Sigma Receptor Antagonist

Sigma-1 receptor antagonist 7 is a selective sigma-1 receptor antagonist capable of crossing the blood-brain barrier, with an IC₅₀ of 12.7 nM against guinea pig σ1R. Sigma-1 receptor antagonist 7 binds to σ1R, and its binding affinity decreases in the presence of Phenytoin (HY-B0448). Sigma-1 receptor antagonist 7 alleviates mechanical and thermal hyperalgesia induced by acute inflammation in rats. Sigma-1 receptor antagonist 7 can be used for research related to hyperalgesia.

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

Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a K_i value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).

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.

BD-1047 is a selective functional antagonist of sigma receptors. BD-1047 attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches.

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.

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.

Rimcazole dihydrochloride (Standard) is the analytical standard of Rimcazole (dihydrochloride) (HY-108510). This product is intended for research and analytical applications. Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.

BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.

BD-1047 (dihydrobromide) (Standard) is the analytical standard of BD-1047 (dihydrobromide). This product is intended for research and analytical applications. BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches.

Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT_2A (K_i=0.812 nM) and dopamine D2 receptor (K_i =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

IPAG (Standard) is the analytical standard of IPAG (HY-100985). This product is intended for research and analytical applications. IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3. IPAG induces apoptosis.

Zervimesine (Standard) is the analytical standard of Zervimesine (HY-111669). This product is intended for research and analytical applications. 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.

Cinuperone is a multi-target competitive receptor ligand and σ receptor antagonist that acts on Dopamine D1, σ, Dopamine D1, and 5-HT₂ receptors. Cinuperone shows significantly higher affinity for σ receptors than for Dopamine D1 receptors, and only exhibits moderate binding activity for dopamine D2 receptors. Cinuperone can be used in the research of central nervous system diseases.

Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

BMY-14802 hydrochloride (Standard) is the analytical standard of BMY-14802 (hydrochloride) (HY-108509). This product is intended for research and analytical applications. BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC₅₀ of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.

NE-100 hydrochloride (Standard) is the analytical standard of NE-100 hydrochloride (HY-101484A). This product is intended for research and analytical applications. NE-100 hydrochloride is an orally active and selective sigma-1 receptor antagonist with an IC₅₀ of 4.16 nM. NE-100 hydrochloride can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE-100 hydrochloride can be used for research on nervous system diseases.

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.

Opipramol (Standard) is the analytical standard of Opipramol. This product is intended for research and analytical applications. Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a K_i value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).