Wei E Q, Xin X H, Wang Y C, Chen L P, Zhang L F, Bian R L
Department of Pharmacology, Zhejiang Medical University, Hangzhou, China.
Zhongguo Yao Li Xue Bao. 1995 Nov;16(6):485-8.
To determine the role of ONO-1078, 4-oxo-8 -[p-(4-phenylbutyloxy) benzoylamino]- 2-(tetrazol-5-yl) -4H-1-benzopyran hemihydrate, in cardiovascular responses induced by vagal stimulation, capsaicin, and substance P.
Evans blue extravasation in the atrium and ventricle, and mean arterial pressure (MAP) were observed.
Electric stimulation of vagus (ESV, 10 Hz, 5 ms, 2 or 10 V, for 90 s) increased Evans blue extravasation in the hearts of atropine (1 mg.kg-1, i.v.)-pretreated guinea pigs. Capsaicin (0.05 mg.kg-1, i.v.) and substance P (1 microgram.kg-1, i.v.) enhanced the dye extravasation and elicited a drop in MAP. ONO-1078 (0.03 and 0.1 mg.kg-1, i.v.) inhibited ESV-induced response, especially at stimulation of 2 V. ONO-1078 (0.03 mg.kg-1) attenuated capsaicin-induced cardiac microvascular leakage and hypotensive response, but failed to inhibit substance P-induced responses.
ONO-1078 can modulate the cardiovascular responses in neurogenic inflammation, possibly mediated by inhibiting sensory neuropeptide release.
确定ONO - 1078(4 - 氧代 - 8 - [对 -(4 - 苯基丁氧基)苯甲酰氨基] - 2 -(四氮唑 - 5 - 基)- 4H - 1 - 苯并吡喃半水合物)在迷走神经刺激、辣椒素和P物质诱导的心血管反应中的作用。
观察心房和心室中伊文思蓝外渗情况以及平均动脉压(MAP)。
电刺激迷走神经(ESV,10Hz,5ms,2或10V,持续90s)使预先经静脉注射阿托品(1mg·kg⁻¹)处理的豚鼠心脏中伊文思蓝外渗增加。辣椒素(0.05mg·kg⁻¹,静脉注射)和P物质(1μg·kg⁻¹,静脉注射)增强了染料外渗并引起MAP下降。ONO - 1078(0.03和0.1mg·kg⁻¹,静脉注射)抑制ESV诱导的反应,尤其是在2V刺激时。ONO - 1078(0.03mg·kg⁻¹)减弱了辣椒素诱导的心脏微血管渗漏和降压反应,但未能抑制P物质诱导的反应。
ONO - 1078可调节神经源性炎症中的心血管反应,可能是通过抑制感觉神经肽释放介导的。