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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BD 1008 dihydrobromide是活性的， 选择性 σ 配体。
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4-PPBP maleate是特异性 σ 配体， NMDA 拮抗剂。
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4-IBP是σ 配体， σ1 > σ2。
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2-MPMDQ是活性的， 选择性 α1 拮抗剂。也是σ2 配体。
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(±)-PPCC oxalate是Selective sigma (σ) 激动剂 (σ1> σ2)。
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