Cohen A F, Hamilton M J, Liao S H, Findlay J W, Peck A W
Eur J Clin Pharmacol. 1985;28(2):197-204. doi: 10.1007/BF00609692.
The new H1-receptor antagonist BW 825C and triprolidine (2.5 and 5 mg) were administered to 12 healthy male volunteers in a double blind placebo controlled, balanced, crossover design. Histamine antagonism was measured by assessment of flare and weal areas after intradermal injection of histamine. The 2 compounds were approximately equipotent in blocking the flare and weal response to intradermal histamine and had a similar duration of action. Triprolidine impaired performance of vigilance and reaction time (p less than 0.05) compared with placebo while BW 825C did not. Drowsiness measured using visual analogue scales followed both triprolidine treatments, but not BW 825C. BW 825C had a plasma half-life (t1/2) of 1.7 +/- 0.2 h and triprolidine of 4.6 +/- 4.3 h. The peak plasma level of BW 825C was approximately 6 times that of triprolidine. It was concluded that BW 825C might be a clinically active H1-antagonist with reduced sedative side-effects.
新型H1受体拮抗剂BW 825C和曲普利啶（2.5毫克和5毫克）以双盲、安慰剂对照、均衡、交叉设计给予12名健康男性志愿者。通过评估皮内注射组胺后的风团和红晕面积来测定组胺拮抗作用。这两种化合物在阻断皮内注射组胺引起的风团和红晕反应方面大致等效，且作用持续时间相似。与安慰剂相比，曲普利啶会损害警觉性表现和反应时间（p<0.05），而BW 825C则不会。使用视觉模拟量表测量的嗜睡情况在两种曲普利啶治疗后均出现，但BW 825C治疗后未出现。BW 825C的血浆半衰期（t1/2）为1.7±0.2小时，曲普利啶为4.6±4.3小时。BW 825C的血浆峰值水平约为曲普利啶的6倍。结论是BW 825C可能是一种具有降低镇静副作用的临床活性H1拮抗剂。
