Hibino Tomoko, Yuzurihara Mitsutoshi, Kase Yoshio, Takeda Atsushi
Tsumura Research Laboratories, Tsumura & Co., Japan.
J Pharmacol Sci. 2009 Sep;111(1):73-81. doi: 10.1254/jphs.09077fp. Epub 2009 Aug 29.
We investigated the effects of Evodiae Fructus and synephrine, one of the components of Evodiae Fructus, on blood vessels. We found that Evodiae Fructus (1 x 10(-6) - 3 x 10(-4) g/mL) had constrictive effects on rat aorta. The vasoconstrictive effects of Evodiae Fructus were significantly inhibited by pretreatment with prazosin (adrenergic alpha(1)-receptor antagonist), BRL15572 [5-hydroxytryptamine (5-HT)(1D) antagonist], and ketanserin (5-HT(2A) antagonist), but its vasoconstrictive effects were not inhibited by pretreatment with SB216641 (5-HT(1B) antagonist) or propranolol (adrenergic beta-receptor antagonist). These results suggest that Evodiae Fructus constricts rat aorta via adrenergic and serotonergic receptors. We also investigated the constrictive effects of synephrine on blood vessels. The vasoconstrictive effects of synephrine (1 x 10(-7) - 3 x 10(-5) mol/L) were significantly inhibited by pretreatment with prazosin, BRL15572, and ketanserin. However, its constrictive effects were not inhibited by pretreatment with SB216641 and propranolol. The pA(2) values of prazosin or ketanserin were nearly equal between Evodiae Fructus and synephrine. Because the constrictive effects of both Evodiae Fructus and synephrine were exerted via adrenergic alpha(1)-receptors and serotonergic (5-HT(1D) and 5-HT(2A)) receptors, synephrine may be one of the important components in the constrictive effects of Evodiae Fructus.
我们研究了吴茱萸及其成分之一辛弗林对血管的影响。我们发现吴茱萸(1×10⁻⁶ - 3×10⁻⁴ g/mL)对大鼠主动脉有收缩作用。哌唑嗪(肾上腺素α₁受体拮抗剂)、BRL15572 [5-羟色胺(5-HT)₁D拮抗剂] 和酮色林(5-HT₂A拮抗剂)预处理可显著抑制吴茱萸的血管收缩作用,但SB216641(5-HT₁B拮抗剂)或普萘洛尔(肾上腺素β受体拮抗剂)预处理则不能抑制其血管收缩作用。这些结果表明,吴茱萸通过肾上腺素能和5-羟色胺能受体收缩大鼠主动脉。我们还研究了辛弗林对血管的收缩作用。哌唑嗪、BRL15572和酮色林预处理可显著抑制辛弗林(1×10⁻⁷ - 3×10⁻⁵ mol/L)的血管收缩作用。然而,SB216641和普萘洛尔预处理不能抑制其收缩作用。吴茱萸和辛弗林的哌唑嗪或酮色林的pA₂值几乎相等。由于吴茱萸和辛弗林的收缩作用均通过肾上腺素α₁受体和5-羟色胺能(5-HT₁D和5-HT₂A)受体发挥,因此辛弗林可能是吴茱萸收缩作用的重要成分之一。