SL651498 is an anxiolytic and

anticonvulsant Anticonvulsants (also known as antiepileptic drugs or recently as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of b ...

drug used in scientific research, with a chemical structure most closely related to

β-carboline β-Carboline (9''H''- pyrido ,4-''b'' ndole) represents the basic chemical structure for more than one hundred alkaloids and synthetic compounds. The effects of these substances depend on their respective substituent. Natural β-carbolines prima ...

derivatives such as abecarnil and gedocarnil. It has similar effects to

benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...

drugs, but is structurally distinct and so is classed as a

nonbenzodiazepine Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive drugs that are very benzodiazepine-like in nature. They are used in the treatment of sleep proble ...

anxiolytic. SL651498 is a subtype-selective GABA_A agonist, which acts as a

full 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 ago ...

at α₂ and α₃ subtypes, and as a

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

at α₁ and α₅ (although its action at α₅ subtypes is much weaker than at the others). In animal studies, it has primarily anxiolytic effects, although some

sedation Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure. Examples of drugs which can be used for sedation include isoflurane, diethyl ether, ...

ataxia Ataxia is a neurological sign consisting of lack of voluntary coordination of muscle movements that can include gait abnormality, speech changes, and abnormalities in eye movements. Ataxia is a clinical manifestation indicating dysfunction of ...

and muscle relaxant effects are observed at higher doses. It substitutes fully for the anxiolytic benzodiazepine chlordiazepoxide, but only partially substituted for the

imidazopyridine An imidazopyridine is a nitrogen containing heterocycle that is also a class of drugs that contain this same chemical substructure. In general, they are GABAA receptor agonists, however recently proton pump inhibitors, aromatase inhibitors, NSAI ...

hypnotic drug zolpidem and the benzodiazepine

hypnotic Hypnotic (from Greek ''Hypnos'', sleep), or soporific drugs, commonly known as sleeping pills, are a class of (and umbrella term for) psychoactive drugs whose primary function is to induce sleep (or surgical anesthesiaWhen used in anesthesia ...

triazolam. When given repeatedly it failed to produce tolerance or dependence, probably due to its low affinity and efficacy at the α₅ subtype. SL651498 has been suggested for development as a novel non-sedating anxiolytic drug for humans, although it is still only at an early stage of research. Preliminary human trials suggest similar efficacy to

lorazepam Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication. It is used to treat anxiety disorders, trouble sleeping, severe agitation, active seizures including status epilepticus, alcohol withdrawal, and c ...

as an anxiolytic, but with little or no sedation or impairment of memory, motor skills or cognitive function. There are other possibly anxioselective compounds in development, such as

L-838,417 L-838,417 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. The compound was developed by Merck, Sharp and Dohme ...

NGD 91-3 NGD may refer to * Project 18, India's Next Generation Destroyer * New Guinea Dingo, New Guinea Singing Dog * Non-Good Delivery gold or silver bars * NGD Studios, a game development company * NGD-4715, a drug * New Gibraltar Democracy, a poli ...

References

{{GABAAR PAMs Anxiolytics Beta-Carbolines Pyrrolidines Fluoroarenes Lactams Carboxamides GABAA receptor positive allosteric modulators