Morin-Surun M P, Gacel G, Champagnat J, Denavit-Saubie M, Roques B P
Eur J Pharmacol. 1984 Feb 17;98(2):241-7. doi: 10.1016/0014-2999(84)90595-8.
The opiate receptors of central neurons related to the generation of the respiratory rhythm were identified using microiontophoresis of the synthetic opioid peptides DSLET (Tyr-D-Ser-Gly-Phe-Leu-Thr) and TRIMU-4 (Tyr-D-Ala-Gly-NH-CH (CH3)-CH2-CH(CH3)2), exhibiting a high selectivity for delta and mu receptors respectively. Both agonists induced depressions of spontaneous and L-glutamate-induced discharges; the effects were antagonized by naloxone and not mimicked by a related almost inactive peptide DSLLET (Tyr-D-Ser-Gly-Leu-Leu-Thr). The effect of DSLET had a faster time course than that of TRIMU-4 and persisted after prolonged applications of TRIMU-4. It is concluded that delta and mu receptors subtypes are distinct and are both present on central respiratory-related neurons.
使用合成阿片肽DSLET（酪氨酰-D-丝氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸）和TRIMU-4（酪氨酰-D-丙氨酰-甘氨酰-NH-CH(CH₃)-CH₂-CH(CH₃)₂）的微量离子电泳技术，分别鉴定了与呼吸节律产生相关的中枢神经元的阿片受体，这两种肽对δ受体和μ受体分别具有高选择性。两种激动剂均诱导自发性放电和L-谷氨酸诱导的放电减少；这些效应可被纳洛酮拮抗，而与之相关的几乎无活性的肽DSLLET（酪氨酰-D-丝氨酰-甘氨酰-亮氨酰-亮氨酰-苏氨酸）则不能模拟该效应。DSLET的作用时相比TRIMU-4更快，并且在长时间应用TRIMU-4后仍持续存在。结论是，δ受体和μ受体亚型是不同的，且均存在于中枢呼吸相关神经元上。
