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Dr. Bob is Robert Hsiung, MD,
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Posted by Jeroen on August 16, 2011, at 1:45:13
Overall, the results show that cariprazine demonstrated superiority over
placebo for both the positive and negative symptoms of schizophrenia with good
tolerability, Dr. Bose observed.
this med is similar then abilify, i wanna get into this trial any ideas?
Posted by SLS on August 16, 2011, at 7:37:34
In reply to cariprazine superior anti psychotic!!, posted by Jeroen on August 16, 2011, at 1:45:13
> Overall, the results show that cariprazine demonstrated superiority over
> placebo for both the positive and negative symptoms of schizophrenia with good
> tolerability, Dr. Bose observed.
>
>
> this med is similar then abilify, i wanna get into this trial any ideas?From what I gather, cariprazine does share some properties with Abilify. Cariprazine is the only other AP to be available that acts as a DA receptor partial agonist. Cariprazine differs in that it is preferential for D3 receptors, although it does act at D2 receptors as well. It might actually produce a greater effect for negative symptoms than Abilify, as it acts more potently in the limbic system than the striatum.
Good luck with this drug. It is in Phase III in the US.
- Scott
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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.The Journal of pharmacology and experimental therapeutics 2010 Jan 21; In press
Link to PubMed abstract
Kiss B, Horvath A, Nemethy Z, Schmidt E, Laszlovszky I, Bugovics G, Fazekas K, Hornok K, Orosz S, Gyertyan I, Agai-Csongor E, Domany G, Tihanyi K, Adham N, Szombathelyi Z
1 Gedeon Richter Plc.;
Cariprazine (RGH-188, trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N',N'-dimethylurea hydrochloride), a novel candidate antipsychotic demonstrated approximately 10-fold higher affinity for human D(3) versus hD(2L) and hD(2S) receptors (pKi: 10.07, 9.16, 9.31, respectively). It displayed high affinity at h5-HT(2B) receptors (pKi: 9.24) with pure antagonism. Cariprazine had lower affinity at human and rat hippocampal 5-HT(1A) receptors (pKi: 8.59 and 8.34, respectively) and demonstrated low intrinsic efficacy. Cariprazine displayed low affinity at human 5-HT(2A) receptors (pKi: 7.73). Moderate or low affinity for histamine H1 and 5-HT(2C) receptors (pKi: 7.63 and 6.87, respectively) suggest cariprazine's reduced propensity for adverse events related to these receptors. Cariprazine demonstrated different functional profiles at dopamine receptors depending on assay system. It displayed D(2) and D(3) antagonism in [(35)S]GTPgammaS binding assays, but stimulated inositol phosphate (IP) production (pEC(50): 8.50, E(max) 30%) and antagonized (+/-)-quinpirole-induced IP accumulation (pKb: 9.22) in murine cells expressing human D(2L) receptors. It had partial agonist activity (pEC(50): 8.58, E(max) 71%) by inhibiting cAMP accumulation in CHO cells expressing hD(3) receptors and potently antagonized 7-OH-DPAT-induced suppression of cAMP formation (pKb: 9.57). In these functional assays, cariprazine showed similar (D(2)) or higher (D(3)) antagonist-partial agonist affinity and greater (3- to 10-fold) D(3) versus D(2) selectivity compared with aripiprazole. In in vivo turnover and biosynthesis experiments, cariprazine demonstrated D(2)-related partial agonist and antagonist properties, depending on actual dopaminergic tone. The antagonist-partial agonist properties of cariprazine at D(3) and D(2) receptors, with very high and preferential affinity to D(3) receptors, make it a candidate antipsychotic with a unique pharmacological profile among known antipsychotics.
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Posted by Phillipa on August 16, 2011, at 10:50:15
In reply to Re: cariprazine superior anti psychotic!! » Jeroen, posted by SLS on August 16, 2011, at 7:37:34
Jeroen I guess you will have to go with your previous ideas of a med in the new clinic. Love Phillipa
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