上海WAY-100635 Maleate1092679-51-0价格供应产品资料
WAY-100635 Maleate
分子式：C25H34N4O2.C4H4O4     分子量：538.64
质量标准：>98%,BR
产品描述
WAY-100635 Maleate是有效的，选择性5-HT1A受体激动剂，pIC50为8.87, 比作用于其他5-HT受体亚型和主要的神经递质受体选择性高100倍以上。
靶点
5-HT
IC50
0.95 nM
体外研究
In dorsal raphe nucleus (DRN) slices superfused with WAY-100635 Maleate(10 nM), the majority of putative 5-HT neurons increase their firing rate (13% of baseline rate). In addition, WAY-100635 Maleate completely prevents the decrease in firing rate produced by 5-HT (3-15 μM), 8-OH-DPAT (10 nM), 5-carboxamidotryptamine (20 nM) ａnd lesopitron (100 nM). The antagonism exerted by WAY-100635 Maleate is fully surmounted by increasing the concentration of 5-HT to 300 μM with an IC50 of 0.95 nM. In hippocampal slices, WAY 100635 (0.5 nM -10 nM) does not alter the resting membrane potential or the membrane input resistance of intracellularly recorded CA1 pyramidal cells. However, WAY-100635 Maleate completely prevents not only the hyperpolarization, with an IC50 of 1.3 nM, but also the decrease in membrane input resistance produced by 5-HT ａnd 5-carboxamidotryptamine with IC50 of 22.5 μM ａnd 50 nM, respectively.WAY-100635 Maleate has an IC50 of 1.35 nM ａnd is > 100-fold selective for the 5-HT1A site relative to a range of other CNS receptors. The Bmax of [3H]WAY-100635 Maleate specific binding is consistently 50-60% greater than that of the agonist radioligand, [3H]8-OH-DPAT. Mn2+, but not guanine nucleotides, inhibits [3H]WAY-100635 Maleate-specific binding. WAY-100635 Maleate has no 5-HT1A receptor agonist actions, but dose-dependently blocks the effects of agonists at both the postsynaptic 5-HT1A receptor in the CA1 region of the hippocampus, ａnd the somatodendritic 5-HT1A receptor locates on dorsal raphe 5-HT neurones.[3H]WAY 100635 has a Kd of approximately 2.5 nM.In the isolated guinea-pig ileum WAY 100635 is a potent and, at high concentrations, an insurmountable antagonist of the 5-HT1A receptor agonist action of 5-carboxamidotryptamine, with an apparent pA2 value (at 0.3 nM) of 9.71.Five minutes after the i.v. injection of [3H]WAY 100635 (4 μCi -7.6 μCi per mouse) the amount of tritium found in the whole brain only accounted for 1.5-1.8% of the injected radioactivity, regional differences in 3H accumulation already correspondes to those of 5-HT1A receptor density.In light of its only recently discovered dopaminergic activity, conclusions drawn from studies that employs WAY-100635 Maleate as a selective 5-HT1A antagonist may need to be re-evaluated.
体内研究
[3H]WAY-100635 Maleate is shown to bind selectively to brain 5-HT1A receptors, following intravenous administration to mice. WAY 100635 also dose-dependently blocks the ability of 8-OH-DPAT to inhibit the firing of dorsal raphe 5-HT neurones, ａnd to induce the ＇5-HT syndrome＇, hypothermia, hyperphagia ａnd to elevate plasma ACTH levels. In the mouse light/dark box anxiety model, WAY-100635 Maleate induces anxiolytic-like effects. WAY-100635 Maleate has no intrinsic effect on cognition in the delayed-matching-to-position model of short-term memory in the rat, but reverses the disruptive effects of 8-OH-DPAT on motor motivational performance.WAY-100635 Maleate blocks the inhibitory action of 8-OH-DPAT on dorsal raphe neuronal firing in the anaesthetised rat at doses which has no inhibitory action per se. In behavioural models, WAY-100635 Maleate itself induces no overt behavioural changes but potently antagonises the behavioural syndrome induced by 8-OH-DPAT in the rat ａnd guinea-pig (minimum effective dose = 0.003 mg/kg s.c. ａnd ID50 = 0.01 mg/kg s.c., respectively). WAY-100635 Maleate also blocks the hypothermia induced by 8-OH-DPAT in the mouse ａnd rat with ID50 values of 0.01 mg/kg s.c.
溶解性
DMSO 85 mg/mL，水 <1 mg/mL，乙醇 85 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO
特征
[3H]WAY-100635 Maleate is characterised as the first 5-HT1A antagonist radioligand.
上海WAY-100635 Maleate1092679-51-0价格供应订购流程
告知客服人员1092679-51-0这个CAS号，并告知您的需求量，让客服人员为您介绍包装跟价格！为回馈新老客户公司不定期会搞促销活动，优惠可咨询客服！！
发货情况：我司默认发圆通速递，如需更改快递请提前告知！江浙沪2天内到货，其他地区3-5天！
上海WAY-100635 Maleate1092679-51-0价格供应注意事项
产品图片仅供参考，以实物为准！国产进口均可提供！！！由于网站规则的限制，产品无法全部上传，有需要实验室产品尽可联系客服询价，万种产品随亲挑选，正规生物公司，可开具正规机打发票。厂家直销，价格优势！
任何试剂严禁用手直接触摸及用嘴尝，酸性或碱性液体溅至皮肤不得用中和剂处理，防止放热烧伤。
上海WAY-100635 Maleate1092679-51-0价格供应常见问题
1，取用药品时要做到三不原则：不能用手接触药品。不要把鼻孔凑到容器口直接去闻药品的气味，应用手在瓶口轻轻煽动，仅使少量气味进入鼻孔。不得品尝药品。
　　2，注意节约药品。如果没有说明用量，一般取少量。液体取用1-2ml，固体只需盖满试管底部。
　　3，实验完毕后，剩余药品要做到三不一要，即不放回原瓶，不随意丢弃，不拿出实验室。一要，要放入指定容器内。
　　4，固体药品的取用。块状用镊子，粉末用药匙（或纸槽）。取固体应做到“一横二送三慢竖”以免打破试管底。用粉末时应做到“一斜二送三直立”
　　5，液体药品的取用。1，应把瓶塞拿下，倒放在实验台上防止污染溶液。2，倾倒时标签应向着手心，以免腐蚀标签。3，瓶口紧挨试管口。取少量时，应用胶头滴管滴加，滴加时要保持垂直悬空滴加，不能伸入瓶内或试管内，防止污染试剂。取一定量时，常用量筒量出体积，量筒必须放平，读数时，事先要与量筒内凹液面处保持水平。