Psychiatria pre prax 4/2018
Úloha dopamínových D3 parciálnych agonistov v modernej liečbe schizofrénie
Schizophrenia is chronic psychotic disease, affects various symptom domains including positive, negative, affective symptoms and cognition. Despite the etiopathogenesis of schizophrenia is not well known, the mesolimbic hyperfunction in dopamine neurotransmitter system together with mesocortical hypofunction play an important role. There are several postsynaptic dopaminergic receptors; the function of the D2 receptors are best understood and the role of D3 receptors is largely unknown, but may be linked to cognition, mood, emotions and reward, all of them strongly related to negative symptoms in schizophrenia. Targeting the D3 receptor is hypothesized to increase dopaminergic transmission to the prefrontal cortex, alleviating cognitive and negative symptoms. It is proposed that targeting the D3 and D2 receptor simultaneously in ventral striatum will continue to alleviate positive symptoms. Cariprazine is a dopamine D3 /2 receptor partial agonist with higher affinity to D3 than to D2 receptors. And since cariprazine has a higher affinity to D3 receptors than dopamine itself, it has the ability to actually occupy D3 receptors in the presence of dopamine and exhibit the improvement of negative symptoms, cognition and mood.
Keywords: dopamine theory of schizophrenia, D3 receptors, partial agonists, cariprazine
