氟哌啶醇在增强脑膜与依托啡结合的同时加强针刺镇痛

THE POTENTIATION EFFECT OF HALOPERIDOL ON THE BIXDING OF ETORPHINE TO BRAIN MEMBRANES IN ACUPUNCTURE ANALGESIA

用氚标记依托啡［３Ｈ］－ｅｔｏｒｐｈｉｎｅ与兔脑匀浆蛋白作受体结合试验，Ｓｃａｔｃｈａｒｄ分析的结果显示兔脑内的阿片受体有高低两种亲和力结合，对照组兔脑高亲和力解离常数Ｋｄｌ为２．５７±０．３３ｎｍｏｌ／Ｌ，氟哌啶醇（ｈａｌｏｐｅｒｉｄｏｌ，ｈａｌ）或针刺引起镇痛时，Ｋｄｌ值分别降至１．４４±０．０３ｎｍｏｌ／Ｌ和１．５３±０．０５ｎｍｏｌ／Ｌ（Ｐ＜０．０５）；当ｈａｌ和针刺合用进一步加强镇痛时，Ｋｄｌ值进一步降至１．２５±０．３３ｎｍｏｌ／Ｌ（Ｐ＜０．０１），提示在ｈａｌ加强针刺镇痛时兔脑阿片受体的亲和力提高。兔脑同［３Ｈ］－ｅｔｏｒｐｈｉｎｅ作体外受体结合放射自显影，结果显示ｈａｌ加强针刺镇痛时，尾核、视前外侧区、丘脑室旁核、中央正中核、丘脑背外侧核和中脑导水管周围灰质等脑区的阿片受体结合密度均有显著提高。上述结果提示，多巴胺受体拮抗剂ｈａｌ加强针刺镇痛的机制之一，可能是由于产生了脑内阿片受体的上行调节。

H]-etorphine was used in receptor binding studies on membrane preparation from rabbit brain. Scatchard analysis revealed that rabbit brain had two different affinity binding sites. In the high affinity site, the dissociation constant (Kdl) of the control group was 2. 57± 0. 33 nmol/L. When analgesia was induced by haloperidol or acupuncture, the Kdl values decreased respectively (P<0. 05) to 1. 44±0. 03 nmol/L and 1. 53±0. 05 nmol/L. These Kdl values further decreased to 1. 25± 0. 03 nmol/L when acupuncture analgesia was potentiated by combined action of acupuncture and iv.haloperidol (P<0. 01). In case of autoradiographic analysis of brain slices showed that the density of opioid receptors in many brain regions, such as N. Caudatus, preoptic lateral area, N. Paraventricularis, N. Centromedianus, Periaqueductal gray, showed significant increase, a results indicating that the upregulation of opioid receptors in rabbit brain may be one of the mechanisms in the potentiating action of haloperidol on acupuncture analgesia.