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In addition to aripiprazole's partial agonism and functional selectivity characteristics, its effectiveness may be mediated by its very high dopamine D 2 receptor occupancy (approximately 31%, 44%, 75%, 80%, and 95% at daily dosages of 0.5 mg, 2 mg, 10 mg, 30mg and 40 mg respectively) [87] [88] Aripiprazole has been characterized as possessing ...
Aripiprazole (Abilify) – dopamine D 2 and D 3 partial agonist, serotonin 5-HT 1A and 5-HT 7 receptor partial agonist, serotonin 5-HT 2A and 5-HT 2B receptor antagonist or inverse agonist, and atypical antipsychotic [96] [97]
Antipsychotics by class Generic name Brand names Chemical class ATC code Typical antipsychotics; Acepromazine: Atravet, Acezine: phenothiazine: N05AA04
AR-08 – adrenergic receptor agonist [65] Aripiprazole (Abilify, Abilify Maintena, Abilify MyCite, Abilitat, Ao Pai, Aripiprazole depot, Aripiprazole ECER tablets, Arlemide; OPC-14597, OPC-14597 IMD, OPC-31) – atypical antipsychotic / dopamine receptor partial agonist and serotonin receptor modulator [66]
Dopamine receptor D 2, also known as D 2 R, is a protein that, in humans, is encoded by the DRD2 gene.After work from Paul Greengard's lab had suggested that dopamine receptors were the site of action of antipsychotic drugs, several groups, including those of Solomon H. Snyder and Philip Seeman used a radiolabeled antipsychotic drug to identify what is now known as the dopamine D 2 receptor. [5]
Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS) and are implicated in many neurological processes, including motivational and incentive salience, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling.
Third-generation antipsychotics were introduced in the 2000s and offer partial agonism, rather than blockade, of dopamine receptors. [14] Neuroleptic , originating from Ancient Greek : νεῦρον ( neuron ) and λαμβάνω ( take hold of )—thus meaning "which takes the nerve" —refers to both common neurological effects and side effects.
Aripiprazole lauroxil, sold under the brand name Aristada, is a long-acting injectable atypical antipsychotic that was developed by Alkermes. [3] [4] [5] It is an N-acyloxymethyl prodrug of aripiprazole that is administered via intramuscular injection once every four to eight weeks for the treatment of schizophrenia.
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