Early development of sigma-receptor ligands
(2011) Future Medicinal Chemistry — Vol. 3, n° 1, p. 79-94 (2011)
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- Abstract
- Sigma receptors (σ-1 and σ-2) are non-opioid proteins implicated in the pathophysiology of various neurological disorders and cancer. The σ-1 subtype is a chaperon protein widely distributed in the CNS and peripheral tissues. These receptors are involved in the modulation of K(+)- and Ca(2+)-dependent signaling cascades at the endoplasmic reticulum and modulation of neurotransmitter release. σ-1 receptors are emerging targets for the treatment of neurophychiatric diseases (schizophrenia and depression) and cocaine addiction. σ-2 receptors are lipid raft proteins. They are highly expressed on many tumor cells and hence considered potential targets for anticancer drugs. σ receptors bind to a diverse class of pharmacological compounds like cocaine, methamphetamine, benzomorphans like (±)-pentazocine, (±)-SKF-10,047 and endogenous neurosteroids and sphingolipids. In this review we focus on the early development of σ receptor-specific ligands and radiolabeling agents.
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Narayanan, S., Bhat, R., Mésangeau, C., Poupaert, J., & McCurdy, C. R. (2011). Early development of sigma-receptor ligands. Future Medicinal Chemistry, 3(1), 79-94. https://doi.org/10.4155/fmc.10.279 (Original work published 2011)