PB-28
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| Names | |
|---|---|
| IUPAC name
1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetra-
hydronaphthalen-1-yl)propyl]piperazine | |
| Other names
PB28 | |
| Identifiers | |
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3D model (JSmol) |
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| ChEBI | |
| ChEMBL | |
| ChemSpider | |
| ECHA InfoCard | 100.215.826 |
| MeSH | C097775 |
PubChem CID |
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| UNII | |
CompTox Dashboard (EPA) |
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| Properties | |
| C24H38N2O | |
| Molar mass | 370.57 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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PB-28[1] is an agonist of the sigma-2 receptor.[2][3][4][5][6]
It is derived from cyclohexylpiperazine.
Usage
[edit]Research and oncology
[edit]In oncology, it has been noted that PB-28 reverts doxorubicin resistance of breast cancer cells by supplementing Oxygen (O
2) receptor binding.[7]
References
[edit]- ↑ Berardi F, Colabufo NA, Giudice G, Perrone R, Tortorella V, Govoni S, Lucchi L (1996). "New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives". J. Med. Chem. 39 (1): 176–82. doi:10.1021/jm950409c. PMID 8568804.
- ↑ Cassano G, Gasparre G, Contino M, Niso M, Berardi F, Perrone R, Colabufo NA (2006). "The sigma-2 receptor agonist PB28 inhibits calcium release from the endoplasmic reticulum of SK-N-SH neuroblastoma cells". Cell Calcium. 40 (1): 23–8. doi:10.1016/j.ceca.2006.03.004. PMID 16687172.
- ↑ Azzariti A, Colabufo NA, Berardi F, Porcelli L, Niso M, Simone GM, Perrone R, Paradiso A (2006). "Cyclohexylpiperazine derivative PB28, a sigma2 agonist and sigma1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer" (PDF). Mol. Cancer Ther. 5 (7): 1807–16. doi:10.1158/1535-7163.MCT-05-0402. PMID 16891467. S2CID 24267660.
- ↑ Colabufo NA, Berardi F, Abate C, Contino M, Niso M, Perrone R (July 2006). "Is the sigma2 receptor a histone binding protein?". Journal of Medicinal Chemistry. 49 (14): 4153–8. doi:10.1021/jm0600592. PMID 16821775.
- ↑ Berardi F, Abate C, Ferorelli S, Uricchio V, Colabufo NA, Niso M, Perrone R (December 2009). "Exploring the importance of piperazine N-atoms for sigma(2) receptor affinity and activity in a series of analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28)". Journal of Medicinal Chemistry. 52 (23): 7817–28. doi:10.1021/jm9007505. PMID 19842660.
- ↑ Abate C, Elenewski J, Niso M, Berardi F, Colabufo NA, Azzariti A, Perrone R, Glennon RA (February 2010). "Interaction of the sigma(2) receptor ligand PB28 with the human nucleosome: computational and experimental probes of interaction with the H2A/H2B dimer". ChemMedChem. 5 (2): 268–73. doi:10.1002/cmdc.200900402. PMID 20077462. S2CID 33532349.
- ↑ Francesco Berardi, Carmen Abate, Savina Ferorelli, Vincenzo Uricchio, Nicola A. Colabufo, Mauro Niso, Roberto Perrone; Exploring the Importance of Piperazine N-Atoms for σ2 Receptor Affinity and Activity in a Series of Analogs of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28)†. J. Med. Chem. 10 December 2009; 52 (23): 7817–7828. https://doi.org/10.1021/jm9007505
External links
[edit]- PB28+compound at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
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