Sigma Receptor Agonist

S1R agonist 2 (Compound 8b) hydrochloride is a selective S1R agonist with K_is of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a K_i of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.

AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease.

CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC₅₀ of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer.

PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC₅₀ of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

AD186 is a potent and selective S1R agonist with K_is of 2.7, 27 nM for S1R and S2R, respectively. AD186 fully reverses the antiallodynic effect of BD-1063 (HY-18101A).

(±)-PPCC is a sigma-1 agonist that mainly interacts with sigma-1 receptors with K_i of 1.5 nM. (±)-PPCC has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.

Blarcamesine hydrochloride (Standard) is the analytical standard of Blarcamesine hydrochloride (HY-101864). This product is intended for research and analytical applications. Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC₅₀ of 860 nM.

4-IBP (Standard) is the analytical standard of 4-IBP (HY-100155). This product is intended for research and analytical applications. 4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research.

Blarcamesine (Standard) is the analytical standard of Blarcamesine (HY-105296). This product is intended for research and analytical applications. Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.

Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

Igmesine (JO 1784) is a selective σ-1 receptor agonist (IC₅₀ = 39 nM) with oral activity and blood-brain barrier penetration. Igmesine stimulates duodenal bicarbonate secretion in rats via a σ1/vagal/CCK-A-dependent pathway, without antisecretory activity. Igmesine centrally blocks CRF-mediated gastrin-inhibitory effects, and in TMT toxicity and MCAO focal ischemia models, it downregulates PTBBS, reduces NOS, and modulates M1/M2 density. Igmesine is used in research on duodenal ulcers, Alzheimer's disease, and related diseases.

Oxeladin (citrate) (Standard) is the analytical standard of Oxeladin (citrate). This product is intended for research and analytical applications. Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research.

Cutamesine dihydrochloride (Standard) is the analytical standard of Cutamesine dihydrochloride. This product is intended for research and analytical applications. Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.