1. GPCR/G Protein
  2. 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 (16):

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-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-16996A
    BD-1047 dihydrobromide Antagonist >98.0%
    BD-1047二氢溴酸盐是sigma受体选择性拮抗剂,作用于精神分裂症动物模型,具有抗精神病活性。
  • HY-18100A
    PRE-084 hydrochloride Agonist 99.79%
    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-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 99.60%
    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%
    MIN-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 >98.0%
    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%
    S1RA(E-52862)盐酸盐是高活性和选择性的sigma-1受体(σ1R)拮抗剂,Ki为17nM,而对σ2R的Ki则高于1000nM。
  • 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
    SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  • HY-18099
    S1RA Antagonist
    S1RA(E-52862)是高活性和选择性的sigma-1受体(σ1R)拮抗剂,Ki为17nM,而对σ2R的Ki则高于1000nM。
  • 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
    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。
Isoform Specific Products

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.