Abstract:
:Prolyl oligopeptidase (POP) has been connected to learning, memory and mood. Changes in serum or plasma POP activity have been linked to psychiatric disorders. POP has been thought to interfere in these conditions by cleaving neuroactive peptides or via the phosphatidylinositol second messenger system. However, little is known about the possible POP inhibition of commonly used psychoactive drugs. In this study, we measured the effects of various psychotropic drugs, including antidepressants, antipsychotics, mood stabilisers and anxiolytics, on the activity of the rat brain homogenate POP. Of the 38 compounds tested, 18 inhibited POP by at least 20% at 10 μM (buspirone, chlorpromazine, citalopram, clozapine, desipramine, duloxetine, escitalopram, flupenthixol, imipramine, ketanserin, lamotrigine, levomepromazine, prazosin, prochlorperazine, promazine, risperidone ritanserin and thioridazine). Thioridazine and valproate (VPA) acted at therapeutic plasma levels. Kinetically, VPA was a competitive inhibitor, thioridazine a non-competitive inhibitor and ketanserin a mixed type inhibitor. Being lipophilic, many of the psychoactive compounds are present in the brain at several-times higher concentrations than in plasma. At concentrations reported to be reached in the brain, chlorpromazine, clozapine, desipramine, imipramine, prochlorperazine and promazine inhibited POP by 30-50% suggesting that they could inhibit POP in vivo. However, when studied ex vivo, a single dose of 10 mg/kg thioridazine caused a deep sedation in the mice but did not inhibit the activity of POP. In conclusion, compared with conventional POP inhibitors, all psychopharmacological compounds tested are very weak inhibitors in vitro, and we doubt that their POP inhibition would be therapeutically meaningful.
journal_name
Basic Clin Pharmacol Toxicoljournal_title
Basic & clinical pharmacology & toxicologyauthors
Peltonen I,Männistö PTdoi
10.1111/j.1742-7843.2010.00626.xsubject
Has Abstractpub_date
2011-01-01 00:00:00pages
46-54issue
1eissn
1742-7835issn
1742-7843pii
PTO626journal_volume
108pub_type
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