Iodophenpropit dihydrobromide

• 常用名: Iodophenpropit dihydrobromide
• 英文名: Iodophenpropit dihydrobromide
• CAS号: 145196-87-8
• 分子量: 576.13200
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₅H₂₁Br₂IN₄S
• 熔点: N/A
• 闪点: N/A

Iodophenpropit dihydrobromide用途

Iodophenpropit dihydrobromide 是一种有效的选择性组胺 H3 受体 (histamine H3 receptor) 拮抗剂。[125I] Iodophenpropit 结合 H3 受体具有选择性,可饱和,易于可逆,及高亲和力 (KD 为 0.32 nM)。

Iodophenpropit dihydrobromide名称

• 中文名: 碘苯丙酮二氢溴化物
• 英文名: 3-(1H-Imidazol-4-yl)propyl N-[2-(4-iodophenyl)ethyl]carbamimidoth ioate dihydrobromide

Iodophenpropit dihydrobromide生物活性

• 描述: Iodophenpropit dihydrobromide 是一种有效的选择性组胺 H3 受体 (histamine H3 receptor) 拮抗剂。[125I] Iodophenpropit 结合 H3 受体具有选择性,可饱和,易于可逆,及高亲和力 (KD 为 0.32 nM)。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 靶点实验:

  H3 Receptor:0.32 nM (Kd)

• 体外研究: 碘苯丙酯是一种非常有效的H3受体拮抗剂,对H1和H2受体只有中等亲和力[2]。碘苯丙酯抑制5-羟色胺(5-HT)反应,IC50为1.57±0.3μM[3]。
• 体内研究: 碘苯丙酯(1μg/kg；肌肉注射；b.i.d.；持续10天)显示兔体内抗羊红细胞(SRBC)-免疫球蛋白(Igs)总量显著增加[4]。动物模型：新西兰成年健康兔,雌雄各半,体重1.63±0.36 kg[4],剂量：1μg/kg,肌肉注射(i.m.)；b.i.d.,连续10天,结果：可影响可检测到的SRBC抗体反应。
• 参考文献:

  [1]. Jansen FP, et al. The first radiolabeled histamine H3 receptor antagonist, [¹²⁵I]Iodophenpropit: saturable and reversible binding to rat cortex membranes. Eur J Pharmacol. 1992 Jul 7;217(2-3):203-5.

  [2]. Leurs R, et al. Evaluation of the receptor selectivity of the H3 receptor antagonists, Iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed. Br J Pharmacol. 1995 Oct;116(4):2315-21.

  [3]. Allen MC. Agonist and antagonist effects of histamine H3 receptor ligands on 5-HT3 receptor-mediated ion currents in NG108-15 cells. Eur J Pharmacol. 1998 Nov 20;361(2-3):261-8.

  [4]. Trivendra Tripathi, et al. In vivo immunomodulatory profile of histamine receptors (H1, H2, H3 and H4): a comparative antagonists study. Asian Pac J Trop Med. 2010 Jun;3(6):465-470.

Iodophenpropit dihydrobromide物理化学性质

• 分子式: C₁₅H₂₁Br₂IN₄S
• 分子量: 576.13200
• 精确质量: 573.89000
• PSA: 89.86000
• LogP: 5.85400
• InChIKey: BOSOGNBLIWPCMS-UHFFFAOYSA-N
• SMILES: Br.Br.NC(=NCCc1ccc(I)cc1)SCCCc1cnc[nH]1

Iodophenpropit dihydrobromide靶点实验

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Iodophenpropit dihydrobromide英文别名

• L-BMAA hydrochloride