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Index Gabapentinoid

Gabapentinoids, also known as α2δ ligands, are a class of drugs that are derivatives of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) (i.e., GABA analogues) which block α2δ subunit-containing voltage-dependent calcium channels (VDCCs). [1]

11 relations: CACNA2D1, Calcium channel blocker, GABA analogue, Gabapentin, Gabapentin enacarbil, Hypnotic, Imagabalin, Mirogabalin, Phenibut, Pregabalin, Voltage-gated calcium channel.


Voltage-dependent calcium channel subunit alpha-2/delta-1 is a protein that in humans is encoded by the CACNA2D1 gene.

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Calcium channel blocker

Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are several medications that disrupt the movement of calcium through calcium channels.

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GABA analogue

A GABA analogue is a compound which is an analogue or derivative of the neurotransmitter gamma-Aminobutyric acid (GABA) (the IUPAC of which is 4-aminobutanoic acid).

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Gabapentin, sold under the brand name Neurontin among others, is a medication which is used to treat epilepsy (specifically partial seizures), neuropathic pain, hot flashes, and restless legs syndrome.

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Gabapentin enacarbil

Gabapentin enacarbil (Horizant, Regnite (in Japan)) is an anticonvulsant and analgesic drug of the gabapentinoid class, and a prodrug to gabapentin.

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Hypnotic (from Greek Hypnos, sleep) or soporific drugs, commonly known as sleeping pills, are a class of psychoactive drugs whose primary function is to induce sleep and to be used in the treatment of insomnia (sleeplessness), or surgical anesthesia.

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Imagabalin (INN, USAN; PD-332,334) is a drug which acts as a ligand for the α2δ subunit of the voltage-dependent calcium channel, with some selectivity for the α2δ1 subunit over α2δ2.

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Mirogabalin (developmental code name DS-5565) is a drug developed by Daiichi Sankyo, a gabapentinoid.

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Phenibut, sold under the brand names Anvifen, Fenibut, and Noofen among others, is a central nervous system depressant with anxiolytic and sedative effects which is used in the treatment of anxiety, insomnia, and for a variety of other indications.

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Pregabalin, marketed under the brand name Lyrica among others, is a medication used to treat epilepsy, neuropathic pain, fibromyalgia, and generalized anxiety disorder.

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Voltage-gated calcium channel

Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (e.g., muscle, glial cells, neurons, etc.) with a permeability to the calcium ion Ca2+.

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Gabapentanoid, Gabapentanoids, Gabapentinoids.


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

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