Category: 156028-26-1

Discovery of 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone

Interested yet? Read on for other articles about 156028-26-1, you can contact me at any time and look forward to more communication. Category: quinuclidines.

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 156028-26-1, Name is 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone, SMILES is O=C(C1=CC(Cl)=C(C2=C(Cl)C=C3C4=C2C5=C(Cl)C=C4C(OC3=O)=O)C6=C5C(Cl)=CC7=C16)OC7=O, in an article , author is Ishihara, T, once mentioned of 156028-26-1, Category: quinuclidines.

Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: Enzyme inhibition and effects on plasma lipid levels

Squalene synthase (E.C. 2.5.1.21) is a microsomal enzyme which catalyzes the reductive dimerization of two molecules of farnesyl diphosphate to form squalene, and is involved in the first committed step in cholesterol biosynthesis. It is an attractive target for hypocholesterolemic and hypotriglyceridemic strategies. We synthesized a series of 3-ethylidenequinuclidine derivatives, and evaluated their ability to inhibit squalene synthase in vitro and to lower non-HDL cholesterol levels in hamsters. 3-Ethylidene-quinuclidine derivatives incorporating an unsubstituted 9H-carbazole moiety reduced plasma non-HDL cholesterol levels and did not affect plasma transaminase levels, indicating a lack of hepatotoxicity. Among the novel Compounds, (Z)-2-[2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 8 (YM-53579) and (E)-2-[2-fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride 28 (YM-53601) were potent inhibitors of squalene synthase derived from human hepatoma cells, with IC50 Values Of 160 and 79 nM. respectively. They also reduced plasma non-HDL cholesterol levels in hamsters by approximately 50 and 70%, respectively. at all oral dose of 50 mg/kg/day for 5 days. (C) 2003 Elsevier Ltd. All rights reserved.

Interested yet? Read on for other articles about 156028-26-1, you can contact me at any time and look forward to more communication. Category: quinuclidines.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Top Picks: new discover of 156028-26-1

Application of 156028-26-1, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 156028-26-1.

Application of 156028-26-1, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 156028-26-1, Name is 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone, SMILES is O=C(C1=CC(Cl)=C(C2=C(Cl)C=C3C4=C2C5=C(Cl)C=C4C(OC3=O)=O)C6=C5C(Cl)=CC7=C16)OC7=O, belongs to quinuclidines compound. In a article, author is Quadri, Marta, introduce new discover of the category.

Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the alpha 7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation

alpha 7 nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for a variety of disorders alpha including neurodegeneration, cognitive impairment, and inflammation. Although traditionally identified as an ionotropic receptor, the alpha 7 subtype showed metabotropic-like functions, mainly linked to the modulation of immune responses. In the present work, we investigated the structure-activity relationships in a set of novel alpha 7 ligands incorporating the 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazole scaffold, i.e. derivatives 21a-34a and 21b-34b, aiming to identify the structural requirements able to preferentially trigger one of the two activation modes of this receptor subtype. The new compounds were characterized as partial and silent alpha 7 nAChR agonists in electrophysiological assays, which allowed to assess the contribution of the different groups towards the final pharmacological profile. Overall, modifications of the selected structural backbone mainly afforded partial agonists, among them tertiary bases 27a-33a, whereas additional hydrogen -bond acceptor groups in permanently charged ligands, such as 29b and 31b, favored a silent desensitizing profile at the alpha 7 nAChR. (C) 2018 Elsevier Masson SAS. All rights reserved.

Application of 156028-26-1, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 156028-26-1.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider

Extracurricular laboratory: Discover of C24H4Cl4O6

If you¡¯re interested in learning more about 156028-26-1. The above is the message from the blog manager. Computed Properties of 530.1.

156028-26-1, Name is 5,6,12,13-Tetrachloroanthra[2,1,9-def:6,5,10-d’e’f’]diisochromene-1,3,8,10-tetraone, molecular formula is C24H4Cl4O6, belongs to quinuclidines compound, is a common compound. In a patnet, author is Kobayashi, S, once mentioned the new application about 156028-26-1, Computed Properties of 530.1.

Effects of YM905, a novel muscarinic M-3-receptor antagonist, on experimental models of bowel dysfunction in vivo

We investigated the effects of YM905 [(+)-(1S,3’R)-quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monosuccinate], a new orally active muscarinic M-3-receptor antagonist, on bowel dysfunction in vivo using experimental models that reproduce the symptoms present in irritable bowel syndrome (IBS). YM905 potently inhibited restraint stress-induced fecal pellet output in fed rats (ED50: 4.0 mg/kg) and diarrhea in fasted rats (ED50: 1.7 mg/kg), with similar potencies to the inhibition of bethanechol-, neostigmine- and nicotine-induced fecal pellet output in rats (ED50: 3.3, 7.9 and 4.5 mg/kg, respectively). YM905 also inhibited 5-hydroxytryptamine (5-HT)-, prostaglandin E-2- and castor oil-induced secretory diarrhea in mice (ED50: 5.5, 14 and 6.3 mg/kg, respectively), but showed no significant effect on cholera toxin-induced intestinal secretion in mice. In addition, YM905 (3, 10 mg/kg) reversed morphine-decreased postprandial defecation in ferrets, a model of spastic constipation, whereas remosetron, a 5-HT3-receptor antagonist, was not effective. The mode of YM905 action was similar to that of darifenacin, a selective M3-receptor antagonist, with equivalent potencies. By contrast, propantheline, an antimuscarinic drug that has been used for IBS, was much less potent. These results show that YM905 ameliorates a wide spectrum of bowel dysfunctions through the blockade Of M-3 receptors, suggesting its therapeutic potential for treating IBS.

If you¡¯re interested in learning more about 156028-26-1. The above is the message from the blog manager. Computed Properties of 530.1.

Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider