Sigma-1 receptor ligand

C.S. Dence, C.S. John, W.D. Bowen, M.J. Welch, Synthesis and evaluation of [F-18] labeled benzamides High affinity sigma receptor ligands for PET imaging, Nucl. Med. Biol. 24 (1997) 333-340. 

Zamanillo D, Andreu F, Ovalle S, Perez MP, Romero G, et al. 2000. Up-regulation of sigma(l) receptor mRNA in rat brain by a putative atypical antipsychotic and sigma receptor ligand. Neurosci Lett 282 169-172. 

Many other GPCRs mediate the effects of hormones and NTs involved in a wide variety of responses. Some of these are also targets for plant defensive compounds (Table 5.8) and are listed alphabetically for convenience in the outline presented below. Note that all of the hormones listed below are peptides except for (a) ATP, (c) anandamide, (j) melatonin and (p) some non-peptide sigma receptor ligands. 

Sigma receptor ligands bind to metabotropic GPCRs as well as ionotropic cr-Rs (Chapter 3). Endogenous ligands for cr-Rs include some opiates. Sigma-R activation can have antitussive, anxiolytic and ulceroprotective effects. Hypericin from Hypericum perforatum (St John s wort) is... 

Steinfels GF, Alberici GP, Tam SW. et al. Biochemical, behavioral, and electrophysiologic actions of the selective sigma receptor ligand (+)-pentazocine. Neuropsychopharmacology 1998 1 321-7. 

For an update on the structure-activity-relationships of sigma receptor ligands see de Costa BR, He XS in Itzhak J, Chapman C, eds. The Sigma Receptors. London Academic Press, 1994 45-111. 

Bowen, W.D., Jin, B., Blann, E., Vilner, B.J., Lyn-Cook, B.D., 1997. Sigma receptor ligands modulate expression of the multidrug resistance gene in human and rodent brain tumor cell lines. Proceedings of the American Association for Cancer Research 38 (3206), 479. 

McCracken, K.A., Bowen, W.D., de Costa, B.R., Matsumoto, R.R., 1999. Two novel sigma receptor ligands, BD1047 and LR172, attenuate cocaine-induced toxicity and locomotor activity. Eur. J. Pharmacol. 370, 225-232. 

Vilner, B.J., Bowen, W.D., 1995. Dual modulation of cellular calcium by sigma receptor ligands release from intracellular stores and blockade of voltage-dependent influx. Society for Neuroscience Abstracts 21 (631.3), 1608. 

Waterhouse RN, Chapman J, Izard B, Donald A, Belbin K, O Brien JC, Collier TL. Examination of four I-labeled piperidine-based sigma receptor ligands as potential melanoma imaging agents initial studies in mouse tumor models. Nucl Med Biol 1997 24 587-593. 

Berardi F, Ferorelli S, Abate C, Colabufo NA, Contino M, Perrone R, Tortorella V. 4-(Tetralin-l-yl)- and 4-(naphthalen-l-yl)alkyl derivatives of 1-cyclohexylpipera-zine as sigma receptor ligands with agonist sigma2 activity. J Med Chem 2004 47 2308-2317. 

Gewirtz GR, Gorman JM, Volavka J, Macaluso J (1994) BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology 10 37 0... 

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