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A common metabolite of several azapirones including buspirone, gepirone, ipsapirone, revospirone, and tandospirone is 1-(2-pyrimidinyl)piperazine (1-PP). [47] [48] [49] 1-PP possesses 5-HT 1A partial agonist and α 2-adrenergic antagonist actions and likely contributes overall mostly to side effects. [47] [48] [50]
Buspirone has also been found to bind with much higher affinity to the dopamine D 3 and D 4 receptors, where it is similarly an antagonist. [45] A major metabolite of buspirone, 1-(2-pyrimidinyl)piperazine (1-PP), occurs at higher circulating levels than buspirone itself and is known to act as a potent α 2-adrenergic receptor antagonist.
A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking the action of the serotonin transporter (SERT). This in turn leads to increased extracellular concentrations of serotonin and, therefore, an increase in serotonergic ...
Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. [1] It is uncommonly used in humans as an antipsychotic drug.
In the United States and Canada, clorazepate is available in 3.75, 7.5, and 15 mg capsules or tablets. In Europe, tablet formations are 5 mg, 10 mg, 20 mg and 50 mg. [6] Clorazepate SD (controlled release) is available and may have a reduced incidence of adverse effects. The sustained-release formulation of clorazepate has some advantages in ...
Tofisopam [3] (Emandaxin, Grandaxin, Sériel) is an anxiolytic that is marketed in several European countries. [4] Chemically, it is a 2,3-benzodiazepine. Unlike other anxiolytic benzodiazepines (which are generally 1,4- or 1,5-substituted) however, tofisopam does not have anticonvulsant, sedative, [5] skeletal muscle relaxant, motor skill-impairing or amnestic [6] properties.