Raffa R B, Martinez R P, Porreca F
R.W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477.
Eur J Pharmacol. 1992 Jun 17;216(3):453-6. doi: 10.1016/0014-2999(92)90446-b.
The antinociceptive efficacy of [D-Pen2,D-Pen5]enkephalin (DPDPE) (delta 1 agonist) and [D-Ala2,Glu4]deltorphin (delta 2 agonist) was evaluated following intracerebroventricular (i.c.v.) or intrathecal (i.t.) administration in CD-1 and CXBK strains of mice using the radiant heat tail-flick test. Following i.c.v. administration, [D-Ala2,Glu4]deltorphin was effective in CD-1, but not CXBK, mice; DPDPE was approximately equiactive in both strains. While i.c.v. [D-Ala2,Glu4]deltorphin did not produce antinociception in the CXBK mouse, it effectively antagonized the antinociceptive actions of i.c.v. DPDPE. [D-Ala2,Glu4]deltorphin was effective following i.t. administration in both strains. These data suggest possible differences in the supraspinal populations of opioid delta receptor subtypes in the CXBK strain. On the basis of previously established selectivity of these agonists, the CXBK mouse may have a predominate population of supraspinal opioid delta 1, rather than delta 2, receptors.
采用辐射热甩尾试验，在CD-1和CXBK品系小鼠中，经脑室内（i.c.v.）或鞘内（i.t.）注射后，评估了[D-青霉胺2，D-青霉胺5]脑啡肽（DPDPE）（δ1激动剂）和[D-丙氨酸2，谷氨酸4]强啡肽（δ2激动剂）的镇痛效果。脑室内注射后，[D-丙氨酸2，谷氨酸4]强啡肽对CD-1小鼠有效，但对CXBK小鼠无效；DPDPE在两种品系中活性大致相同。虽然脑室内注射[D-丙氨酸2，谷氨酸4]强啡肽对CXBK小鼠没有产生镇痛作用，但它有效地拮抗了脑室内注射DPDPE的镇痛作用。[D-丙氨酸2，谷氨酸4]强啡肽经鞘内注射后在两种品系中均有效。这些数据表明，CXBK品系中阿片类δ受体亚型的脊髓上群体可能存在差异。根据这些激动剂先前确定的选择性，CXBK小鼠脊髓上阿片类δ1受体而非δ2受体的群体可能占主导地位。
