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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(+)-SK&F 10047 hydrochloride是σ1 选择性 激动剂。
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(+)-Igmesine hydrochloride是选择性 σ1 配体， antidepressant activity。
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threo Ifenprodil hemitartrate是NR2B-选择性NMDA拮抗剂，也是 σ 激动剂。
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SA 4503 dihydrochloride是选择性 σ1 受体激动剂。
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Rimcazole dihydrochloride是σ2 拮抗剂。 也是DAT的抑制剂。
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