Immepip dihydrobromide是一种强效且特异性的H3受体激动剂。
Cas No.:164391-47-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Immepip dihydrobromide is a potent and specific H3 agonist[1]. Immepip dihydrobromide can readily cross the blood-brain barrier and drastically decrease brain neuronal histamine release in the rat [2]. Immepip dihydrobromide has been widely used to regulate the levels of GABA and glutamate and to alleviate the movement disorders in animals[3].
In vitro, Immepip dihydrobromide treatment (100nM) for 15min prevented the inhibitory effect of H3 receptor activation on forskolin-induced [3H]-cAMP accumulation in [3H]-adenine-labeled rat striatal slices[4]. The treatment with Immepip dihydrobromide (1µM) for 1 hour significantly inhibited the secretion of glucagon by αTC1.6 cells and suppressed the increase in intracellular Ca2+ concentration[5].
In vivo, Immepip dihydrobromide treatment via intravenous injection at a dose of 10µg/kg/min for 10 minutes significantly inhibited the tachycardia response induced by the sympathetic nerve in rats[6]. Injection of Immepip dihydrobromide (10µl; 30μM) through the third cerebral ventricle (i3v) reduced the locomotor behavior of rats within 90 minutes and induced feeding behaviors[7].
References:
[1] Lamberty Y, Margineanu D G, Dassesse D, et al. H3 agonist immepip markedly reduces cortical histamine release, but only weakly promotes sleep in the rat[J]. Pharmacological research, 2003, 48(2): 193-198.
[2] Jansen F P, Mochizuki T, Yamamoto Y, et al. In vivo modulation of rat hypothalamic histamine release by the histamine H3 receptor ligands, immepip and clobenpropit. Effects of intrahypothalamic and peripheral application[J]. European journal of pharmacology, 1998, 362(2-3): 149-155.
[3] Avila-Luna A, Ríos C, Gálvez-Rosas A, et al. Chronic administration of the histamine H3 receptor agonist immepip decreases l-Dopa-induced dyskinesias in 6-hydroxydopamine-lesioned rats[J]. Psychopharmacology, 2019, 236(6): 1937-1948.
[4] Garduño‐Torres B, Arias‐Montaño J A. Homologous down‐regulation of histamine H3 receptors in rat striatal slices[J]. Synapse, 2006, 60(2): 165-171.
[5] Nakamura T, Yoshikawa T, Naganuma F, et al. Role of histamine H3 receptor in glucagon-secreting αTC1. 6 cells[J]. FEBS Open bio, 2015, 5: 36-41.
[6] Pinacho-García M, Marichal-Cancino B A, Villalón C M. Further evidence for the role of histamine H3, but not H1, H2 or H4, receptors in immepip-induced inhibition of the rat cardioaccelerator sympathetic outflow[J]. European Journal of Pharmacology, 2016, 773: 85-92.
[7] Chiba S, Itateyama E, Sakata T, et al. Acute central administration of immepip, a histamine H3 receptor agonist, suppresses hypothalamic histamine release and elicits feeding behavior in rats[J]. Brain research bulletin, 2009, 79(1): 37-40.
Immepip dihydrobromide是一种强效且特异性的H3受体激动剂[1]。Immepip dihydrobromide易于通过血脑屏障，并能显著降低大鼠脑内神经元组胺的释放[2]。Immepip dihydrobromide已被广泛用于调节GABA 和谷氨酸水平，并缓解动物的运动障碍[3]。
在体外，使用100nM的Immepip dihydrobromide处理15分钟，可阻止H3受体激活对[³H]-腺嘌呤标记的大鼠纹状体切片中毛喉素诱导的[3H]-cAMP积累所产生的抑制作用[4]。使用1µM的Immepip dihydrobromide处理αTC1.6细胞1小时，显著抑制了胰高血糖素的分泌，并抑制了细胞内Ca2+浓度的升高[5]。
在体内，静脉注射10µg/kg/min剂量的Immepip dihydrobromide，持续10分钟，显著抑制了交感神经诱导的大鼠心动过速反应[6]。通过第三脑室(i3v)注射10µl的30μM的Immepip dihydrobromide，可在90分钟内减少大鼠的运动行为并诱导摄食行为[7]。
| Cell experiment [1]: | |
Cell lines | αTC1.6 cells |
Preparation Method | αTC1.6 cells were cultured in DMEM containing 10% fetal calf serum, 15mM HEPES, 0.1mM non-essential amino acids, 0.02% BSA, 1.5g/dl sodium bicarbonate, 2g/l d-glucose, 75mg/ml penicillin G potassium, and 100mg/l streptomycin sulfate at 37°C in a 5%-CO2 humidified incubator. αTC1.6 cells were seeded into a 24-well plate at a density of 2.0×105 cells per well and then preincubated in 500μl of Krebs–Ringer bicarbonate buffer (KRB) containing 20mM glucose for 30min at 37°C in 5% CO2. Subsequently, αTC1.6 cells were incubated in 500μl of KRB containing 20 or 2.8mM glucose±1μM histamine, 1μM of Immepip dihydrobromide, or the selective H3R inverse agonist JNJ-5207852, or KRB containing 20mM KCl±1μM Immepip dihydrobromide, for 1h at 37°C in 5% CO2. The glucagon concentration was measured. |
Reaction Conditions | 1µM; 1h |
Applications | Immepip dihydrobromide treatment significantly reduced the secretion of glucagon by αTC1.6 cells. |
| Animal experiment [2]: | |
Animal models | Male Wistar King A rats |
Preparation Method | Mature male Wistar King A rats weighing 300g were housed four per cage in a soundproof room under a 12h/12h light/dark cycle (lights on at 07:00) and were fed a standard laboratory diet and tap water ad libitum. Under intraperitoneal sodium pentobarbital anesthesia (45 mg/kg), rats were placed in a stereotaxis apparatus, and a stainless-steel guide cannula (23-gauge) was chronically implanted into the third cerebroventricle (i3v) of rats at least 1 week before the start of infusions. A stainless-steel wire stylet (29-gauge) was inserted in the guide cannula to prevent leakage of the cerebrospinal fluid and obstruction of the cannula. The rats were given an i3v infusion with 10μl of 30μM Immepip dihydrobromide or the same volume of PBS as controls. Subsequently, the behavior of the rats was examined by determining whether they were feeding, drinking, grooming, rearing, sniffing, exploring, or showing ataxy or hypokinesia every 30s for 90min. |
Dosage form | 30μM (10µl) for once; i3v administration |
Applications | Immepip dihydrobromide treatment significantly reduced the locomotor behaviors and induced feeding behaviors in rats. |
References: | |
| Cas No. | 164391-47-3 | SDF | |
| 别名 | 4-(1H-咪唑基-4-甲基)哌啶二氢溴酸盐 | ||
| 化学名 | 4-((1H-imidazol-5-yl)methyl)piperidine dihydrobromide | ||
| Canonical SMILES | C1(CC2=CN=CN2)CCNCC1.Br.Br | ||
| 分子式 | C9H15N3.2HBr | 分子量 | 327.06 |
| 溶解度 | <32.71mg/ml in water | 储存条件 | Desiccate at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0575 mL | 15.2877 mL | 30.5754 mL |
| 5 mM | 611.5 μL | 3.0575 mL | 6.1151 mL |
| 10 mM | 305.8 μL | 1.5288 mL | 3.0575 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet