treatment of certain typ…
Gabapentin enacarbil is marketed under the name Horizant. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Gaboxadol also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) is an experimental sleep aid drug developed by Lundbeck and Merck, who reported increased deep sleep without the reinforcing effects of benzodiazepines. Development of Gaboxadol was…
The most common inhibitory neurotransmitter in the central nervous system.
Ganaxolone is the 3?-methylated synthetic analog of [allopregnanolone],[L41130] a metabolite of [progesterone].[A3197] Ganaxolone belongs to a class of compounds referred to as neurosteroids.[A3197] Endogenous neurosteroids, which comprise certain metabolites…
Guvacine is a pyridine alkaloid found in the Areca nut (also known as the Betel nut). It is an experimental drug with no approved indication. Experimental studies are still being investigated to determine all of the physiological effects and mechanisms of act…
Hopantenic acid (Pantogam) is a central nervous system depressant. Hopantenic acid has a unique spectrum of pharmacological effects (nootropic, anticonvulsant, mild activating) in the absence of addiction, hyperstimulation or withdrawal syndrome. [A33115]
Imagabalin has been investigated in Generalized Anxiety Disorder.
Lemborexant is a novel dual orexin receptor antagonist used in the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.[L10863] Recent research in the field of sleep disorders has revealed that insomnia is likely driv…
Loprazolam is an imidazobenzodiazepine with anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. It is indicated for the short-term treatment of insomnia including difficulty in falling asleep and/or frequent nocturnal awake…
Mirogabalin has been used in trials studying the treatment of Post-herpetic Neuralgia, Pain Associated With Fibromyalgia, and Diabetic peripheral neuropathic pain.
Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, w…
MRK-409 is a GABA-A receptor agonist [A31972].
NLX-P101, gene therapy is developed by Neurologix to treat Parkinson’s disease. The gene is glutamic acid decarboxylase (GAD), whose product synthesizes the major inhibitory neurotransmitter in the brain, (gamma)-aminobutyric acid (GABA), and targets the subt…
Pentetrazol, also known as pentylenetetrazole, is a gamma-aminobutyric acid type A (GABA<sub>A</sub>) receptor antagonist that was approved by the FDA until 1982.[A254437]
Phenazepam is under investigation in clinical trial NCT03017430 (Pregabalin for Opiate Withdrawal Syndrome).
A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the gamma-aminobutyric acid-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poison…
Piracetam is a nootropic drug in the racetams group, with chemical name 2-oxo-1-pyrrolidine acetamide. It shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid and is a cyclic derivative of the neurotransmitter ?-aminobutyric acid (GABA). Ho…
Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter.[A173995] It may be used to manage neuropathic pain, postherpetic neuralgia, and fibromyalgia among other conditions.[A187190] Although as per the FDA Label …
Progabide is an analog and prodrug of gamma-aminobutyric acid. It is commonly used in the treatment of epilepsy. It has agonistic activity for both the GABAA and GABAB receptors. In clinical trials, progabide has been investigated for Parkinson's disease, sch…
Pyridoxine is the 4-methanol form of vitamin B6, an important water-soluble vitamin that is naturally present in many foods. As its classification as a vitamin implies, Vitamin B6 (and pyridoxine) are essential nutrients required for normal functioning of man…
Quazepam is a trifluoroethyl benzodiazepine derivative. It was first approved in the US in 1985 and is used as a hypnotic for the treatment of insomnia.[L44913] It appears to be unique amongst other benzodiazepine derivatives in its relatively high affinit…
Sodium oxybate (Xyrem) is a central nervous system (CNS) depressant used to treat cataplexy or excessive daytime sleepiness associated with narcolepsy.[L30598] It is a sodium salt of [gamma-Hydroxybutyric acid], an endogenous cerebral inhibitory neurotransmit…
Temazepam, like many other similar and related benzodiazepines, acts as a gamma-aminobutyric acid (GABA) modulator and is capable of eliciting a variety of actions including sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolyt…
Tiagabine is an anti-convulsive medication. It is also used in the treatment for panic disorder as are a few other anticonvulsants. Though the exact mechanism by which tiagabine exerts its effect on the human body is unknown, it does appear to operate as a se…
TPMPA ((1,2,5,6-tetrahydropyridine-4-yl)methylphosphinic acid) is a selective antagonist of GABA<sub>C</sub> receptors (also known as GABA-? or GABA<sub>A-?</sub> receptors).[A245303] GABA<sub>C</sub> receptors are found primarily in the retina, although they…
Vigabatrin is an analog of gamma-aminobutyric acid ([GABA]), the main inhibitory neurotransmitter in the central nervous system, used in the treatment of refractory seizures and infantile spasms.[L13616] It irreversibly inhibits the enzyme responsible for GAB…