Budipine
- N04BX03 (WHO)
- 1-tert-butyl-4,4-diphenylpiperidine[1]
- 57982-78-2 Y
- 68778
- 62021 Y
- L9026OPI2Z
- D07306 Y
- ChEMBL334491 Y
- DTXSID20206709
- Interactive image
- c1(ccccc1)C3(c2ccccc2)CCN(C(C)(C)C)CC3
- InChI=1S/C21H27N/c1-20(2,3)22-16-14-21(15-17-22,18-10-6-4-7-11-18)19-12-8-5-9-13-19/h4-13H,14-17H2,1-3H3 Y
- Key:QIHLUZAFSSMXHQ-UHFFFAOYSA-N Y
Budipine (brand name Parkinsan) is an antiparkinson agent marketed for the treatment of Parkinson's disease.[2][3][4]
While its exact mechanism of action is not well characterized,[2] it is believed to be an NMDA receptor antagonist,[5][6] but also promoting the synthesis of dopamine.[7]
Because it provides additional benefits relative to existing treatments, it probably does not precisely mimic the mechanism of an existing known treatment.[7][8]
Synthesis
Budipine can be prepared from the 1-tert-butyl-4-piperidone [1465-76-5] directly by treatment with benzene in the presence triflic acid.[9] This method of synthesis enables a 99% yield of product.
4-Phenyl-1-t-butyl-4-piperidinol,[11] (1)
1-t-butyl-3-benzoyl-4-phenyl-4-piperidinol [81831-81-4] (3)
See also
- AD-1211
- Delucemine
- Diphenidine
- Ephenidine
- Fluorolintane
- Lanicemine
- Methoxphenidine (MXP)
- MT-45
- Remacemide
References
- ^ Sweetman SC, ed. (2007). Martindale: The Complete Drug Reference (35th ed.). London: Pharmaceutical Press. ISBN 978-0-85369-687-2.
- ^ a b Reichmann H (October 2006). "Budipine in Parkinson's tremor". Journal of the Neurological Sciences. 248 (1–2): 53–55. doi:10.1016/j.jns.2006.05.039. PMID 16784759. S2CID 21540225.
- ^ Przuntek H, Müller T (1999). "Clinical efficacy of budipine in Parkinson's disease". Diagnosis and Treatment of Parkinson's Disease — State of the Art. Journal of Neural Transmission. Supplementa. Vol. 56. pp. 75–82. doi:10.1007/978-3-7091-6360-3_3. ISBN 978-3-211-83275-2. PMID 10370903.
{{cite book}}
:|journal=
ignored (help) - ^ "Budipine". AdisInsight. Springer Nature Switzerland AG.
- ^ Kornhuber J, Herr B, Thome J, Riederer P (1995). "The antiparkinsonian drug budipine binds to NMDA and sigma receptors in postmortem human brain tissue". Journal of Neural Transmission. Supplementum. 46: 131–137. PMID 8821048.
- ^ Palmer GC (September 2001). "Neuroprotection by NMDA receptor antagonists in a variety of neuropathologies". Current Drug Targets. 2 (3): 241–271. doi:10.2174/1389450013348335. PMID 11554551.
- ^ a b Przuntek H, Bittkau S, Bliesath H, Büttner U, Fuchs G, Glass J, et al. (May 2002). "Budipine provides additional benefit in patients with Parkinson disease receiving a stable optimum dopaminergic drug regimen". Archives of Neurology. 59 (5): 803–806. doi:10.1001/archneur.59.5.803. PMID 12020263.
- ^ Owen JC, Whitton PS (October 2006). "Effects of amantadine and budipine on antidepressant drug-evoked changes in extracellular dopamine in the frontal cortex of freely moving rats". Brain Research. 1117 (1): 206–212. doi:10.1016/j.brainres.2006.07.039. PMID 16996043. S2CID 29177107.
- ^ Klumpp, D. A., Garza, M., Jones, A., Mendoza, S. (1 September 1999). "Synthesis of Aryl-Substituted Piperidines by Superacid Activation of Piperidones". The Journal of Organic Chemistry. 64 (18): 6702–6705. doi:10.1021/jo990454i.
- ^ Schaefer H, Hackmack G, Eistetter K, Krüger U, Menge HG, Klosa J (1984). "[Synthesis, physical-chemical properties and pharmacologically-oriented screening studies on budipine and related 4,4-diphenylpiperidines]". Arzneimittel-Forschung (in German). 34 (3): 233–240. PMID 6539602.
- ^ "4-Phenyl-1-t-butyl-4-piperidinol". PubChem. U.S. National Library of Medicine. CID:20536606.
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DA precursors | |
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DA receptor agonists |
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MAO-B inhibitors | |
COMT inhibitors | |
AAAD inhibitors |
- Amantadine
- Budipine
- Istradefylline
- Methylxanthines (e.g., caffeine)
- Rimantadine
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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