GlpBio

Immepip dihydrobromide

目录号: GC12966纯度: >98.00%同义词: 4-(1H-咪唑基-4-甲基)哌啶二氢溴酸盐
Immepip dihydrobromide是一种强效且特异性的H3受体激动剂。
Immepip dihydrobromide
Cas No.: 164391-47-3
规格价格库存数量操作
5mg¥880.00现货
1
10mg¥1,280.00现货
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25mg¥2,560.00现货
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50mg¥4,000.00现货
1
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产品描述 Description

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]。

实验参考方法 Experimental Reference Method

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:
[1] 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.
[2] 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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
164391-47-3
同义词
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
SMILES
C1(CC2=CN=CN2)CCNCC1.Br.Br
分子式
C9H15N3.2HBr
分子量
327.06 g/mol
溶解性
<32.71mg/ml in water
保存条件
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°C，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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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