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T 82 Sale

目录号 : GC31044

T82是一种有效的5-HT3拮抗剂和乙酰胆碱酯酶(AChE)的抑制剂,用于阿尔茨海默症的研究。

T 82 Chemical Structure

Cas No.:252264-92-9

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产品描述

T 82 is a potent 5-HT3 antagonist and acetylcholinesterase (AChE) inhibitor, used for treatment of Alzheimer's Disease.

Chemical Properties

Cas No. 252264-92-9 SDF
Canonical SMILES O=C(O)/C=C/C(O)=O.O=C1N(CCC2CCN(CC3=CC=CC=C3)CC2)CC4=NC5=CC=CC=C5C(OC)=C41.[0.5]
分子式 C26H29N3O2 . 1/2C4H4O4 分子量 473.56
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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Research Update

Effects of T-82, a new quinoline derivative, on cholinesterase activity and extracellular acetylcholine concentration in rat brain

The effects of T-82 (2-[2-(1-benzylpiperidin-4-yl)ethyl]-2,3-dihydro-9-methoxy-1H-pyrrolo [3,4-b]quinolin-1-one hemifumarate), a new quinoline derivative, on acetylcholinesterase (AChE) activity and acetylcholine (ACh) release were compared with those of the well-known cholinesterase inhibitors tacrine and E2020. T-82, tacrine and E2020 all concentration-dependently inhibited AChE in rat brain homogenate (IC50 = 109.4, 84.2 and 11.8 nM, respectively). In addition, although tacrine strongly inhibited butyrylcholinesterase (BuChE), T-82 and E2020 showed only weak activity on BuChE in human plasma. In ex vivo experiments, intraperitoneal administration of T-82 at a dose of 30 mg/kg inhibited AChE activity in the hippocampus, frontal cortex and parietal cortex of rats. The effect of T-82 on the extracellular ACh concentration in rat brain was measured using in vivo microdialysis. T-82 at doses of 10 and 30 mg/kg, i.p. increased the extracellular ACh concentration in the hippocampus and striatum in a dose-dependent manner. These findings suggest that T-82 activates the central cholinergic system by selectively inhibiting AChE activity, while weakly affecting peripheral BuChE activity, and that T-82 increases the extracellular ACh concentration in the brain, which is followed by inhibited AChE activity.

Effects of T-82, a novel acetylcholinesterase inhibitor, on impaired learning and memory in passive avoidance task in rats

Effects of 2-[2-(1-benzylpiperidin-4-yl)ethyl]-2,3-dihydro-9-methoxy-1H-pyrrolo[3,4-b]quinolin-1-one hemifumarate (T-82), a new quinoline derivative, on drug- and basal forebrain lesion-induced amnesia models were examined in rats. Scopolamine (0.5 mg/kg, i.p.) and cycloheximide (1.5 mg/kg, s.c.) shortened the step-through latency in the passive avoidance task. T-82 significantly ameliorated amnesia induced by scopolamine or cycloheximide at the dose of 0.03, 0.1 and 0.3 mg/kg, p.o., and 0.3 and 1.0 mg/kg, p.o., respectively. Basal forebrain lesions with ibotenic acid shortened the step-through latency in passive avoidance task. An acute (0.1 and 0.3 mg/kg, p.o.) or subacute (0.03-0.3 mg/kg, p.o., for 7 days) treatment of T-82 significantly reversed the shortened latency. These results suggest that T-82 may ameliorate the impairment of memory induced by acetylcholinergic dysfunction.

Pseudomonas bubulae sp. nov., isolated from beef

Two Pseudomonas isolates derived independently from raw refrigerated processing meat of bovine origin intended for the manufacture of Bologna-type cooked sausage could be distinguished from other known species in subsequent phylogenetic analyses. Comparison of the complete rpoB gene sequences in combination with nearly complete 16S rRNA gene sequences revealed a separate branch within the Pseudomonas fragi group. In further analyses, comprising phenotypic and chemotaxonomic characterization as well as average nucleotide identity (ANI) values obtained from the draft genome assemblies, the two isolates could be distinguished from all so far published closely related species. The closest relative was P. fragi DSM 3456T with ANI values of about 90.2 %. Other close Pseudomonas neighbours were P. psychrophila DSM 17535T (86.5 %), P. deceptionensis DSM 26521T (86.4 %), P. versuta DSM 101070T (83.8 %), P. taetrolens DSM 21104T (83.2 %), P. weihenstephanensis DSM 29166T (82.3 %), P. helleri DSM 29165T (82.7 %) and P. lundensis DSM 6252T (81.9 %). The G+C contents of isolates TH39T and TH26 were both 58.2 mol%. The major cellular lipids of strain TH39T were phosphatidylethanolamine, phosphatidylglycerol and diphosphatidylglycerol; the major quinone was Q9 with small amounts of Q8. Based on these data, the isolates TH39T and TH26 (=DSM 107389=LMG 30831) represent a novel species within the genus Pseudomonas , for which the name Pseudomonas bubulae sp. nov. is proposed. The type strain is TH39T (=DSM 107390T=LMG 30830T).

Ottowia testudinis sp. nov., isolated from the cloaca of a giant Asian pond turtle ( Heosemys grandis)

A bacterial strain designated 27CT isolated from the cloaca of a giant Asian pond turtle was subjected to polyphasic taxonomic characterization. The strain was Gram-stain negative and oxidase- and catalase-positive. It had highest 16S rRNA gene sequence similarity to Ottowia beijingensis GCS-AN-3T (97.6 %) and Ottowia flava GY511T 96.0% and less than 96.0 % to other established species including Ramlibacter rhizophilus YS3.2.7T, Ottowia konkukae SK3863T, Acidovorax caeni E-24608T and Ottowia thiooxydans DSM 14619T. Phylogenetically, strain 27CT formed a branch with O. beijingensis GCS-AN-3T within the Ottowia clade. The genome size was 4.32 Mbp and the G+C content was 65.7 mol%. Strain 27CT shared highest ANIb values with O. beijingensis GCS-AN-3T (82.71/82.73 %) followed by O. oryzae KADR8-3T (78.9/79.0 %) and O. caeni BD-1T (73.3/75.2 %). The diagnostic diamino acid of the peptidoglycan was meso-diaminopimelic acid and the quinone system was ubiquinone Q-8. Predominant compounds in the polar lipid profile were diphosphatidylglycerol, phosphatidylglycerol, phosphatidylethanolamine and phosphatidylmonomethylethanolamine. Major polyamines were 2-hydroxyputrescine and putrescine. In the fatty acid profile, summed feature 3 (C16 : 1 ω7c and/or C16 : 1 ω6c), C16 : 0, summed feature 8 (C18 : 1 ω7c and/or C18 : 1 ω6c), C14 : 0, C10 : 0 3-OH and C16 : 0 2-OH were detected. All these data identify strain 27CT as representing a novel species of the genus Ottowia and hence we propose the name Ottowia testudinis sp. nov. The type strain is 27CT (=CCM 9138T=LMG 32213T).

Postpartum Maternal Emotional Disorders and the Physical Health of Mother and Child

Purpose: The purpose of this study is to identify the relationships between postpartum emotional manifestations and various neonatal variables, as well as variables within this category, in the context of hospitalization together after birth.
Patients and methods: Between 1 March 2020 and 1 September 2020, a cross-sectional research design was used including mother-child couples (112 mothers, 121 newborns - 13 twins/triplets).
Results: Using a t-test for independent samples, we observed: a) the symptoms of depression were more severe in mothers of newborns hospitalized in neonatal intensive care units (NICUs) [t(110) = 4.334)], provided oxygen therapy [t(109.99) = 3.162], born prematurely [t(110) = 3.157], or with adjustment disorders [t(109) = -2.947] (p < 0.01); b) a similar, for anxiety as a state [t(82.38) = 5.251], t(107.29) = 4.523, t(110) = 3.416, t(109) = -3.268, p < 0.01], and as a trait was more common [t(80.79) = 4.501, t(108.790) = 4.669, t(109) = -3.268, p < 0.001] compared to other mothers. Using Pearson's test (p < 0.001), several very strong correlations were observed between neonatal variables, including number (no.) of days of hospitalization with birth weight (BW) (r = -0.802), head circumference (HC) (r = -0.822), and gestational age (GA) (r = -0.800) and the mother's postpartum anxiety as a state/trait (r = 0.770). Using Poisson regression, it was observed that anxiety as a state (Λ = 0.020, z = 4.029, p < 0.001) and as a trait (Λ = 0.800, z = 6.160, p < 0.001) stimulated the intensity of symptoms of postpartum depression (optimal models).
Conclusion: Postpartum maternal psychological manifestations were associated with NICU hospitalization, pathology, and some neonatal therapies. We also noticed, that the duration of hospitalization, BW, HC, and GA, were correlated with maternal emotional disorders. Results will facilitate future optimization of birth management and postnatal care.