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Chemical Compound Review

Budipina     4,4-diphenyl-1-tert-butyl- piperidine

Synonyms: Budipine, Budipin, Budipinum, Budipine (INN), Budipine [INN], ...
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Disease relevance of Budipine


High impact information on Budipine

  • Dopamine release was blocked by the centrally acting AADC inhibitor NSD 1015, but facilitated by the central AADC activator budipine [6].
  • The NMDA receptor antagonistic effects of budipine were assessed using concentration- and patch-clamp techniques on cultured striatal, hippocampal, cortical and superior colliculus neurones [7].
  • Budipine is a low affinity, N-methyl-D-aspartate receptor antagonist: patch clamp studies in cultured striatal, hippocampal, cortical and superior colliculus neurones [7].
  • Budipine exhibited concentration-dependent open channel blocking kinetics (kappa(on) = 0.71 x 10(4) M(-1) s(-1)) whereas the fast offset rate was concentration-independent (kappa(off) = 0.63 s(-1)) [7].
  • Whereas both drugs (1-10 microM) strongly increased spontaneous [3H]outflow in caudate nucleus slices preincubated with [3H]DA, budipine inhibited but biperiden facilitated the evoked DA release [8].

Chemical compound and disease context of Budipine


Biological context of Budipine

  • Therefore, these two aromatic residues in the channel pore are likely to form a main part of the binding site for budipine.In summary, this is the first study that provides a molecular basis for the budipine-associated aLQTS observed in clinical practice [4].
  • In receptor-binding assays, budipine inhibited thienylcyclohexylpiperidyl-3,4-[3H](n) ([I3H]TCP) (2.5 nM)-binding with an IC50 of 36 microM and [3H]3-quinuclidinol benzilate-binding with an IC50 of 1.1 microM [9].
  • The area under the concentration vs time curve (AUC) and the maximum serum concentration (Cmax) showed a linear increase in line with ascending doses of orally given budipine [11].
  • Dose linearity and steady state pharmacokinetics of the new antiparkinson agent budipine after oral administration [11].
  • 10(-7), 10(-8), 10(-9) mol/l of budipine significantly reduced release of TNF-alpha and Il-6 in PBMC and decreased apoptotic cell death after 50 hours and 74 hours in the SH-SY 5Y cells [12].

Anatomical context of Budipine


Associations of Budipine with other chemical compounds


Gene context of Budipine


Analytical, diagnostic and therapeutic context of Budipine

  • To determine the impact of impaired hydromorphone formation on the behavioral effects of the parent compound, hydrocodone-induced analgesia and hyperactivity, hydrocodone discrimination and self-administration were examined in male Wistar rats, with or without pretreatment with CYP2D1 inhibitors (quinine and budipine) [22].
  • In clinical trials budipine reduced tremor, akinesia and rigidity [3].
  • Budipine is a potent non-dopaminergic antiparkinsonian drug with pharmacological effects that are not comparable to those of conventional drugs applied in Parkinsonian pharmacotherapy [23].
  • To investigate whether the uptake of the anti-Parkinson drug budipine into the brain is mediated by P-glycoprotein, abcb1ab(-/-) double knock-out mice and wild-type control mice received budipine continuously over 11 days via implanted osmotic infusion pumps at the rate of 30ug over 24h [15].
  • Effects of the antiparkinson drug budipine on EEG activity in unrestrained rats [24].


  1. Budipine provides additional benefit in patients with Parkinson disease receiving a stable optimum dopaminergic drug regimen. Przuntek, H., Bittkau, S., Bliesath, H., Büttner, U., Fuchs, G., Glass, J., Haller, H., Klockgether, T., Kraus, P., Lachenmayer, L., Müller, D., Müller, T., Rathay, B., Sgonina, J., Steinijans, V., Teshmar, E., Ulm, G., Volc, D. Arch. Neurol. (2002) [Pubmed]
  2. Synergism between topiramate and budipine in refractory status epilepticus in the rat. Fisher, A., Wang, X., Cock, H.R., Thom, M., Patsalos, P.N., Walker, M.C. Epilepsia (2004) [Pubmed]
  3. Clinical efficacy of budipine in Parkinson's disease. Przuntek, H., Müller, T. J. Neural Transm. Suppl. (1999) [Pubmed]
  4. Drug binding to aromatic residues in the HERG channel pore cavity as possible explanation for acquired Long QT syndrome by antiparkinsonian drug budipine. Scholz, E.P., Zitron, E., Kiesecker, C., Lueck, S., Kathöfer, S., Thomas, D., Weretka, S., Peth, S., Kreye, V.A., Schoels, W., Katus, H.A., Kiehn, J., Karle, C.A. Naunyn Schmiedebergs Arch. Pharmacol. (2003) [Pubmed]
  5. Prophylactic treatment of cluster headache with budipine. Krüger, H., Kohlhepp, W., Reimann, G., Przuntek, H. Headache. (1988) [Pubmed]
  6. Dual effects of L-3,4-dihydroxyphenylalanine on aromatic L-amino acid decarboxylase, dopamine release and motor stimulation in the reserpine-treated rat: evidence that behaviour is dopamine independent. Fisher, A., Biggs, C.S., Eradiri, O., Starr, M.S. Neuroscience (2000) [Pubmed]
  7. Budipine is a low affinity, N-methyl-D-aspartate receptor antagonist: patch clamp studies in cultured striatal, hippocampal, cortical and superior colliculus neurones. Parsons, C.G., Hartmann, S., Spielmanns, P. Neuropharmacology (1998) [Pubmed]
  8. Effects of the antiparkinsonian drug budipine on neurotransmitter release in central nervous system tissue in vitro. Jackisch, R., Huang, H.Y., Reimann, W., Limberger, N. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  9. Effects of the antiparkinsonian drug budipine on central neurotransmitter systems. Klockgether, T., Wüllner, U., Steinbach, J.P., Petersen, V., Turski, L., Löschmann, P.A. Eur. J. Pharmacol. (1996) [Pubmed]
  10. The protective effect of 1-tert.butyl-4,4-diphenylpiperidine against the nigrostriatal neurodegeneration caused by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. Przuntek, H., Russ, H., Henning, K., Pindur, U. Life Sci. (1985) [Pubmed]
  11. Dose linearity and steady state pharmacokinetics of the new antiparkinson agent budipine after oral administration. Bethke, T.H., Merz, M., Zech, K., Seiberling, M., Hauschke, D., Heinze, H., Wurst, W. International journal of clinical pharmacology and therapeutics. (2001) [Pubmed]
  12. Antiapoptotic effects of budipine. Müller, T., Przuntek, H., Krüger, R., Mackowiak, A. Journal of neural transmission (Vienna, Austria : 1996) (2004) [Pubmed]
  13. The antiparkinsonian drug budipine stimulates the activity of aromatic L-amino acid decarboxylase and enhances L-DOPA-induced dopamine release in rat substantia nigra. Biggs, C.S., Fisher, A., Starr, M.S. Synapse (1998) [Pubmed]
  14. Microdialysis study of the effects of the antiparkinsonian drug budipine on L-DOPA-induced release of dopamine and 5-hydroxytryptamine by rat substantia nigra and corpus striatum. Biggs, C.S., Starr, M.S. Synapse (1999) [Pubmed]
  15. The anti-Parkinson drug budipine is exported actively out of the brain by P-glycoprotein in mice. Uhr, M., Ebinger, M., Rosenhagen, M.C., Grauer, M.T. Neurosci. Lett. (2005) [Pubmed]
  16. The antiparkinsonian drug budipine binds to NMDA and sigma receptors in postmortem human brain tissue. Kornhuber, J., Herr, B., Thome, J., Riederer, P. J. Neural Transm. Suppl. (1995) [Pubmed]
  17. Effects of amantadine and budipine on antidepressant drug-evoked changes in extracellular dopamine in the frontal cortex of freely moving rats. Owen, J.C., Whitton, P.S. Brain Res. (2006) [Pubmed]
  18. Costs in the treatment of parkinsonism. Jost, W.H. J. Neurol. (2000) [Pubmed]
  19. The effects of prodipine and budipine on 14C-5-hydroxytryptamine uptake and release by human blood platelets. Eltze, M. Arzneimittel-Forschung. (1980) [Pubmed]
  20. Workshop III: late motor complications of Parkinson's disease. Jost, W.H., Berg-Mantkowski, A., Baas, H., Gemende, I., Glass, J., Kogan, E., Schneider, E., Storch, A. J. Neurol. (2000) [Pubmed]
  21. Intracerebroventricular administration of 1-methyl-4-phenylpyridinium ion in mice: effects of simultaneously administered nomifensine, deprenyl, and 1-t-butyl-4,4-diphenylpiperidine. Mihatsch, W., Russ, H., Przuntek, H. J. Neural Transm. (1988) [Pubmed]
  22. Effect of cytochrome P450 2D1 inhibition on hydrocodone metabolism and its behavioral consequences in rats. Tomkins, D.M., Otton, S.V., Joharchi, N., Li, N.Y., Balster, R.F., Tyndale, R.F., Sellers, E.M. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  23. Non-dopaminergic therapy in Parkinson's disease. Przuntek, H. J. Neurol. (2000) [Pubmed]
  24. Effects of the antiparkinson drug budipine on EEG activity in unrestrained rats. Dimpfel, W., Spüler, M., Menge, H.G. Arzneimittel-Forschung. (1989) [Pubmed]
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