Sigma(1) and sigma(2) receptors have been detected in many tissues and are highly expressed in several tumour cell lines from various tissues. The high level of expression observed for sigma receptors and their involvement in cell proliferation and apoptosis has led to the development of several sigma ligands in order to obtain a molecular probe for in-vivo diagnostic imaging techniques such as positron emission tomography (PET) and single photon emission computerized tomography (SPECT). The EMT-6 cells implanted in mice were a good model for evaluating the proliferation of solid tumours by in-vivo PET. Moreover, we developed the sigma ligand PB167, a cyclohexylpiperazine derivative, previously evaluated for sigma(2) receptor affinity and activity in standard protocols. The related results encouraged us to verify if this compound could be developed as a radiotracer for in-vivo PET in order to visualize sigma(2) receptors expressed in EMT-6 cells when implanted in mice. This perspective was thought to be favourable because PB167 bears a methoxy substituent on the tetraline nucleus, an easy point for (11)C labelling. The aims of this preliminary study were both to assess the relative distribution of sigma(1) and sigma(2) receptors in EMT-6 cells and to verify if PB167 could be developed as a sigma(2) radiotracer for in-vivo PET. The results showed that both sigma(1) and sigma(2) receptors were overexpressed in EMT-6 cells and that the ligand PB167 can be positively considered for radiosynthesis preparation in order to suitably visualize sigma(2) receptors by the in-vivo PET technique and correlate their presence to tumour proliferation.

Colabufo, N., Berardi, F., Contino, M., Fazio, F., Matarrese, M., Moresco, R., et al. (2005). Distribution of sigma receptors in EMT-6 cells: Preliminary biological evaluation of PB167 and potentials for in vivo PET. JOURNAL OF PHARMACY AND PHARMACOLOGY, 57(11), 1453-1460 [10.1211/jpp.57.11.0011].

Distribution of sigma receptors in EMT-6 cells: Preliminary biological evaluation of PB167 and potentials for in vivo PET

FAZIO, FERRUCCIO;MORESCO, ROSA MARIA;
2005

Abstract

Sigma(1) and sigma(2) receptors have been detected in many tissues and are highly expressed in several tumour cell lines from various tissues. The high level of expression observed for sigma receptors and their involvement in cell proliferation and apoptosis has led to the development of several sigma ligands in order to obtain a molecular probe for in-vivo diagnostic imaging techniques such as positron emission tomography (PET) and single photon emission computerized tomography (SPECT). The EMT-6 cells implanted in mice were a good model for evaluating the proliferation of solid tumours by in-vivo PET. Moreover, we developed the sigma ligand PB167, a cyclohexylpiperazine derivative, previously evaluated for sigma(2) receptor affinity and activity in standard protocols. The related results encouraged us to verify if this compound could be developed as a radiotracer for in-vivo PET in order to visualize sigma(2) receptors expressed in EMT-6 cells when implanted in mice. This perspective was thought to be favourable because PB167 bears a methoxy substituent on the tetraline nucleus, an easy point for (11)C labelling. The aims of this preliminary study were both to assess the relative distribution of sigma(1) and sigma(2) receptors in EMT-6 cells and to verify if PB167 could be developed as a sigma(2) radiotracer for in-vivo PET. The results showed that both sigma(1) and sigma(2) receptors were overexpressed in EMT-6 cells and that the ligand PB167 can be positively considered for radiosynthesis preparation in order to suitably visualize sigma(2) receptors by the in-vivo PET technique and correlate their presence to tumour proliferation.
Articolo in rivista - Articolo scientifico
PET sigma receptor, binding
English
2005
57
11
1453
1460
none
Colabufo, N., Berardi, F., Contino, M., Fazio, F., Matarrese, M., Moresco, R., et al. (2005). Distribution of sigma receptors in EMT-6 cells: Preliminary biological evaluation of PB167 and potentials for in vivo PET. JOURNAL OF PHARMACY AND PHARMACOLOGY, 57(11), 1453-1460 [10.1211/jpp.57.11.0011].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/1870
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