Beets J L, Meade H M, Morley J
Int Arch Allergy Appl Immunol. 1980;61(4):449-56. doi: 10.1159/000232473.
The effects of PRD-92 Ea were examined on the increased plasma protein extravasation in the skin of guinea pig and rat elicited by specific antigens and spasmogenic mediators. PRD-92 Ea was found to be a potent inhibitor of rat PCA reactions when administered intradermally, intravenously or orally. This compound did not antagonize the local inflammatory responses of histamine, bradykinin or 5HT. This implies that in vivo PRD-92 Ea acts predominantly as an anti-allergy agent rather than a spasmogen antagonist. At high concentrations PRD-92 Ea directly increased vascular permeability when injected intradermally (greater than 250 micrograms/site) or administered by aerosol into the lung (greater than 10%). The importance of investigating such direct irritant actions of similar new drugs is discussed.
研究了PRD - 92 Ea对豚鼠和大鼠皮肤中由特异性抗原和致痉介质引起的血浆蛋白外渗增加的影响。发现PRD - 92 Ea经皮内、静脉或口服给药时,是大鼠被动皮肤过敏反应(PCA)的有效抑制剂。该化合物不拮抗组胺、缓激肽或5 - 羟色胺(5HT)的局部炎症反应。这表明在体内PRD - 92 Ea主要作为一种抗过敏剂,而非致痉原拮抗剂。高浓度时,皮内注射(大于250微克/部位)或经气溶胶吸入肺部(大于10%)PRD - 92 Ea可直接增加血管通透性。讨论了研究类似新药这种直接刺激作用的重要性。