MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 119630-94-3
MCE 国际站:Naloxone benzoylhydrazone
产品活性:Naloxone benzoylhydrazone (NalBzoH) 是一种混合的激动剂/拮抗剂。Naloxone benzoylhydrazone 是原型 κ3 -阿片样受体激动剂,是克隆的 μ 和 δ 阿片样受体的部分激动剂,在阿片样 NOP 受体上是拮抗剂。Naloxone benzoylhydrazone 可用于缓解疼痛的研究。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Opioid Receptor
In Vitro: At the mu-opioid receptor (MOR), Naloxone benzoylhydrazone stimulates [35S]GTPγS binding (pEC50=8.59) and inhibits cyclic AMP accumulation (pEC50=8.74) with maximal effects (Emax) corresponding to 55 and 65% of those obtained with the MOR agonist DAMGO, respectively.
At the κ-opioid receptor (KOR), Naloxone benzoylhydrazone stimulates [35S]GTPγS binding (pEC50=9.70) and inhibits cyclic AMP formation (pEC50=9.45) .
In CHO cells expressing the δ-opioid receptor (DOR), Naloxone benzoylhydrazone increases [35S]GTPγS binding (pEC50=8.49) and inhibits cyclic AMP formation (pE50=8.61).
In Vivo: Analgesic studies in mice examining increasing doses of Naloxone benzoylhydrazone with a fixed dose of morphine reveals a biphasic curve. Naloxone benzoylhydrazone at doses as low as 1 μg/kg partially antagonized morphine analgesia. Higher Naloxone benzoylhydrazone doses continued to inhibit morphine analgesia in a dose-dependent manner, with the 1-mg/kg dose antagonizing completely morphine analgesia. As the Naloxone benzoylhydrazone dose increased beyond 1 mg/kg analgesia returned. Naloxone benzoylhydrazone also prduces a similar analgesic response when administered alone in mice and also is active in rats. Naloxone benzoylhydrazone has excellent p.o. activity, with an analgesic potency in mice equivalent to s.c. administration. In addition to blocking morphine analgesia, low doses of Naloxone benzoylhydrazone also partially reverses the inhibition of gastrointestinal transit in mice produced by morphine, antagonizes completely morphine lethality and precipitates withdrawal in morphine-dependent mice.
相关产品:Methyl-6-alpha-Naltrexol | [D-Ala2]-Met-Enkephalin | GSK1521498 free base | (-)-U-50488 hydrochloride | SB-612111 | BMS-986188 | Loxicodegol | Deltakephalin | MOR agonist-1 | CTAP | Deltorphin I | Nociceptin(1-7) | EST73502 | Enadoline | Ro 64-6198 | Norbinaltorphimine dihydrochloride | SR-16435 | JTC-801 | (+)-N-Allylnormetazocine hydrochloride | β-Endorphin (6-31), human | 5'-Guanidinonaltrindole hydrochloride | D-Ala-Gly-Phe-Met-NH2 monoacetate | Corydaline | Trimebutine-d5 fumarate | Gluten Exorphin C | Dynorphin A (1-10) (TFA) | Naloxegol-d5 oxalate | Matrine | [Nphe1]Nociceptin(1-13)NH2
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-107743
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。