1. Signaling Pathways
  2. GPCR/G Protein
  3. Sigma Receptor

Sigma Receptor

Sigma receptor is a non-opioid receptor that binds diverse classes of psychotropic drugs. Sigma receptors are subdivided into two subtypes, sigma-1 and sigma-2. The sigma-1 receptor is a 25-kDa protein possessing one putative transmembrane domain and an endoplasmic reticulum retention signal. Sigma-1 receptors are highly expressed in deeper laminae of the cortex, olfactory bulb, nuclei of mesencephalon, hypothalamus, and Purkinje cells in the brain. Sigma-1 receptors are predominantly localized at the endoplasmic reticulum of both neurons and oligodendrocytes. From behavioral studies, sigma-1 receptors were shown to be involved in higher-ordered brain functions including memory and drug dependence. The sigma-2 receptor (σ2R) is a sigma receptor subtype which preferentially binds to siramesine and PB28. PGRMC1 was recently identified as the sigma-2 receptor. Unlike sigma-1 receptor, it has not yet been cloned. Activation of the receptor can cause apoptosis. A pharmacophore model based on benzooxazolone derivatives has been developed.

Sigma Receptor 相关产品 (19):

Cat. No. Product Name Effect Purity
  • HY-13980
    UNC0642 Inhibitor 99.81%
    UNC0642是有效,选择性的 G9a/GLP 抑制剂, IC50值小于2.5 nM。
  • HY-16996A
    BD-1047 dihydrobromide Antagonist 98.18%
  • HY-13510
    Cutamesine dihydrochloride Agonist 98.74%
    Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种有效的 Sigma 1受体激动剂,在豚鼠脑膜中的IC50值为17.4 nM。
  • HY-18100A
    PRE-084 hydrochloride Agonist 99.80%
    PRE-084盐酸盐是一种高亲合性的选择性σ1激动剂, 在sigma受体检测中IC50值为44 nM。
  • HY-13716
    Noscapine Activator
    Noscapine是一种口服止咳药, 主要通过其 σ受体激动剂活性调节, 且Noscapine具有抗癌活性。
  • HY-116463
    E1R Agonist
    E1R 是一种 sigma-1 受体的正变构调节剂,具有认知增强效果。
  • HY-111669
    Sigma-2 receptor antagonist 1 Antagonist
    Sigma-2 receptor antagonist 1 是 sigma-2 (σ-2) 受体拮抗剂。
  • HY-14218
    Ditolylguanidine Agonist 99.26%
    Ditolylguanidine (1,3-Di-o-tolylguanidine; DTG) 是一种 sigma 受体 (σ1/σ2 receptor) 激动剂。
  • HY-18101A
    BD1063 dhydrochloride Antagonist >98.0%
    BD1063 dhydrochloride是有效选择性的sigma 1受体拮抗剂。
  • HY-14221A
    Siramesine hydrochloride Agonist 99.91%
    Siramesine(Lu 28-179)盐酸盐是sigma-2受体激动剂,能引发癌细胞的死亡,并在体内具有抗癌活性。
  • HY-19469
    Roluperidone 98.26%
    Roluperidone (CYR-101) 是一种新型环酰胺衍生物,对 5-HT2Asigma-2 受体具有高亲和力,Ki 分别为 7.53 nM 和 8.19 nM。
  • HY-101864
    AVex-73 hydrochloride Agonist 99.72%
    AVex-73 hydrochloride 是一个 Sigma-1 受体激动剂,其 IC50 值为 860 nM。
  • HY-100155
    4-IBP Agonist 98.90%
    4-IBP是一种选择性σ1 激动剂,高亲和性地结合到σ1 受体 (Ki = 1.7 nM) 对 σ2 受体的亲和力稍弱 (Ki = 25.2 nM) 。
  • HY-18099A
    S1RA hydrochloride Antagonist 99.57%
  • HY-B2215
    Dimemorfan phosphate Agonist 98.42%
    Dimemorfan phosphate 是 sigma 1 receptor 的有效激动剂,能够有效止咳。
  • HY-14813
    Cutamesine Agonist
    Cutamesine (SA4503; AGY-94806) 是一种选择性 sigma 1 受体激动剂,IC50 为 17.4 nM,而对 sigma 2 受体的亲和力低 100 倍。
  • HY-18099
    S1RA Antagonist
  • HY-14221
    Siramesine Agonist
    Siramesine(Lu 28-179)是sigma-2受体激动剂,能引发癌细胞的死亡,并在体内具有抗癌活性。
  • HY-101626
    Sigma-LIGAND-1是σ受体 (sigma receptor) 的选择性配体, 在DTG和PPP位点的 IC50 值分别为16和19 nM,在多巴胺受体D2的 Ki 值为4000 nM。
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