Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
46 Results for "
Sigma-receptor
" in MedChemExpress (MCE) Product Catalog:
Products (46)
46 Results for "Sigma-receptor" in MCE Product Catalog:
12
12 Publications Verification
Cat. No.: HY-16996A
CAS No.: 138356-21-5
Target:
Research Areas:
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 .
2
2 Cited Publications
Synonyms: 1,3-Di-o-tolylguanidine; DTG
Target:
Research Areas:
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer .
Target:
Research Areas:
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 Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
Target:
Research Areas:
BD-1008 is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 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 .
Synonyms: BW 234U dihydrochloride
Target:
Research Areas:
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 .
Cat. No.: HY-155887
CAS No.: 474922-26-4
Synonyms: DSPE-PEG-NH2, MW 3400 ammonium
Synonyms: EMD 57445
Target:
Research Areas:
Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
Target:
Research Areas:
OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .
Target:
Research Areas:
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics .
Cat. No.: HY-169914
CAS No.: 130152-35-1
Synonyms: JO 1784 hydrochloride
Target:
Research Areas:
Igmesine hydrochloride (JO 1784) is an orally active σ-receptor ligand capable of blocking the increase in colonic electromechanical activity induced by emotional stress. Igmesine hydrochloride also eliminates the colonic motility stimulation induced by dopamine, as well as the stimulation induced by centrally injected D1 or D2 receptor agonists. Furthermore, Igmesine hydrochloride can block the colonic motility responses induced by corticotropin-releasing factor (CRF) and ES through central cholecystokinin (CCK) release and/or activation of supraspinal CCK pathways .
Cat. No.: HY-173475
CAS No.: 1259949-84-2
Target:
Research Areas:
CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively .
Cat. No.: HY-47228
CAS No.: 113594-64-2
Target:
Research Areas:
KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent .
Target:
Research Areas:
BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis 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 (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 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 .
Cat. No.: HY-107047
CAS No.: 444667-97-4
Synonyms: RS-1259
Target:
Cholinesterase (ChE) Serotonin Transporter 5-HT Receptor Calcium Channel Sodium Channel Sigma Receptor
Research Areas:
BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease .
Research Areas:
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.
Cat. No.: HY-120360
CAS No.: 157752-20-0
Target:
Research Areas:
CB-64D is the agonist for sigma receptor 2 and sigma receptor 1 with Ki of 16.5 and 3063 nM. CB-64D induces apoptosis in cancer cell SK-N-SH .
Cat. No.: HY-130179
CAS No.: 1346016-43-0
Target:
Research Areas:
RC-33 hydrochloride is a selective and metabolically stable σ receptor agonist with activity in enhancing nerve growth factor (NGF)-induced neurite outgrowth. Both enantiomers of RC-33 hydrochloride bind to the σ receptor with similar affinity and show almost equal effectiveness as σ receptor agonists. The R-configured enantiomer of RC-33 hydrochloride shows higher liver metabolic stability in the presence of NADPH. RC-33 hydrochloride was selected as the best candidate for further in vivo studies in animal models of amyotrophic lateral sclerosis .
Cat. No.: HY-120236
CAS No.: 1415247-18-5
Target:
Research Areas:
KSCM-5 is a sigma receptor ligand with high affinity activity on sigma-1 receptor. The Ki value of KSCM-5 is about 34nM, showing significant selectivity. KSCM-5 has potential application value in compound development, especially for diseases related to sigma receptors .
Cat. No.: HY-19120
CAS No.: 129200-10-8
Target:
Research Areas:
KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
