TY - JOUR. T1 - Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents. AU - Rui, Marta. AU - Rossi, Daniela. AU - Marra, Annamaria. AU - Paolillo, Mayra. AU - Schinelli, Sergio. AU - Curti, Daniela. AU - Tesei, Anna. AU - Cortesi, Michela. AU - Zamagni, Alice. AU - Laurini, Erik. AU - Pricl, Sabrina. AU - Schepmann, Dirk. AU - Wűnsch, Bernhard. AU - Urban, Ernst. AU - Pace, Vittorio. AU - Collina, Simona. PY - 2016/11/29. Y1 - 2016/11/29. N2 - In the early 2000s, the Sigma Receptor (SR) family was identified as potential "druggable" target in cancer treatment. Indeed, high density of SRs was found in breast, lung, and prostate cancer cells, supporting the idea that SRs could play a role in tumor growth and progression. Moreover, a link between the degree of SR expression and tumor aggressiveness has been postulated, justified by the presence of SRs in high metastatic-potential cancer cells. As a ...
2,5-Dimethoxyphenethyl isothiocyanate chemical properties, What are the chemical properties of 2,5-Dimethoxyphenethyl isothiocyanate 56771-74-5, What are the physical properties of 2,5-Dimethoxyphenethyl isothiocyanate ect.
PubMed Central Canada (PMC Canada) donne libre accès en ligne à des archives numériques fiables et permanentes qui contiennent le texte intégral de publications de recherches évaluées par des pairs en santé et en sciences de la vie. Il fait fond sur PubMed Central (PMC), les archives numériques gratuites des National Institutes of Health (NIH) des États-Unis qui proviennent de revues biomédicales et sur les sciences de la vie, et il est membre du réseau élargi PMC International (PMCI).
Clobenpropit dihydrobromide | H3 antagonist | VUF 9153 dihydrobromide | VUF9153 | VUF-9153 | CAS [145231-35-2] - [145231-45-4] | Axon 1209 | Axon Ligand™ with >99% purity available from supplier Axon Medchem, prime source of life science reagents for your
AnavexLifeSci Anavex Life Sciences Reports Potential Normalization of Hypertension with ANAVEX®2-73 Published in The Journal of C… twitter.com/i/web/status/9… ...
ONEILL, M,CALDWELL, M,EARLEY, B,CANNEY, M,OHALLORAN, A,KELLY, J,LEONARD, BE,JUNIEN, JL (1995) THE SIGMA-RECEPTOR LIGAND JO-1784 (IGMESINE-HYDROCHLORIDE) IS NEUROPROTECTIVE IN THE GERBIL MODEL OF GLOBAL CEREBRAL-ISCHEMIA. European Journal Of Pharmacology, 283 :217-225 [Details] ...
BioAssay record AID 204454 submitted by ChEMBL: In vitro binding affinity towards sigma receptor by the displacement of [3H]PPP from guinea pig brain.
6-[6-(4-Hydroxypiperidinyl)hexyloxy]-3-methylflavone HCI (NPC 16377), a structurally novel compound, was found to be a highly potent and selective ligand for sigma-sites. Although 5-fold less potent than haloperidol and 2-fold less potent than ifenprodil to inhibit 1,3-di-o-tolylguanidine binding, NPC 16377 (IC50 = 36 nM) was more potent than alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinyl butanol (BMY 14802), rimcazole and the atypical antipsychotic, clozapine. A similar rank order of potency was observed when [3H](+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperdine was used as the radioligand. Like BMY, rimcazole and clozapine, NPC 16377 (IC50 = 2671 nM) had low affinity for dopamine type 2 receptors. Additionally, the compound was only weakly active in 35 additional receptor binding assays including those for serotonin2 and serotonin1C receptors. In vivo, NPC 16377 potently inhibited the binding of [3H]-(+)-N-allylnormetazocine to sigma sites after both intraperitoneal and oral ...
Sigma receptors, both Sigma‐1(S1R) and Sigma‐2 (S2R), are small molecule‐regulated, primarily endoplasmic reticulum (ER) membrane‐associated sites
AnavexLifeSci Anavex Life Sciences Reports Potential Normalization of Hypertension with ANAVEX®2-73 Published in The Journal of C… twitter.com/i/web/status/9… ...
74037-97-1 - YGTQTFSRQACJSV-UHFFFAOYSA-N - Piperazine, 4-methyl-1-(1-phenylbutyl)-, hydrochloride - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Phosphonic acid, (3-hydroxy-1-phenylbutyl)-, diethyl ester | C14H23O4P | CID 71385097 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
4-Hydroxy-3-(3-oxo-1-phenylbutyl)-2H-1-benzopyran-2-one - chemical information, properties, structures, articles, patents and more chemical data.
2H-1-Benzopyran-2-one,4,6-dihydroxy-3-(3-oxo-1-phenylbutyl)-/ACM17834025 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
CAS: 1174661-92-7 Chemical Name: (±)-[1(S),2-alpha,5-beta]-4-[[2,5-Dimethyl-4-(2-propenyl)-1-piperazinyl](3-hydroxyphenyl)methyl]-N,N-diethylbenzamide dihydrobromide ...
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take your medicine at regular intervals. Do not take your medicine more often than directed.. Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 6 years of age for selected conditions, precautions do apply.. Patients over 65 years old may have a stronger reaction and need a smaller dose.. ...
Tell your doctor or healthcare professional if your symptoms do not start to get better or if they get worse.. You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.. ...
Tell your doctor or healthcare professional if your symptoms do not start to get better or if they get worse.. You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.. ...
DI-fusion, le Dépôt institutionnel numérique de lULB, est loutil de référencementde la production scientifique de lULB.Linterface de recherche DI-fusion permet de consulter les publications des chercheurs de lULB et les thèses qui y ont été défendues.
A central tenet in support of research reproducibility is the ability to uniquely identify research resources, i. include Research Resource Identifiers (RRIDs) MEK162 in their articles prior to publication for three resource types: antibodies, model organisms, and tools (i.e., software and databases). RRIDs are assigned by an authoritative database, for example, a model organism database for each type of resource. To make it less difficult for authors to obtain RRIDs, resources were aggregated from the appropriate databases and their RRIDs made available in a central Web portal (http://scicrunch.org/resources). RRIDs meet three key criteria: they are machine\readable, free Rabbit Polyclonal to MRPS36. to generate and access, and are consistent across publishers and journals. MEK162 In Feb of 2014 and over 300 content have got appeared that record RRIDs The pilot premiered. The accurate amount of publications taking part provides extended from the initial 25 to a lot more than 40, with RRIDs ...
E-52862, also known as S1RA, is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. In preclinical studies, S1RA has demonstrated efficacy in relieving neuropathic pain and pain in other sensitizing conditions, associated with an improvement of the emotional negative state. E-52862 attenuates neuropathic pain of different aetiology in rats.
In vitro studies Gene mutations A key study on 1,4-benzenediamine, N,N-mixed Ph and tolyl derivs. for gene mutations (Ames reverse mutation test) was performed according to the GLP guidelines and OECD guideline 471 (Stanikowski, 1993). In this main study 5 strains of Salmonella typhimurium and one strain of Escherichia coli were treated with test substance, using the pre-incubation methodology in the absence and in the presence of Aroclor 1254 induced rat liver S9. The top concentration was 1000 microgram/plate but no bacterial growth was already evidenced at the concentration of 167 µg/plate with all the Salmonella strains in the absence and in the presence of S9. However, with Escherichia coli, 1,4-benzenediamine, N,N-mixed Ph and tolyl derivs. could be tested up to 1000 µg/plate showing slight to moderate toxicity. Although most of the strains showed no increased levels of mutation in the main experiment, the strains TA1538 and TA98 in the first experiment, and the strain TA1538 in the ...
Anavex Life Sciences Corp. ("Anavex" or the "Company") (OTCQB: AVXL) has announced that the current issue of the peer-reviewed scientific journal PLOS ONE explains that sigma-1 receptor (Sig-1R) activity is involved in cellular survival by regulating and stabilizing a key cell stress sensor… Read & Research Alzheimers More. ...
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Structure, properties, spectra, suppliers and links for: N-Benzyl-N-(2-phenylethyl)-1-(3-phenylpropyl)-4-piperidinecarboxamide ethanedioate (1:1).
usr/bin/perl -w use Crypt::OpenPGP; use Crypt::OpenPGP::KeyRing; my($keyfile, $email) = @ARGV; my $ring = Crypt::OpenPGP::KeyRing-,new(Filename =, $keyfile); my $pgp = Crypt::OpenPGP-,new(PubRing =, $ring); my $kb = $ring-,find_keyblock_by_uid($email); my $alg = $kb-,preferred_sk_alg; my $crypt = $pgp-,encrypt( Data =, squeamish ossifrage, Recipients =, [ $email ], Armour =, 1, ($alg ? (Cipher =, $alg) : ()), # use default if no preference loc +ated ); print $crypt; exit 0; { package Crypt::OpenPGP::KeyBlock; sub preferred_sk_alg { my $self = shift; use Crypt::OpenPGP::Cipher; my $supported = Crypt::OpenPGP::Cipher-,supported; my @prefs; for my $sig (@{ $self-,get(Crypt::OpenPGP::Signature) }) { if ($sig-,is_primary) { unshift @prefs, @{ $sig-,preferred_sk_alg }; } else { push @prefs, @{ $sig-,preferred_sk_alg }; } } for (@prefs) { return $_ if $supported-,{$_}; } return; } } { package Crypt::OpenPGP::Signature; sub is_primary { my $self = shift; my $packet = $self-,find_subpacket(25); # ...
Please register to see prices including your discount. Registration may take up to 24h. For guest orders the standard discount of your institution will apply and discounts are visible on the order confirmation.. ...
Gentaur molecular products has all kinds of products like :search , Zyagen \ Bovine Colon cDNA \ BD-311 for more molecular products just contact us
Learn about the potential side effects of brompheniramine/carbetapentane/phenylephrine. Includes common and rare side effects information for consumers and healthcare professionals.
Learn about the potential side effects of carbetapentane/chlorpheniramine/phenylephrine. Includes common and rare side effects information for consumers and healthcare professionals.
N,N-DI-1 NAPHTHYLGUANIDINE HCL (NAGH) AND N,N-DI-P-NITROPHENYLGUANIDINE HCL (NAD) TREATMENT FOR STROKE AT DELAYED TIMEPOINTS - A composition and method of treating stroke by administration of a novel sigma agonist is presented. Twenty-four hours after MCAO, systemic administration of several novel sigma agonists including: Bromo-DTG; Chloro-DTG; N,N′-di-1-Naphthylguanidine hydrochloride (NAGH); N,N′-di-p-Nitrophenylguanidine HCL (NAD) or vehicle were injected subcutaneously daily for 3 days. Rats treated with Bromo-DTG and Chloro-DTG had no significant improvements in any of the motor or cognitive tests while NAGH treated rats showed improved vertical movement and had significantly less motor asymmetry and bias than vehicle treated rats. Sigma receptor agonist NAGH also was found to exert its long-term neuroprotective effects by preserving both gray matter and white matter tracts. Both NAD and NAGH, when administered 24 hours after experimental stroke, reduced neural damage and enhanced ...
TY - JOUR. T1 - Sigma receptor 1 modulates endoplasmic reticulum stress in retinal neurons. AU - Ha, Yonju. AU - Dun, Ying. AU - Thangaraju, Muthusamy. AU - Duplantier, Jennifer. AU - Dong, Zheng. AU - Liu, Kebin. AU - Ganapathy, Vadivel. AU - Smith, Sylvia B.. PY - 2011/1/1. Y1 - 2011/1/1. N2 - PURPOSE. To investigate the mechanism of σ receptor 1 (σR1) neuroprotection in retinal neurons. METHODS. Oxidative stress, which is implicated in diabetic retinopathy, was induced in mouse primary ganglion cells (GCs) and RGC-5 cells, and the effect of the σR1 ligand (+)-pentazocine on pro- and anti-apoptotic and endoplasmic reticulum (ER) stress gene expression was examined. Binding of σR1 to BiP, an ER chaperone protein, and σR1 phosphorylation status were examined by immunoprecipitation. Retinas were harvested from Ins2Akita/+ diabetic mice treated with (+)-pentazocine, and the expression of ER stress genes and of the retinal transcriptome was evaluated. RESULTS. Oxidative stress induced the ...
The flat surface spheroid migration assay suggested that siramesine killed migrating glioma cells. PI uptake in migrating tumor cells already detached from the spheroids was seen and there was a significant decrease in spheroid migration distance. Part of this decrease may also be explained by tumor cell death in the spheroid itself. In the organotypic 3D migration assay distance of invasion was not affected by siramesine in any of the cultures. However, some of the migrating tumor cells appeared to have lost their membrane protrusions, appearing as small rounded cells suggesting a stop in migration. These cells were primarily seen at concentrations of 100 μM siramesine being however toxic to the brain tissue and thus irrelevant in a clinical setting. It could be speculated if the lack of effect of siramesine on implanted invasive spheroids was due to a phenotypic migration-related shift making the tumor cells siramesine resistant. A phenotypic shift has previously been described as part of the ...
The effect of phencyclidine (PCP) on carbachol-induced phosphoinositol hydrolysis was examined in rat brain slices taken from cortex, caudate-putamen and hippocampus. In all three regions studied, PCP significantly inhibited carbachol-induced [3H]inositol phosphate accumulation working as low as 10(-6) M in the cerebral cortex. Because PCP has been shown to act at two sites, a PCP-site and a sigma site, various PCP-like agonists [levoxadrol (Lev), dexoxadrol (Dex) and MK-801 [(+)-5-methyl-10,11-dihydro- 5H-dibenzo(a,b)cyclo-hepaten-5, 10-imine maleate]] as well as sigma agonists [(+)-SKF10047 and 1,3-di(2-toly)guanidine (DTG) were examined for their effects on carbachol-induced phosphoinositol hydrolysis. All but MK-801 significantly inhibited the carbachol action; however, their order of potencies, Lev greater than or equal to Dex much greater than PCP greater than or equal to DTG greater than or equal to (+)-SKF10047 differed from those of other known PCP interactions at PCP and sigma sites. ...
Take this medicine by mouth. Follow the directions on the prescription label. Shake well before using. Use a specially marked spoon or dropper to measure each dose. Ask your pharmacist if you do not have one. Household spoons are not accurate. Take your medicine at regular intervals. Do not take it more often than directed.. Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 2 years old for selected conditions, precautions do apply.. Patients over 60 years old may have a stronger reaction and need a smaller dose.. ...
Take this medicine by mouth. Follow the directions on the prescription label. Shake well before using. Use a specially marked spoon or dropper to measure each dose. Ask your pharmacist if you do not have one. Household spoons are not accurate. Take your medicine at regular intervals. Do not take it more often than directed.. Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 2 years old for selected conditions, precautions do apply.. Patients over 60 years old may have a stronger reaction and need a smaller dose.. ...
Visit your doctor or health care professional for regular check ups. Tell your doctor if your symptoms do not improve or if they get worse.. Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.. This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.. You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.. ...
Visit your doctor or health care professional for regular check ups. Tell your doctor or healthcare professional if your symptoms do not start to get better or if they get worse.. Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.. This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.. You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.. ...
Tell your doctor or healthcare professional if your symptoms do not start to get better or if they get worse. If you have a fever, skin rash, or persistent headache as well as a cough, see your doctor or health care professional.. You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.. ...
If you are having a medical emergency, call 911 or seek emergency medical help immediately.. We will contact you within 2-3 business days to review your appointment request. Do not use for immediate or urgent care needs. Some specialties may require a referral from a primary care provider prior to scheduling an appointment.. ...
1,3-Di-o-tolylguanidine 97-39-2 Precursor and Downstream products, 1,3-Di-o-tolylguanidine Precursor products, 1,3-Di-o-tolylguanidine Downstream products ect.
Since axons were disrupted in the ONH of the older σR1 −/− mice, we asked whether there was evidence of apoptosis in the RGCs, the source of these axons, in the σR1-null mice. Ultrastructural examination of the GCL showed that the σR1 +/+ mice (age 59 weeks) had normal-appearing neurons; cell bodies were plump, and there was no evidence of apoptotic cell death (Figs. 9A, 9C) consistent with the TUNEL assay data described above (Figs. 7A, 7D). Retinas of the age-matched σR1 −/− mice showed cell dropout and apoptosis in the GCL (Figs. 9B, 9D). These data were confirmed by immunohistochemical detection of active caspase-3 in the GCL of the 1-year-old σR1 −/− mice (Fig. 9H), which was not detected in the age-matched σR1 +/+ mice (Fig. 9F). Quantification of the number of cells in the GCL revealed significantly fewer cells (expressed per 100-μm length of retina) in the σR1 −/− mice than in the σR1 +/+ (Fig. 9I), particularly in the central retina. In the peripheral retina, ...
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the SIGMAR1 gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system. It has been implicated in several phenomena, including cardiovascular function, schizophrenia, clinical depression, the effects of cocaine abuse, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand for the σ1 receptor has yet to be conclusively identified, but tryptaminergic trace amines, as well as neuroactive steroids such as dehydroepiandrosterone (DHEA) and pregnenolone all activate the receptor. The σ1 receptor is defined by its unique pharmacological profile. In 1976 Martin reported that the effects of ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...