Sigma Receptor
Activation of σ–receptors by an agonist ligand may induce hallucinogenic effects and also may be responsible for the paradoxical convulsions sometimes seen in opiate overdose. Drugs known to be σ–agonists include cocaine, morphine/diacetylmorphine, opipramol, PCP, fluoxetine, methamphetamine, dextromethorphan, and the herbal antidepressant berberine. Physiologic effects when the σ–receptor is activated include hypertonia, tachycardia, tachypnea, antitussive effects, and mydriasis. However the exact role of σ–receptors is difficult to establish as many σ–agonists also bind to other targets such as the κ-opioid receptor and the NMDA glutamate receptor. In animal experiments, σ–antagonists such as rimcazole were able to block convulsions from cocaine overdose. σ–antagonists are also under investigation for use as antipsychotic medications.
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PD 144418 oxalate是高亲和性， 选择性 σ1 配体。
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PB 28 dihydrochloride是高亲和性 σ2 激动剂。
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NE 100 hydrochloride是选择性 σ1 拮抗剂。
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N-[2-(Piperidinylamino)ethyl]-4-iodobenzamide是σ1 选择性配体。
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Metaphit是Metaphit is an acylator of PCP and σ receptors。
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