PR-000608
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| Other names | PR 000608 |
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| Formula | C29H35F2N3 |
| Molar mass | 463.617 g·mol−1 |
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PR-608 is a potent dopamine reuptake inhibitor of the 4,4-diphenylbutylpiperazine class, structurally related to vanoxerine. Other members of this class include amperozide and lidoflazine. A related stimulant is difluanazine.[1][2] A further example of a drug that was researched for the treatment of substance abuse disorder is called FG 5893. It was patented by Pfizer.[3]
It has been shown in preclinical studies to inhibit dopamine uptake in the central nervous system and may have potential applications in neuropsychiatric and cardiovascular disorders.[4][5][6][7]
The calcium channel blocking properties of PR-608 might make it useful as a cardiac stimulant for the treatment of heart disease or as a cerebral vasodilator.[8] Alternative applications of this agent include for the treatment of psychostimulant addiction, neurodegenerative diseases including (but not limited to) Parkinson's disease,[9][10] and as a treatment for depression.[11][12][13] Since dopamine regulates the appetite, PR-608 might also find use for treating binge eating disorder (BED) as well as treating narcolepsy.
See also
[edit]References
[edit]- ^ "Difluanazine". PubChem. U.S. National Library of Medicine.
- ^ US 3267104, Hermans HK, Karl-Adolf SW, "1,4-Disubstituted piperazines and diazepines", issued 16 August 1966, assigned to Janssen Pharmaceutica NV
- ^ Anders Björk & Gunnar Andersson, WO1993020821 (to Pfizer Health AB).
- ^ Kimura M, Masuda T, Yamada K, Mitani M, Kubota N, Kawakatsu N, et al. (April 2003). "Syntheses of novel diphenyl piperazine derivatives and their activities as inhibitors of dopamine uptake in the central nervous system". Bioorganic & Medicinal Chemistry. 11 (8): 1621–1630. doi:10.1016/s0968-0896(03)00061-0. PMID 12659747.
- ^ Kimura M, Masuda T, Yamada K, Mitani M, Kubota N, Kawakatsu N, et al. (September 2003). "Novel diphenylalkyl piperazine derivatives with high affinities for the dopamine transporter". Bioorganic & Medicinal Chemistry. 11 (18): 3953–3963. doi:10.1016/s0968-0896(03)00428-0. PMID 12927856.
- ^ Kimura M, Masuda T, Yamada K, Mitani M, Kubota N, Kawakatsu N, et al. (June 2004). "Efficient asymmetric syntheses, determination of absolute configurations and biological activities of 1-[4,4-bis(4-fluorophenyl)butyl]-4-[2-hydroxy-3-(phenylamino)propyl]piperazine as a novel potent dopamine uptake inhibitor in the central nervous system". Bioorganic & Medicinal Chemistry. 12 (11): 3069–3078. doi:10.1016/j.bmc.2004.02.041. PMID 15142566.
- ^ US 5391552, Inazu M, Miyata Y, Morimoto T, Yamamoto T, Yoshiko Y, Harada K, Momota Y, Yanagi M, Yokota R, Katoh T, Namiki T, Kimura M, Kawakatsu N, "Diphenylpiperazine derivative and drug for circulatory organ containing the same.", issued 21 February 1995, assigned to Pola Orbis Holdings Inc.
- ^ Kimura M, Masuda T, Yamada K, Kubota N, Kawakatsu N, Mitani M, et al. (August 2002). "Novel diphenylalkyl piperazine derivatives with dual calcium antagonistic and antioxidative activities". Bioorganic & Medicinal Chemistry Letters. 12 (15): 1947–1950. doi:10.1016/s0960-894x(02)00322-0. PMID 12113815.
- ^ "PR-000608". PatSnap.
- ^ Harada M, Kubota N, Masuda T, Inazu M (January 1996). "P-525: Effects of PR-000608, a novel antiparkinson drug, on MPTP-induced parkinsonism". Japanese Journal of Pharmacology. 71: 190. doi:10.1016/S0021-5198(19)36998-7.
- ^ Orr K, Taylor D (2007). "Psychostimulants in the treatment of depression : a review of the evidence". CNS Drugs. 21 (3): 239–57. doi:10.2165/00023210-200721030-00004. PMID 17338594.
- ^ Dunlop BW, Nemeroff CB (March 2007). "The role of dopamine in the pathophysiology of depression". Archives of General Psychiatry. 64 (3): 327–37. doi:10.1001/archpsyc.64.3.327. PMID 17339521.
- ^ Gershon AA, Vishne T, Grunhaus L (January 2007). "Dopamine D2-like receptors and the antidepressant response". Biological Psychiatry. 61 (2): 145–53. doi:10.1016/j.biopsych.2006.05.031. PMID 16934770.