生物活性
|
产品描述 |
Iodophenpropit dihydrobromide is an effective and selective antagonist of the histamine H3 receptor. The binding of [125I]Iodophenpropit is readily reversible, selective, and of high affinity (KD: 0.32 nM). |
|
靶点活性 |
H3 Receptor,0.32 nM (kd) |
|
体外活性 |
Iodophenpropit suppresses 5-hydroxytryptamine (5-HT) responses (IC50 of 1.57±0.3 μM)[3]. Iodophenpropit is a very potent H3 receptor antagonist and displays only a moderate affinity for the H1 and H2 receptors [2]. |
|
体内活性 |
In rabbits, Iodophenpropit (1 μg/kg; through intramuscular; b.i.d.; for 10 days) displays obviously enhancement of total anti-sheep red blood cells (SRBC)- immunoglobulins (Igs)[4]. |
化学信息
|
分子量 |
576.13 |
|
分子式 |
C15H21Br2IN4S |
|
CAS |
145196-87-8 |
|
溶解度 |
（ < 1 mg/ml refers to the product slightly soluble or insoluble ) |
|
储存条件 |
store at -80°C |
|
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.736 ml | 8.679 ml | 17.357 ml |
| 5 mM | 0.347 ml | 1.736 ml | 3.471 ml |
| 10 mM | 0.174 ml | 0.868 ml | 1.736 ml |
| 50 mM | 0.035 ml | 0.174 ml | 0.347 ml |
参考文献
- 1. Jansen FP, et al. The first radiolabeled histamine H3 receptor antagonist, [
- 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.
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