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Substituted norbenzomorphans are known to display high affinity and selectivity for the two sigma receptor (σR) subtypes. In order to study the effects of simplifying the structures of these compounds, a scaffold hopping strategy was used to design several novel sets of substituted isoindolines, tetrahydroisoquinolines and tetrahydro-2-benzazepines. The binding affinities of these new compounds for the sigma 1 (σ1R) and sigma 2 (σ2R) receptors were determined, and some analogs were identified that exhibit high affinity (K ≤ 25 nM) and significant selectivity (>10-fold) for σ1R or σ2R. The preferred binding modes of selected compounds for the σ1R are predicted by modeling studies, and the nature of substituents on the aromatic ring and the nitrogen atom of the bicyclic skeleton appears to affect the preferred binding orientation of σ1R-preferring ligands.
This article was published in the following journal.
Name: European journal of medicinal chemistry
Sigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 rec...
The P2Y receptor is one of eight known P2Y receptor subtypes, and belongs to the G-protein-coupled receptor (GPCR) family. The P2Y receptor is highly expressed on blood platelets and in the brain. Pot...
The sigma-1 (σ) receptor is a chaperone protein located on the mitochondria-associated membrane of the endoplasmic reticulum, while the sigma-2 receptor (σ) is an endoplasmic reticulum-resident memb...
The histamine H receptor is a G protein-coupled receptor (GPCR) drug target that is highly expressed in the CNS, where it acts as both an auto- and hetero-receptor to regulate neurotransmission. As su...
The use of liquid chromatography coupled with mass spectrometry (LC-MS/MS) is advantageous in in-vivo receptor occupancy assays at pre-clinical drug developmental stages. Relatively, its application i...
The main objective of this study is to determine if the P.F.C. Sigma RP-F Knee delivers a greater post-operative range of motion (ROM) compared with the P.F.C. Sigma RP Knee in primary TKA...
The primary objective of this investigation is to evaluate the performance (in terms of post-operative active range of motion at one year) of the P.F.C. Sigma and P.F.C. Sigma Rotating Pla...
Comparison of two unicompartmental knee arthroplasties (UKA), to see if Sigma UKA performs equally good as the Oxford UKA. The study focuses on how well the arthroplasty is fixated to the ...
Chronic pain can result from injured or inflamed nerves, as happens in people suffering from sciatica and CRPS. These nerve injuries or regions of nerve irritation are often the cause of p...
Evaluate the feasibility of using a novel imaging test, [18F]ISO-1 PET/CT to image sigma-2 receptor binding in cancer. Correlate uptake with standard and experimental pathology assays of b...
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
A DNA-directed RNA polymerase found in BACTERIA. It is a holoenzyme that consists of multiple subunits including sigma factor 54.
The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)
A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE.
Specific sites or molecular structures on cell membranes or in cells with which phencyclidine reacts or to which it binds to elicit the specific response of the cell to phencyclidine. Studies have demonstrated the presence of multiple receptor sites for PCP. These are the PCP/sigma site, which binds both PCP and psychotomimetic opiates but not certain antipsychotics, and the PCP site, which selectively binds PCP analogs.