Sigma 2 Receptor Antagonist

Zervimesine (CT1812) is an orally active and brain penetrant sigma-2 receptor antagonist with a K_i of 8.5 nM. Zervimesine can be used for the research of Alzheimer’s disease.

JVW-1009 is a Sig2R/PGRMC1 antagonist (Sig1R K_i = 96 nM; Sig2R K_i = 70 nM). JVW-1009 acts as a neuroprotective agent. JVW-1009 can be used in the research of Alzheimer's disease.

S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with K_is of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice.

BD-1008 is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor.

BD-1008 dihydrobromide is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor.

AB10 is a selective S1R antagonist. AB10 with K_i of 10, 165 nM for S1R and S2R, respectively. AB10 reverses the effect of Capsaicin (HY-10448) caused pain in model.

AB21 is a potent and selective S1R antagonist with K_is of 13, 102 nM for S1R and S2R. AB21 has the effect of reducing mechanical hypersensitivity.

UMB24 is a potent antagonist of σ2 receptor, with K_i values of 170 nM anf 322 nM for σ2 receptor and σ1 receptor, respectively. UMB24 attenuats cocaine-induced convulsions and locomotor activity, but not lethality.

σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a K_i of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (K_i of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters.