sigma 1 receptor antagonist 2

Sigma-1 receptor antagonist 2 是有效的sigma 1受体选择性拮抗剂，与 σ1 和 σ2 受体结合的Ki 分别为 3.88 和 1288 nM。

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

Pridopidine (FR310826) 是多巴胺稳定剂，是一种低亲和力的多巴胺 D2 受体拮抗剂。它高亲和力作用于 sigma 1受体，Ki=70-80 nM，比其对 D2R 的亲和力高约 100 倍。

KSK68 是一种高效的 sigma-1 和 组胺 H3 受体双重拮抗剂，具有潜在的镇痛活性，对 H3 受体、sigma-1、sigma-2 受体有很高的亲和力。KSK68 可用于研究与疼痛相关的疾病。

KSK94 是一种特异性 H3 受体拮抗剂，抑制 H3、sigma-1、sigma-2受体 ，Ki值分别是7.9、2958 和 75.2 nM，可用于研究伤害性疼痛和神经性疼痛。

S1RA (E-52862) 是一种有效且特异性的 sigma-1受体拮抗剂，Ki 为17nM，对 σ2R 具有良好的选择性，Ki 值大于 1000 nM。

BD 1008 dihydrobromide 是 sigma 1 (σ1) 受体 (Ki = 2 nM) 的选择性拮抗剂。 它对 sigma1 受体具有高亲和力，对 sigma2 受体具有中等亲和力。 它通过拮抗 σ 受体减弱可卡因的毒性和刺激作用。

PB28 is a cyclohexylpiperazine derivative that functions as a potent and highly selective agonist of the sigma 2 (σ2) receptor, exhibiting a Ki (binding affinity) of 0.68 nM. At the same time, PB28 acts as an antagonist of the sigma 1 (σ1) receptor, with a Ki of 0.38 nM. PB28 demonstrates a lower affinity for other receptors. It effectively inhibits electrically evoked twitch in both the guinea pig bladder (EC50 value of 2.62 μM) and ileum (EC50 value of 3.96 μM). Moreover, PB28 exhibits the ability to modulate protein-protein interaction between SARS-CoV-2 and human cells. Additionally, PB28 triggers caspase-independent apoptosis and possesses significant antitumor activity.

BD 1008 Free Base is a selective sigma receptor antagonist, with a reported binding affinity of Kᵢ = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor.