期刊
FUTURE MEDICINAL CHEMISTRY
卷 3, 期 1, 页码 79-94出版社
FUTURE SCI LTD
DOI: 10.4155/FMC.10.279
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资金
- National Institute on Drug Abuse [DA 023205]
- NATIONAL INSTITUTE ON DRUG ABUSE [R01DA023205] Funding Source: NIH RePORTER
Sigma receptors (sigma-1 and sigma-2) are non-opioid proteins implicated in the pathophysiology of various neurological disorders and cancer. The sigma-1 subtype is a chaperon protein widely distributed in the CNS and peripheral tissues. These receptors are involved in the modulation of K+- and Ca2+-dependent signaling cascades at the endoplasmic reticulum and modulation of neurotransmitter release. sigma-1 receptors are emerging targets for the treatment of neurophychiatric diseases (schizophrenia and depression) and cocaine addiction. sigma-2 receptors are lipid raft proteins. They are highly expressed on many tumor cells and hence considered potential targets for anticancer drugs. sigma 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 a receptor-specific ligands and radiolabeling agents.
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