SKF 91488 dihydrochloride  (Synonyms: Homodimaprit dihydrochloride)

SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a K_i value of 0.9 μM. SKF 91488 dihydrochloride can block histamine metabolism and increase histamine concentrations. SKF 91488 dihydrochloride can increase blood pressure and enhance bronchoconstriction. SKF 91488 can be used for the researches of infection, inflammation and cardiovascular disease, such as Mycoplasma pneumonia and hemorrhagic hypotension^[1][2][3][4].

SKF 91488 (100 μM, 20 mins) 可消除感染支原体 (Mycoplasma ) 的肺炎仓鼠气管段中感染诱导的气道对组胺的高反应性^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SKF 91488 (20-100 μg，颅内注射) 会升高 Wistar 大鼠的平均动脉压 (MAP) 和心率 (HR) ^[1]。
SKF 91488 (10 μg，颅内注射，放血前 5 分钟给药) 在 Wistar 大鼠中对将 MAP 降至 60 mmHg 所需的血容量无影响，但会显著增加将 MAP 降至 40 mmHg 和 20 mmHg 所需的血容量^[1]。
SKF 91488 (20-100 μg，颅内注射) 会显著升高 Wistar 大鼠下丘脑和延髓中的组胺浓度^[1]。
SKF 91488 (10 mM，雾化吸入，每次给药 90 次呼吸，OA 激发前 15 分钟给药) 会增强卵清蛋白 (OA) 致敏的 Hartley 豚鼠中由 OA 诱导的支气管收缩^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

248.22

C₇H₁₉Cl₂N₃S

68941-21-9

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Jochem J, et al. Influence of SKF 91488, histamine N-methyltransferase inhibitor, on the central cardiovascular regulation during controlled, stepwise hemorrhagic hypotension in rats. Pol J Pharmacol. 2002 May-Jun;54(3):237-44.  [Content Brief]

  [2]. Sekizawa K, et al. Histamine N-methyltransferase modulates histamine- and antigen-induced bronchoconstriction in guinea pigs in vivo. Am Rev Respir Dis. 1993 Jan;147(1):92-6.  [Content Brief]

  [3]. Tamaoki J, et al. Airway hyperresponsiveness to histamine in mycoplasmal infection: role of histamine N-methyltransferase. Eur J Pharmacol. 1998 Apr 24;347(2-3):257-60.  [Content Brief]

  [4]. Beaven MA, et, al. Inhibition of histamine methylation in vivo by the dimaprit analog, SKF Compound 91488. Agents Actions. 1979 Dec;9(5-6):455-60.  [Content Brief]