• 4-[3-butoxy-4-methoxyphenyl)-methyl]-2-imidazolidinone. (aspetjournals.org)
  • The response of ACTH to intraperitoneal SKF 38393 was blocked by pretreatment with the D1 antagonist SCH 23390 (1-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5 tetrahydro-1H-3-benzazepine, 0.25 mg/kg, i.p.) but not by the D2 antagonist sulpiride (50 mg/kg, i.p. (duke.edu)
  • Preinjection in rats of a NMDA receptor antagonist MK-801((+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10- imine maleate), but neither DA receptor antagonists [SCH-23390 (R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine) plus haloperidol] nor a calcineurin inhibitor (cyclosporine), prevents the nicotine-induced increase in AMPA/NMDA ratio. (barrowneuro.org)
  • The butyl- and 4-fluorobenzyl-substituted derivatives, (±)-5-benzyl-2-butyl-2,3,4,5-tetrahydro-1H-2-benzazepine (19 b) and (±)-5-benzyl-2-(4-fluorobenzyl)-2,3,4,5-tetrahydro-1H-2-benzazepine (19 m), show high selectivity over more than 50 other relevant targets, including the σ2 subtype and various binding sites of the N-methyl-D-aspartate (NMDA) receptor. (idexlab.com)
  • Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies. (idexlab.com)
  • Novel H(3) receptor antagonists such as GSK207040 and GSK334429 may therefore have therapeutic potential not only in dementia but also in neuropathic pain. (ox.ac.uk)
  • SCH-23390 maleate also binds with high affinity to the 5-HT 2 and 5-HT 1C receptors . (medchemexpress.com)
  • Analysis of the relationship between the structure and the σ1 affinity revealed that large substituents such as the butyl, benzyl or 4-phenylbutyl moiety at the benzazepine N-atom resulted in high affinity ligands. (idexlab.com)
  • Lorcaserin "Belviq" is believed to decrease food consumption and promote satiety by selectively activating 5-HT2C receptors. (christianhunter.com)
  • Functional antagonism of central H(3) receptors was demonstrated by blockade of R-alpha-methylhistamine-induced dipsogenia in rats (ID(50)=0.02 and 0.11 mg/kg p.o. for GSK207040 and GSK334429, respectively). (ox.ac.uk)
  • In addition, GSK207040 (0.1, 0.3 and 1mg/kg p.o.) and GSK334429 (3 and 10mg/kg p.o.) significantly reversed capsaicin-induced reductions in paw withdrawal threshold, suggesting for the first time that blockade of H(3) receptors may be able to reduce tactile allodynia. (ox.ac.uk)
  • Postsynaptic and DA "autoreceptor" agonists [apomorphine, (-) 3-PPP], as well as dopaminergic ergot derivatives (bromocriptine, lergotrile, lisuride) and Sch 23390, substituted for Ly 171555, a partial ergoline which has behavioral effects that are blocked by haloperidol and molindone, but not by either Sch 23390 or serotonin (5-HT) antagonists (ketanserin, pizotifen). (utmb.edu)
  • To date phenytoin, some benzazepine derivatives and stereoisomers of methylphenylpiracetam have been reported as PAMs of Sig1R while NAMs of Sig1R have not yet been described. (frontiersin.org)
  • SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D 1 -like receptor antagonist with K i s of 0.2 nM and 0.3 nM for the D 1 and D 5 receptor , respectively. (medchemexpress.com)
  • SCH-23390 maleate is a potent and high efficacy human 5-HT 2C receptor agonist with a K i of 9.3 nM. (medchemexpress.com)
  • At the human recombinant H(3) receptor, GSK207040 and GSK334429 were potent functional antagonists (pA(2)=9.26+/-0.04 and 8.84+/-0.04, respectively versus H(3) agonist-induced changes in cAMP) and exhibited inverse agonist properties (pIC(50)=9.20+/-0.36 and 8.59+/-0.04 versus basal GTPgammaS binding). (ox.ac.uk)
  • In accordance with a novel strategy for generating the 2-benzazepine scaffold by connecting C6-C1 and C3-N building blocks, a set of 5-phenylsulfanyl- and 5-benzyl-substituted tetrahydro-2-benzazepines was synthesized and pharmacologically evaluated. (idexlab.com)
  • A large set of tetrahydro-2-benzazepines with an α-hydroxy or α-(aryl)alkoxy substituted benzyl moiety in the 5-position was prepared according to the recently reported C6C1 + C3N synthetic strategy. (idexlab.com)
  • However, the GluN2B ligands eliprodil, Ro 25-6981, and the non-labeled 3-benzazepine 14 were able to abolish the specific binding of [18 F]14. (idexlab.com)
  • Thus, allosteric modulators of Sig1R are described as compounds that can increase the activity of Sig1R ligands that compete with [ 3 H](+)-pentazocine for binding to Sig1R. (frontiersin.org)
  • Graphite-supported gold nanoparticles as efficient catalyst for aerobic oxidation of benzylic amines to imines and N-substituted 1,2,3,4-tetrahydroisoquinolines to amides: synthetic applications and mechanistic study. (sigmaaldrich.com)
  • You should lose at least 5% of your starting weight during the first 12 weeks of taking Belviq and eating a low calorie diet. (cmoapi.com)
  • Call your doctor if you do not lose at least 5% of your starting weight after taking the medicine for 12 weeks. (cmoapi.com)
  • People who take the drug for a year can expect to lose just 3 to 3.7 percent of their weight, and may gain the weight back, research suggests. (cmoapi.com)
  • In one trial, patients taking Belviq did lose up to 5 percent of their body weight after 12 months, but gained back 25 percent of it by the end of the second year. (cmoapi.com)
  • Four commercial fish feeds having 25%, 30%, 32% and 40% crude protein (CP) levels were fed to fish at 3% of their wet body weight three times a day. (bvsalud.org)
  • More recently this chemical compound is claimed to have been sold as a designer drug under the name A3A,[citation needed] but since the anecdotally reported effects of the product sold under this name do not seem to bear any resemblance to the known pharmacology of genuine 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepine, it seems unlikely that this is actually the compound being sold. (wikipedia.org)
  • L-3,4-dihydroxyphenylalanine (L-DOPA)-induced dyskinesia is an incapacitating complication of L-DOPA therapy that affects most patients with Parkinson's disease. (nih.gov)
  • MolPharm articles become freely available 12 months after publication, and remain freely available for 5 years. (aspetjournals.org)
  • BDBM50021153 (1H-1-Benzazepine-1-acetic acid, 3-((1-(ethoxycarbo. (bindingdb.org)
  • High σ1 affinity was achieved for 2-benzazepines with linear or branched alk(en)yl residue s containing at least an n-butyl substructure . (idexlab.com)
  • These results suggest both pre- and postsynaptic actions of 7-OH-DPAT along with a lack of specificity of the various pharmacological compounds for the D(3) receptor. (nih.gov)
  • Discontinuation because of adverse reactions occurred in 4% of amlodipine besylate and benazepril hydrochloride-treated patients and 3% of placebo-treated patients. (nih.gov)
  • By gene cluster evaluation, proteins inside phosphatidylinositol-3-kinase along with calcium/calmodulin kinase connected networks have been recognized as very important to Zaire Ebola malware an infection and prioritized for more examination. (tcr-signal.com)
  • The five types of dopamine (DA) receptor subtypes have been grouped into two families, the D(1)-like (D(1) and D(5) receptors) and D(2)-like (D(2), D(3), and D(4) receptors). (nih.gov)
  • Controversy exists, however, over the precise location and role of the D(3) subtype of DA receptor. (nih.gov)
  • To investigate this issue, rats were trained using standard operant drug discrimination procedures to discriminate 0.10 mg/kg of the putatively D(3) receptor-preferring agonist R(+)-7-hydroxy-N,N,-di-n-propyl-2-aminotetralin (7-OH-DPAT) from saline. (nih.gov)
  • Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies. (idexlab.com)
  • Text-mining in biology is often used for the automatic extraction of information about genes, proteins and their functional relationships from text documents [ 3 - 6 ]. (biomedcentral.com)
  • METHODS@#Male Sprague-Dawley rats were equally divided into 3 groups using a random number table: the control group, the OIPN group, and the EA (OIPN + EA) group, with 10 rats in each. (bvsalud.org)
  • in the experimental group (3) OVX + E2 + EOI group, 80 μg/d E2 injection was started 7 d after OVX and EOI was applied 17 d after OVX. (bvsalud.org)
  • Human IgG antibody Laboratories manufactures the invivogen benzazepine reagents distributed by Genprice. (cell-ess.com)
  • The Invivogen Benzazepine reagent is RUO (Research Use Only) to test human serum or cell culture lab samples. (cell-ess.com)
  • Jinarc is indicated to slow the progression of cyst development and renal insufficiency of autosomal dominant polycystic kidney disease (ADPKD) in adults with CKD stage 1 to 3 at initiation of treatment with evidence of rapidly progressing disease. (drugpatentwatch.com)