(+)-UH 232, a partial agonist of the D3 dopamine receptors, attenuates cognitive effects of angiotensin IV and des-Phe6-angiotensin IV in rats

2010 ◽  
Vol 20 (4) ◽  
pp. 218-225 ◽  
Author(s):  
Jan J. Braszko
Neuropeptides ◽  
2008 ◽  
Vol 42 (3) ◽  
pp. 301-309 ◽  
Author(s):  
Jan J. Braszko ◽  
Przemysław Wielgat ◽  
Anna Walesiuk

CNS Spectrums ◽  
2018 ◽  
Vol 23 (1) ◽  
pp. 95-95
Author(s):  
Maximous K. Philobos ◽  
Alan R. Hirsch

AbstractIntroductionCariprazine an atypical antipsychotic which acts as a dopamine D3-prefering partial agonist at dopamine D2/D3 receptors, as an antagonist at over stimulated dopamine receptors, as a partial agonist at serotonin 5-HT1A receptors, and as an antagonist of 5-HT2A receptors (Citrome, 2016; Kiss, 2010). While indicated for the treatment of schizophrenia and bipolar disorder, it has never been described to improve disorders of cranial nerve VIII. A patient with hearing loss associated with tinnitus, responsive to cariprazine, is reported.MethodsCase Study: A 34 year old right handed married male 5 years prior to presentation developed bilateral auditory hallucinations of whispers, and one male disparaging voice. Approximately 6 months later it began belittling him, whereupon he was diagnosed with schizoaffective disorder, attention deficit hyperactivity disorder, and obsessive-compulsive disorder.Three months prior to presentation he developed sepsis and became comatose. Upon awakening he experienced constant tinnitus, AS more than AD high pitched, without diurnal variation, which has been unrelenting. Coincident with the tinnitus was decreased hearing AS more than AD. Within a few days of treatment with cariprazine at 1.5 mg a day, the tinnitus transiently resolved and after raising the cariprazine to 3 mg per day the tinnitus abruptly stopped and his hearing returned to normal after 2 months. One and a half days after discontinuing the cariprazine the tinnitus and hearing loss returned. After reinstating the cariprazine to 3 mg a day the tinnitus and hearing loss resolved again.ResultsPsychiatric evaluation: Disheveled with postural tremor of both upper extremities. Pharyngeal dysarthria. Irritable and with expansive and labile affect. Severely impaired attention. Slow tangential thoughts, preoccupied with paranoia and suspiciousness. Paranoid delusions. Mental status examination: Memory testing: Immediate recall: 5 digits forwards and 3 digits backwards. Able to recall none of 4 objects in 3 minutes and 1 with reinforcement. Unable to spell the word “world.” Similarities interpreted concretely. Calculation ability poor.DiscussionIn the cochlea, as an inhibitory neurotransmitter, dopamine reduces sensitivity to auditory sensation (Langguth, 2009). Since ambient sounds are known to reduce tinnitus (masking), an antagonist at overstimulated dopamine receptors, cariprazine may act to reduce dopamine’s effectiveness, reducing inhibition and thus enhancing perceived external sound. It may act as a 5-HT1A serotonin agonist, directly reducing tinnitus. With reduced tinnitus there is less of a distraction and thus enhanced hearing. Or its function may be through its neuroleptic effects; the tinnitus could be a manifestation of auditory hallucinations, through reduction of this noise cariprazine secondarily causes enhanced hearing. Further investigation into the use of cariprazine in those with intractable tinnitus is worthwhile.Funding AcknowledgementsNo funding.


2012 ◽  
Vol 683 (1-3) ◽  
pp. 155-160 ◽  
Author(s):  
Paul R. Gard ◽  
Cathy Naylor ◽  
Sofiya Ali ◽  
Clare Partington

2020 ◽  
Vol 2 (3) ◽  
pp. 58-63
Author(s):  
Igor V. Dorovskikh ◽  
Tatyana A. Pavlova ◽  
Julia M. Scheidegger

This article provides an overview of the causes and mechanisms of drug hyperprolactinemia (GP) associated with the use of antipsychotics, and describes its main clinical symptoms. The most probable factors of the high frequency of GP development that persists to date when using antipsychotics in the practice of a psychiatrist are considered. Modern methods of its prevention and correction developed by domestic and foreign researchers are presented. Emphasis is placed on the importance and necessity of careful collection of the patient's medical history, laboratory and instrumental examination, monitoring of the dynamics of hormonal indicators, correct choice of therapeutic tactics for the prevention of GP and its timely relief. The neuroendocrine profile of the latest generation of antipsychotics is considered. Special attention is paid to the partial agonist of D-2, D3-dopamine receptors cariprazine. Based on the review of recent clinical studies, the possibilities of its use in clinical practice are considered in detail, and the neuroendocrine profile of the drug is presented. The prospects of its use as a corrector of GP associated with the treatment of mental disorders with other antipsychotics are evaluated.


2017 ◽  
Vol 329 ◽  
pp. 140-147 ◽  
Author(s):  
Sara Fidalgo ◽  
Charlotte Skipper ◽  
Abigail Takyi ◽  
Aisling McIver ◽  
Theodoros Tsiligkaridis ◽  
...  

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