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Chemical Compound Review

Alaproclate     [1-(4-chlorophenyl)-2-methyl- propan-2-yl]...

Synonyms: Alaproclato, Alaproclatum, GEA-654, CHEMBL36591, SureCN34357, ...
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Disease relevance of Alaproclate

  • Alaproclate inhibits potassium currents and thereby enhances muscarinic stimulation in N1E-115 neuroblastoma cells [1].
  • A single acute dose of desipramine (20 mg/kg) administered at various time intervals before decapitation (1 to 24 hours) had no effect on the PDC's nor did repeated treatment with the other compounds examined, alaproclate, citalopram, clomipramine, mianserin and zimeldine, have any effect upon the PDC latency [2].

Psychiatry related information on Alaproclate


High impact information on Alaproclate

  • From the tentative pharmacophore and conformations of transmitter (5-HT) and inhibitor (alaproclate) derived from SAR, a hypothetic carrier site for 5-HT uptake is deduced in terms of geometry and electronic properties [8].
  • At depolarized potentials the alaproclate-induced block of the NMDA receptor current was strongly reduced, a result opposite to that seen with the voltage-activated K+ currents, suggesting that the K+ channel block may occur at a superficial internal site, whereas the NMDA receptor block occurs at a deep external site [9].
  • (+)-Alaproclate was a more potent blocker of K+ currents than (-)-alaproclate, whereas a reversed stereoselectivity was observed for NMDA receptor current, supporting the view that alaproclate block of the two channel types occurs at structurally distinct binding sites [9].
  • Alaproclate produced a concentration-dependent block of the sustained voltage-dependent K+ current activated by depolarization from -60 to +40 mV (IC50, 6.9 microM) [9].
  • At similar concentrations alaproclate also blocked the sustained voltage-dependent K+ current in fibroblast cells transformed to stably express Kv1.2 K+ channels [9].

Chemical compound and disease context of Alaproclate


Biological context of Alaproclate


Anatomical context of Alaproclate


Associations of Alaproclate with other chemical compounds


Gene context of Alaproclate

  • This suggests that alaproclate acutely increases the responsiveness of postsynaptic muscarinic and alpha 1 adrenoceptors [23].
  • In the frontal cortex, in which separate monoaminergic and tachykinin-containing neurones interact, treatment with imipramine reduced the levels of SP-LI and NKA/NKB-LI, while treatment with alaproclate had the opposite effect [24].
  • By contrast, the peak of the prolactin surge in model 2 was significantly prolonged by alaproclate [25].
  • In the cingulate cortex, the tissue levels of substance P and cholecystokinin were increased (19-32%) after subcutaneous (s.c.) treatment with alaproclate, compared to controls [26].
  • Pretreatment with the 5-HT receptor antagonist metitepine completely blocked the enhancement of oxotremorine-induced tremor caused by alaproclate [27].

Analytical, diagnostic and therapeutic context of Alaproclate


  1. Alaproclate inhibits potassium currents and thereby enhances muscarinic stimulation in N1E-115 neuroblastoma cells. Hedlund, B. Neuropharmacology (1987) [Pubmed]
  2. Attenuation of the post-decapitation convulsions after repeated treatment of rats with desipramine, imipramine and maprotiline. Archer, T., Ross, S.B., Minor, B.G. Acta pharmacologica et toxicologica. (1984) [Pubmed]
  3. Extracellular serotonin in the lateral hypothalamic area is increased during the postejaculatory interval and impairs copulation in male rats. Lorrain, D.S., Matuszewich, L., Friedman, R.D., Hull, E.M. J. Neurosci. (1997) [Pubmed]
  4. Alaproclate: a pharmacokinetic and biochemical study in patients with dementia of Alzheimer type. Bergman, I., Bråne, G., Gottfries, C.G., Jostell, K.G., Karlsson, I., Svennerholm, L. Psychopharmacology (Berl.) (1983) [Pubmed]
  5. A double-blind comparison of alaproclate and placebo in the treatment of patients with senile dementia. Dehlin, O., Hedenrud, B., Jansson, P., Nörgård, J. Acta psychiatrica Scandinavica. (1985) [Pubmed]
  6. Increased waking as well as increased synchronization following administration of selective 5-HT uptake inhibitors to rats. Ursin, R., Bjorvatn, B., Sommerfelt, L., Underland, G. Behav. Brain Res. (1989) [Pubmed]
  7. Chronic treatment with antidepressant drugs and the analgesia induced by 5-methoxy-N,N-dimethyltryptamine: attenuation by desipramine. Danysz, W., Minor, B.G., Post, C., Archer, T. Acta pharmacologica et toxicologica. (1986) [Pubmed]
  8. Inhibitors of neuronal monoamine uptake. 2. Selective inhibition of 5-hydroxytryptamine uptake by alpha-amino acid esters of phenethyl alcohols. Lindberg, U.H., Thorberg, S.O., Bengtsson, S., Renyi, A.L., Ross, S.B., Ogren, S.O. J. Med. Chem. (1978) [Pubmed]
  9. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Svensson, B.E., Werkman, T.R., Rogawski, M.A. Neuropharmacology (1994) [Pubmed]
  10. Similar effect on REM sleep but differential effect on slow wave sleep of the two 5-HT uptake inhibitors zimeldine and alaproclate in cats and rats. Sommerfelt, L., Hauge, E.R., Ursin, R. J. Neural Transm. (1987) [Pubmed]
  11. Serotonergic potentiation of muscarinic agonist evoked tremor and salivation in rat and mouse. Ogren, S.O., Carlsson, S., Bartfai, T. Psychopharmacology (Berl.) (1985) [Pubmed]
  12. Test-specific effects of the 5-HT reuptake inhibitors alaproclate and zimelidine on pain sensitivity and morphine analgesia. Ogren, S.O., Holm, A.C. J. Neural Transm. (1980) [Pubmed]
  13. Alaproclate increases the excitability of hippocampal CA1 pyramidal cells and blocks the slow after-hyperpolarization. Hedlund, B., Andersen, P. Pharmacol. Toxicol. (1989) [Pubmed]
  14. Correlations between in vitro dissolution rate and bioavailability of alaproclate tablets. Graffner, C., Nicklasson, M., Lindgren, J.E. Journal of pharmacokinetics and biopharmaceutics. (1984) [Pubmed]
  15. Kinetics of the interaction of sertraline with the human platelet plasma membrane 5-hydroxytryptamine carrier. Phillips, O.M., Wood, K.M., Williams, D.C. Eur. J. Pharmacol. (1988) [Pubmed]
  16. Effects of 5-hydroxytryptamine uptake blockers on the concentration in brain of 5-hydroxytryptamine and 5-hydroxyindoleacetic acid in male rats, pro-oestrous rats and ovariectomized rats treated with oestrogen and progesterone. Horn, A.M., Watts, A.G. J. Endocrinol. (1985) [Pubmed]
  17. Acute effects of zimelidine and alaproclate, two inhibitors of serotonin uptake, on neuroendocrine function. Syvälahti, E., Eneroth, P., Ross, S.B. Psychiatry research. (1979) [Pubmed]
  18. The effects of manipulation of presynaptic 5-HT nerve terminals on postsynaptic 5-HT1 and 5-HT2 binding sites of the rat brain. Hall, H., Wedel, I. J. Neural Transm. (1985) [Pubmed]
  19. Antinociceptive effects of serotonergic reuptake inhibitors in mice. Fasmer, O.B., Hunskaar, S., Hole, K. Neuropharmacology (1989) [Pubmed]
  20. Non-reversal of scopolamine- or age-related EEG changes by ondansetron, methysergide or alaproclate. Riekkinen, P., Sirviö, J., Riekkinen, P. Psychopharmacology (Berl.) (1991) [Pubmed]
  21. Cerebral activating properties of indeloxazine HCl and its optical isomers. Shimizu-Sasamata, M., Yamamoto, M., Harada, M. Pharmacol. Biochem. Behav. (1993) [Pubmed]
  22. Investigation into the effects in-vitro of the 5-hydroxytryptamine reuptake inhibitor, alaproclate, on carbachol-stimulated inositol phospholipid breakdown in the rat cerebral cortex. Fowler, C.J., Thorell, G., Ogren, S.O. J. Pharm. Pharmacol. (1987) [Pubmed]
  23. The effects of alaproclate on the pupillary responses to tyramine, phenylephrine and pilocarpine in depressed patients. Thompson, C., Checkley, S.A. Psychopharmacology (Berl.) (1985) [Pubmed]
  24. Effects of subchronic treatment with imipramine, zimelidine and alaproclate on regional tissue levels of substance P- and neurokinin A/neurokinin B-like immunoreactivity in the brain and spinal cord of the rat. Brodin, E., Ogren, S.O., Theodorsson-Norheim, E. Neuropharmacology (1987) [Pubmed]
  25. Effects of 5-hydroxytryptamine uptake blockers on the release of LH and prolactin in several different experimental steroid models in the rat. Horn, A.M., Fink, G. J. Endocrinol. (1985) [Pubmed]
  26. Effects of acute systemic treatment with the 5 HT-uptake blocker alaproclate on tissue levels and release of substance P in rat periaqueductal grey. Rosén, A., Franck, J., Brodin, E. Neuropeptides (1995) [Pubmed]
  27. In vivo and in vitro studies on the potentiation of muscarinic receptor stimulation by alaproclate, a selective 5-HT uptake blocker. Ogren, S.O., Nordström, O., Danielsson, E., Peterson, L.L., Bartfai, T. J. Neural Transm. (1985) [Pubmed]
  28. Acute and chronic treatment with selective serotonin uptake inhibitors in mice: effects on nociceptive sensitivity and response to 5-methoxy-N,N-dimethyltryptamine. Eide, P.K., Hole, K. Pain (1988) [Pubmed]
  29. Alaproclate acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow. Wilkinson, A., Courtney, M., Westlind-Danielsson, A., Hallnemo, G., Akerman, K.E. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
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