Drug intelligence / Profile preview

talbutal

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Talbutal is a short to intermediate-acting barbiturate that acts as a nonselective central nervous system (CNS) depressant. It is capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma; at sufficiently high therapeutic doses it can induce anesthesia. Talbutal binds to a distinct site on the GABAA receptor associated with the chloride ion channel (Cl− ionopore), increasing the duration for which the channel remains open and thereby prolonging the inhibitory effect of GABA at postsynaptic thalamic neurons. It was primarily used as a sedative and hypnotic under the brand name Lotusate but has since been discontinued for these indications in many markets[1][2][3][4][6].

Brand names
Lotusate
Other names
5-allyl-5-sec-butylbarbituric acid5-(1-methylpropyl)-5-(2-propenyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
02

Targets

iGluR (Ionotropic receptor 76b (Ir76b))GABRR (GABA-A receptor subunit rho)Nicotinic Acetylcholine Receptor

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