Kindgen-Milles D, Klement W
Abteilung für Experimentelle Anaesthesiologie, Heinrich-Heine-Universität Düsseldorf, Germany.
Eur J Pharmacol. 1992 Jul 21;218(1):183-5. doi: 10.1016/0014-2999(92)90164-y.
We showed the intrinsic effects of the bradykinin (BK) receptor antagonists, NPC 567 (D-Arg-[Hyp3,D-Phe7]BK) and NPC 349 (D-Arg-[Hyp3,Thi5,8,D-Phe-7]BK), in the skin of humans. NPC 567 and NPC 349 caused dose-dependent pain, wheal, and flare on intracutaneous injection. After bradykinin, only the pain, but not the wheal and flare reactions were dose-dependent. The intravenous application of antihistamines (dimetidinmaleate and ranitidine) had little effect on pain intensity and reduced both wheal and flare response to the antagonists but not to bradykinin. We conclude that NPC 567 and NPC 349 have pain-evoking and histamine-releasing properties in the skin of humans which may limit their therapeutic and experimental use.
我们展示了缓激肽（BK）受体拮抗剂NPC 567（D-精氨酸-[Hyp3，D-苯丙氨酸7]BK）和NPC 349（D-精氨酸-[Hyp3，硫代5,8，D-苯丙氨酸-7]BK）在人体皮肤中的内在作用。NPC 567和NPC 349皮内注射后会引起剂量依赖性疼痛、风团和潮红。注射缓激肽后，只有疼痛呈剂量依赖性，而风团和潮红反应并非如此。静脉应用抗组胺药（马来酸二甲替啶和雷尼替丁）对疼痛强度影响不大，可降低拮抗剂引起的风团和潮红反应，但对缓激肽引起的反应无效。我们得出结论，NPC 567和NPC 349在人体皮肤中具有诱发疼痛和释放组胺的特性，这可能会限制它们在治疗和实验中的应用。
