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)
ARTICLE;
BINDING AFFINITY;
BIOASSAY;
CANCER CELL;
CONTROLLED STUDY;
DRUG POTENCY;
DRUG RECEPTOR BINDING;
DRUG SCREENING;
DRUG STRUCTURE;
DRUG SYNTHESIS;
HUMAN;
HUMAN CELL;
RECEPTOR AFFINITY;
RECEPTOR BINDING;
STRUCTURE ACTIVITY RELATION;
The effect of morphine- and nalorphine-like drugs in the nondependent and morphine-dependent chronic spinal dog
Martin, W. R.; Eades, C. G.; Thompson, J. A.; Huppler, R. E.; Gilbert, P. E. The effect of morphine- and nalorphine-like drugs in the nondependent and morphine-dependent chronic spinal dog. J. Pharmacol. Exp. Ther. 1976, 197, 517-532.
A proposal for the classification of sigma binding sites
Quirion, R.; Bowen, W. D.; Itzhak, Y.; Junien, J. L.; Musacchio, J. M.; Rothman, R. B.; Su, T.-P.; Tam, S. W.; Taylor, D. P. A proposal for the classification of sigma binding sites. Trends Pharmacol. Sci. 1992, 13, 85-86.
Sigma receptors in the central nervous system and the periphery
Itzhak, Y., Ed.; Academic Press: London
Su, T.-P. Sigma receptors in the central nervous system and the periphery. In The Sigma Receptors; Itzhak, Y., Ed.; Academic Press: London, 1994; pp 21-44.
σ Receptors: Historical perspective and background
Matsumoto, R. R.; Bowen,W. D.; Su, T.-P. Ed.; Springer: New York
Matsumoto, R. R. σ Receptors: Historical perspective and background. In Sigma Receptors Chemistry, Cell Biology and Clinical Implications; Matsumoto, R. R.; Bowen,W. D.; Su, T.-P. Ed.; Springer: New York, 2007; pp 1-23.
Labelled sigma receptor ligands: Can their role in neurology and oncology be extended?
Caveliers, V.; Everaet, H.; Lahoutte, T.; Dierickx, L. O.; John, C. S.; Bossuyt, A. Labelled sigma receptor ligands: Can their role in neurology and oncology be extended? Eur. J. Nucl. Med. 2001, 28, 133-135.
Cloning and functional expression of the human type sigma receptor (hSigmaR1)
Kekuda, R.; Prasad, P. D.; Fei, Y.-J.; Leibach, F. H.; Ganapathy, V. Cloning and functional expression of the human type sigma receptor (hSigmaR1). Biochem. Biophys. Res. Commun. 1996, 229, 553-558.
Selective sigma-2 ligands preferentially bind to pancreatic adenocarcinomas: Applications in diagnostic imaging and therapy
doi: 10.1186/1476-4598-6-48
Kashiwagi, H.; McDunn, J. E.; Simon, P. O.; Goedegebuure, P. S.; Xu, J.; Jones, L.; Chang, K.; Johnston, F.; Trinkaus, K.; Hotchkiss, R. S.; Mach, R. H.; Hawkins, W. G. Selective sigma-2 ligands preferentially bind to pancreatic adenocarcinomas: Applications in diagnostic imaging and therapy. Mol. Cancer 2007, 6, 48, doi: 10.1186/1476-4598-6-48.
Sigma-2 receptor agonists activate apoptotic pathway and potentiate antineoplastic drugs in breast tumor cell lines
Crawford, K. W.; Bowen, W. D. Sigma-2 receptor agonists activate apoptotic pathway and potentiate antineoplastic drugs in breast tumor cell lines. Cancer Res. 2002, 62, 313-322.
Sigma receptors ligands: Possible application as therapeutic drugs and as radiopharmaceuticals
Hashimoto, K.; Ishiwata, K. Sigma receptors ligands: Possible application as therapeutic drugs and as radiopharmaceuticals. Curr. Pharm. Des. 2006, 12, 3857-3876.
Fluorine-18 labeled benzamide analogs for imaging the sigma-2 receptor status of solid tumors with positron emission tomography
Tu, Z.; Xu, J.; Jones, L. A.; Li, S.; Dumsdorf, C.; Vangveravong, S.; Chen, D.; Wheeler, K. T.; Welch, M. J.; Mach, R. H. Fluorine-18 labeled benzamide analogs for imaging the sigma-2 receptor status of solid tumors with positron emission tomography. J. Med. Chem. 2007, 50, 3194-3204.
Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress
Ostenfeld, M. S.; Fehrenbacher, N.; Hover-Hansen, M.; Thomsen, C.; Farkas, T.; Jaattela, M. Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress. Cancer Res. 2005, 65, 8975-8983.
1 antagonist receptor inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer
1 antagonist receptor inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer. Mol. Cancer Ther. 2006, 5, 1807-1816.
Is a nitrogen atom an important pharmacophoric element in sigma ligand binding?
Ablordeppey, S. Y; Fischer, J. B.; Glennon, R. A. Is a nitrogen atom an important pharmacophoric element in sigma ligand binding? Bioorg. Med. Chem. 2000, 8, 2105-2111.
The mysteries of sigma receptors: New family members reveal a role in cholesterol synthesis
Moebius, F. F.; Striessnig, J.; Glossmann, H. The mysteries of sigma receptors: New family members reveal a role in cholesterol synthesis. Trends Pharmacol. Sci. 1997, 18, 67-70.
An inexpensive carbohydrate derivative used as a chiral auxiliary in the synthesis of α-hydroxy carboxylic acids
Yu, H.; Ballard, E.; Boyle, P. D.; Wang, B. An inexpensive carbohydrate derivative used as a chiral auxiliary in the synthesis of α-hydroxy carboxylic acids. Tetrahedron 2002, 58, 7663-7679.
Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: Orally active prostacyclin mimetics. Part 2
Hattori, K.; Okitsu O.; Tabuchi, S.; Taniguchi, K.; Nishio, M.; Koyama, S.; Seki, J.; Sakane, K. Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2. Bioorg. Med. Chem. Lett. 2005, 15, 3279-3283.
Characterization of two novel sigma receptor ligands: Antidystonic effects in rats suggest sigma receptor antagonism
Matsumoto, R. R.; Bowen, W. D.; Tom, M. A.; Truong, D. D.; De Costa, B. R. Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur. J. Pharmacol. 1995, 280, 301-310.
