Sigma 1 Receptor Ligand

(+)-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.

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.