2-Pyridylethylamine dihydrochloride是一种组胺-1（H1R）受体激动剂。
Cas No.:3343-39-3
Sample solution is provided at 25 µL, 10mM.
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2-Pyridylethylamine dihydrochloride is a histamine H1 receptor (H1R) agonist[1-2]. 2-Pyridylethylamine dihydrochloride is commonly used in research related to neurological diseases and pain[3-4].
In vitro, treatment of myofibroblasts isolated from intact rat hearts with 2-Pyridylethylamine dihydrochloride (10nM, 1μM, 100μM) significantly increased the collagen content within the cultures[5]. Stimulation of DDT₁MF-2 cells with 2-Pyridylethylamine dihydrochloride (10μM–1mM) for 10 minutes significantly activated inositol phospholipid hydrolysis[6].
In vivo, a single microinjection of 2-Pyridylethylamine dihydrochloride (4μg/site) into the ventral posteromedial nucleus (VPM) of the rat thalamus significantly suppressed hypertonic saline-induced corneal pain responses and capsaicin-induced orofacial pain responses[7]. A single intra-articular injection of 2-Pyridylethylamine (5nmol) into the knee joint of a rat model of formaldehyde-induced knee joint pain produced significant analgesic effects by activating the spinal NPY-Y1 receptor pathway[8].
References:
[1] Gemba C, Nakayama K, Nakamura S, et al. Involvement of histaminergic inputs in the jaw-closing reflex arc. J Neurophysiol. 2015 Jun 1;113(10):3720-35.
[2] Vohra MM. Species differences in the contractile response to two specific histamine H1-receptor agonists: 2-(2-pyridyl)-ethylamine and 2-(2-aminoethyl)-thiazole. J Pharm Pharmacol. 1981 Feb;33(2):104-6.
[3] Shams Ghamsary M, Ghiasi M, Naghavi SS. Insight into the activation mechanism of carbonic anhydrase(II) through 2-(2-aminoethyl)-pyridine: a promising pathway for enhanced enzymatic activity. Phys Chem Chem Phys. 2024 Mar 27;26(13):10382-10391.
[4] Asgharieh-Ahari M, Tamaddonfard E, Erfanparast A, et al. Histamine and its H 1 receptors in the ventral pallidum mediate formalin-induced pain-related behaviors through this region and spinal cord opioid receptors. Behav Pharmacol. 2023 Dec 1;34(8):457-467.
[5] Piera L, Szymański J, Juszczak M, et al. Histamine is involved in the regulation of collagen content in cultured heart myofibroblasts via H2, H3 and H4 histamine receptors. Biomed Rep. 2021 Aug;15(2):71.
[6] Souza-Silva E, Stein T, Mascarin LZ, et al. Intra-articular injection of 2-pyridylethylamine produces spinal NPY-mediated antinociception in the formalin-induced rat knee-joint pain model. Brain Res. 2020 May 15;1735:146757.
[7] Tamaddonfard E, Erfanparast A, Ghasemi H, et al. The role of histamine H1, H2 and H3 receptors of ventral posteromedial nucleus of thalamus in modulation of trigeminal pain. Eur J Pharmacol. 2016 Nov 15;791:696-702.
[8] Gemba C, Nakayama K, Nakamura S, et al. Involvement of histaminergic inputs in the jaw-closing reflex arc. J Neurophysiol. 2015 Jun 1;113(10):3720-35.
2-Pyridylethylamine dihydrochloride是一种组胺-1（H1R）受体激动剂[1-2]。2-Pyridylethylamine dihydrochloride常被用于神经疾病、疼痛相关的研究中[3-4]。
在体外，2-Pyridylethylamine dihydrochloride（10nM、1μM、100μM）处理从完整大鼠心脏分离的肌成纤维细胞，显著提高培养物中胶原蛋白的含量[5]。2-Pyridylethylamine dihydrochloride（10μM–1mM）刺激DDT₁MF-2细胞10分钟，显著激活肌醇磷脂水解[6]。
在体内，2-Pyridylethylamine dihydrochloride（4μg/位点）单次注射到大鼠丘脑腹后内侧核，显著抑制高渗盐水诱导的角膜疼痛反应和辣椒素诱导的口面部疼痛反应[7]。2-Pyridylethylamine（5nmol）膝关节腔内单次注射，用于处理福尔马林诱导的大鼠膝关节疼痛模型，通过激活脊髓NPY-Y1受体通路产生显著镇痛作用[8]。
| Cell experiment [1]: | |
Cell lines | DDT1MF-2 hamster vas deferens smooth muscle cells |
Preparation Method | DDT1MF-2 cells were prelabelled with [³H]-myo-inositol for 24 hours and stimulated with 2-pyridylethylamine dihydrochloride (10μM–1mM) for 10 minutes in the presence of 20mM LiCl. |
Reaction Conditions | 10μM–1mM; 10 minutes |
Applications | 2-Pyridylethylamine dihydrochloride concentration-dependently stimulated [³H]-inositol phosphate accumulation in DDT1MF-2 cells, with an EC₅₀ of 85μM. The maximal response induced by 2-pyridylethylamine dihydrochloride was 67.7% of the response elicited by histamine (100%), indicating partial agonist activity at H₁ receptors. The response was antagonized by mepyramine (Kᴅ=0.36nM). |
| Animal experiment [2]: | |
Animal models | Adult male Wistar rats |
Preparation Method | Rats were bilaterally implanted with guide cannulas targeting the ventral posteromedial (VPM) nucleus of the thalamus. Microinjections of 2-pyridylethylamine dihydrochloride (4µg/site) were administered 3 minutes before inducing trigeminal pain via corneal application of hypertonic saline or subcutaneous capsaicin injection into the vibrissa pad. |
Dosage form | 4µg/site; Intra-VPM microinjection; Single injection. |
Applications | 2-Pyridylethylamine dihydrochloride significantly suppressed both corneal pain (reduced eye wipes) and orofacial pain (decreased face rubbing duration). |
References: | |
| Cas No. | 3343-39-3 | SDF | |
| 化学名 | 2-(pyridin-2-yl)ethanamine dihydrochloride | ||
| Canonical SMILES | NCCC1=NC=CC=C1.Cl.Cl | ||
| 分子式 | C7H10N2.2HCl | 分子量 | 195.09 |
| 溶解度 | <19.51mg/ml in Water; <9.75mg/ml in DMSO | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.1258 mL | 25.6292 mL | 51.2584 mL |
| 5 mM | 1.0252 mL | 5.1258 mL | 10.2517 mL |
| 10 mM | 512.6 μL | 2.5629 mL | 5.1258 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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2.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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