Sigma Receptor Ligand

4-Phenylpiperidine is a σ receptor ligand with a K_i value of 1980 nM for guinea pig σ receptors. 4-Phenylpiperidine binds to σ receptors. 4-Phenylpiperidine is used in psychiatric disease research.

CM398 is a highly selective, orally active Sigma-2 receptor ligand with a K_i value of 0.43 nM. CM398 ameliorates age-related macular degeneration. CM398 exerts analgesic effects on visceral pain, inflammatory pain and neuropathic pain. CM398 can be used in research related to age-related macular degeneration, neuropathic pain and inflammatory pain.

(+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ₁ receptor ligand with an IC₅₀ of 39 nM. (+)-Igmesine hydrochloride binds σ₁ receptors to activate G-proteins and modulate Ca²⁺ uptake. (+)-Igmesine (hydrochloride) attenuates ischaemia-induced nitric oxide synthase activity and hyperactivity. (+)-Igmesine hydrochloride can be used for the research of duodenal ulcers, gastric ulcers, and cerebral ischaemia.

Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective Sigma-2 receptor ligand with a K_i value of 40 nM. Sigma-2 Receptor ligand 1 is promising for research of Alzheimer's disease.

SV119 is a selective sigma-2 (σ₂) receptor ligand (K_i ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer.

SAS-1121 is a subtype-selective sigma 2 receptor/PGRMC1 ligand with a K_i of 16.2 nM. SAS-1121 is 574-fold selective for the signma 2 receptor over the sigma 1 receptor. SAS-1121 is a tertiary amine. SAS-1121 can be studied in neurology-related research.

Caprospinol (SP-233) is a steroid compound candidate based on the structure of 22R-hydroxycholesterol. It has multiple mechanisms of neuroprotection, including binding to β-amyloid protein (Aβ(42)), interacting with the mitochondrial respiratory chain, clearing Aβ(42) monomers, and acting as a σ-1 receptor ligand. It can cross the blood-brain barrier in vivo and restore cognitive impairment, and has the potential to inhibit Alzheimer's disease.

E-5842 citrate is a σ receptor ligand (K_i: 4 nM for σ1 receptor). E-5842 citrate increases levels of Fos in the medial prefrontal cortex and the nucleus accumbens, without affecting the levels of the protein in the striatum. E-5842 citrate can be used in the research of psychiatric disorders.

MS-377 is a selective and orally active sigma-1 receptor ligand (K_i=73 nM) with weak affinity for sigma-2 receptor (K_i=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (K_i: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia.

SV119 hydrochloride is a sigma-2 ligand with a K_i value of 5.2 nM. SV119 hydrochloride enhances the efficient transport of drugs across the plasma membrane of cancer cells. The conjugation of dm-Erastin with SV119 hydrochloride successfully overcomes the internalization barrier observed in pancreatic cancer, while preserving the inherent anti-tumor activity of Erastin (HY-15763). Additionally, SV119 hydrochloride demonstrates cytotoxic effects on triple-negative breast cancer (TNBC) cells and induces apoptosis.