Abcam, ab286948, S1RA (E-52862)

Size: 1mg / 5mg
MW 337.4 Da, Purity >98%. A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.
Key facts
CAS number:878141-96-9,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:337.4 Da,
Molecular formula:C20H23N3O2,
PubChem:44247568,
Nature:Synthetic,
Solubility:~10 mg/ml in DMF~1 mg/ml in ethanol~15 mg/ml in DMSO,
Biochemical name:S1RA,
Biological description:A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.,
Canonical smiles:CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4,
InChi:InChI=1S/C20H23N3O2/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19/h2-7,14-15H,8-13H2,1H3,
InChiKey:DGPGXHRHNRYVDH-UHFFFAOYSA-N,
IUPAC Name:4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine

Product details:
This product is manufactured by BioVision, an Abcam company and was previously called B3048 S1RA (E-52862). B3048-1 is the same size as the 1 mg size of ab286948.

Properties and Storage Information:
Shipped at conditions-Blue Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
The 5-HT-2B receptor and Sigma1-receptor are two important protein targets with distinct mechanical roles. The 5-HT-2B receptor also known as the serotonin receptor 2B is a G-protein-coupled receptor with an approximate molecular mass of 54 kDa. Sigma1-receptor alternatively sometimes called the sigma-1 receptor is a chaperone protein that acts on multiple subcellular locations with a mass of about 25 kDa. The 5-HT-2B receptor is often expressed in the heart lungs and gastrointestinal tract while the Sigma1-receptor shows expression in the central nervous system liver and kidneys.
Biological function summary
Serotonin receptor 2B influences cardiovascular function gastrointestinal movement and mood regulation through serotonin signaling. It forms a complex with G-proteins to transduce signals. The Sigma1-receptor plays a role in cellular stress response and maintenance of calcium signaling affecting neuroplasticity and cellular survival. It associates with various ion channels and receptors to modulate their functions.
Pathways
Serotonin receptor 2B takes part in the serotonin signaling cascade which is important for mood disorders and vasoconstriction. It interacts closely with other serotonin receptors notably 5-HT-2A and 5-HT-2C in the same family. The Sigma1-receptor participates in neuroprotection pathways by modulating the activity of the ion channels and receptors related to calcium and potassium having impactful interactions with proteins like N-methyl-D-aspartate (NMDA) receptors.
Serotonin receptor 2B is involved in heart valve disease and pulmonary hypertension conditions where improper serotonin signaling can result in pathogenic vascular remodeling. It can influence heart-related disorders through interactions with proteins like transforming growth factor-beta (TGF-beta). The Sigma1-receptor is linked to neurodegenerative disorders such as Alzheimer's disease and amyotrophic lateral sclerosis (ALS) where its modulation of neuronal survival pathways and calcium homeostasis shows a protective effect relating it with markers like amyloid precursor protein (APP) in Alzheimer's pathology.