title: Early development of sigma-receptor ligands.
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.
authors.affiliation: Departments of Medicinal Chemsitry, School of Pharmacy, The University of Mississippi, MS 38655, USA.
authors.forename: Sanju
authors.initials: S
authors.lastname: Narayanan
authors.forename: Rohit
authors.initials: R
authors.lastname: Bhat
authors.forename: Christophe
authors.initials: C
authors.lastname: Mesangeau
authors.forename: Jacques H
authors.initials: JH
authors.lastname: Poupaert
authors.forename: Christopher R
authors.initials: CR
authors.lastname: McCurdy
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D008024:Ligands; D009369:Neoplasms / Q000188:drug therapy; D009422:Nervous System Diseases / Q000188:drug therapy; D011485:Protein Binding; D017480:Receptors, sigma / Q000378:metabolism*
chemical_list: D008024:Ligands; D017480:Receptors, sigma