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Cariprazine (RGH-188), a Dopamine D3 Receptor-Preferring, D3/D2 Dopamine Receptor Antagonist–Partial Agonist Antipsychotic Candidate: In Vitro and Neurochemical Profile
TLDR
The antagonist–partial agonist properties of cariprazine at D3 and D2 receptors, with very high and preferential affinity to D3 receptors, make it a candidate antipsychotic with a unique pharmacological profile among known antipsychotics. Expand
Effects of RGH-237 [N-{4-[4-(3-Aminocarbonyl-phenyl)-piperazin-1-yl]-butyl}-4-bromo-benzamide], an Orally Active, Selective Dopamine D3 Receptor Partial Agonist in Animal Models of Cocaine Abuse
TLDR
The results demonstrate that selective D3 partial agonists may be an effective therapeutic means in the treatment of cocaine abuse. Expand
Cariprazine (RGH-188), a potent D3/D2 dopamine receptor partial agonist, binds to dopamine D3 receptors in vivo and shows antipsychotic-like and procognitive effects in rodents
TLDR
The distinct in vivo profile of cariprazine may be due to its higher affinity and in vivo binding to D(3) receptors versus currently marketed typical and atypical antipsychotics. Expand
Cariprazine (RGH-188), a D3-preferring dopamine D3/D2 receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats
TLDR
Results in rats with a history of cocaine self-administration after a period of complete abstinence in a relapse to cocaine-seeking paradigm may predict a relapse-preventing action for cariprazine in humans in addition to its existing antipsychotic and antimanic efficacy. Expand
NR2B subunit selective NMDA antagonists inhibit neurotoxic effect of alcohol-withdrawal in primary cultures of rat cortical neurones
TLDR
It is demonstrated that NR2B SSNAs given in the course of the withdrawal potently reduced the LDH release in ethanol pre-treated cultures of rat cortical neurones and could be promising therapeutic candidates in the pharmacotherapy for physical signs of acute alcohol-withdrawal and associated neuronal damage. Expand
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.
Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D(3)/D(2) compound (1) led to a series of new piperazine derivativesExpand
Neuroprotective Effects of Vinpocetine and its Major Metabolite Cis‐apovincaminic Acid on NMDA‐Induced Neurotoxicity in a Rat Entorhinal Cortex Lesion Model
TLDR
The morphological findings corroborated the behavioral observations and indicated reduced lesion size and microglia activation especially after vinpocetine treatment which supports an in vivo neuroprotective mode of action of vin pocitine and a less potent action of cAVA. Expand
Differential alterations in the expression of NMDA receptor subunits following chronic ethanol treatment in primary cultures of rat cortical and hippocampal neurones
TLDR
It is demonstrated that the maximal inhibitory effect of ethanol was significantly increased after ethanol pre-treatment, and the inhibitory activity of the NR2B subunit selective antagonists threo-ifenprodil, CP-101,606 and CI-1041 was also enhanced. Expand
Identification of metabolic pathways involved in the biotransformation of tolperisone by human microsomal enzymes.
TLDR
It was concluded that tolperisone undergoes P 450-dependent and P450-independent microsomal biotransformations to the same extent and on the basis of metabolites formed and indirect evidences of inhibition studies, a considerable involvement of aMicrosomal reductase is assumed. Expand
NR2B containing NMDA receptor dependent windup of single spinal neurons
TLDR
Results are in agreement with the well-documented effectivity of NR2B subtype selective NMDA receptor antagonists in chronic pain models and give the first direct evidence that spinal mechanisms are involved in this effect. Expand
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