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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Adler B A, Goodman R R, Pasternak G W

Cotzias Laboratory of Neuro-Oncology, Memorial Sloan-Kettering Cancer Center, New York, New York 10021.

Cell Mol Neurobiol. 1988 Dec;8(4):471-6. doi: 10.1007/BF00711230.

Meptazinol is an interesting opioid-producing naloxone-reversible analgesia with few cardiovascular and respiratory effects. Recent studies indicate that mu 1 opioid receptors mediate meptazinol analgesia. Using a computerized autoradiographic subtraction technique, we have examined the regional distribution of meptazinol-sensitive [3H][D-Ala2,MePhe4,Gly(ol)5]enkephalin (DAGO) binding and compared this with the distribution of mu 1 binding determined by competition with low [D-Ala2,D-Leu5]enkephalin (DADL) concentrations. 2. Meptazinol and DADL lowered [3H]DAGO to similar extents in most brain regions studied. The greatest levels of inhibition were observed in the periaqueductal gray, interpeduncular nucleus, thalamus, hypothalamus, and hippocampus. Low levels of inhibition were found in the temporal and frontal cortex. The correlation between the inhibition of [3H]DAGO binding by meptazinol and that by DADL was high (r = 0.83), consistent with the binding of meptazinol to mu 1 sites.

美普他酚是一种有趣的阿片类药物，能产生纳洛酮可逆性镇痛作用，对心血管和呼吸系统影响较小。近期研究表明，μ1阿片受体介导美普他酚的镇痛作用。我们使用计算机自动放射照相减法技术，研究了美普他酚敏感的[3H][D-丙氨酸2，甲硫氨酸苯丙氨酸4，甘氨酸（醇）5]脑啡肽（DAGO）结合的区域分布，并将其与通过低浓度[D-丙氨酸2，D-亮氨酸5]脑啡肽（DADL）竞争测定的μ1结合分布进行比较。2. 在大多数研究的脑区中，美普他酚和DADL降低[3H]DAGO的程度相似。在导水管周围灰质、脚间核、丘脑、下丘脑和海马体中观察到最大程度的抑制。在颞叶和额叶皮质中发现抑制水平较低。美普他酚对[3H]DAGO结合的抑制与DADL的抑制之间的相关性很高（r = 0.83），这与美普他酚与μ1位点的结合一致。

Adler B A, Goodman R R, Pasternak G W

Cotzias Laboratory of Neuro-Oncology, Memorial Sloan-Kettering Cancer Center, New York, New York 10021.

Cell Mol Neurobiol. 1988 Dec;8(4):471-6. doi: 10.1007/BF00711230.

Meptazinol is an interesting opioid-producing naloxone-reversible analgesia with few cardiovascular and respiratory effects. Recent studies indicate that mu 1 opioid receptors mediate meptazinol analgesia. Using a computerized autoradiographic subtraction technique, we have examined the regional distribution of meptazinol-sensitive [3H][D-Ala2,MePhe4,Gly(ol)5]enkephalin (DAGO) binding and compared this with the distribution of mu 1 binding determined by competition with low [D-Ala2,D-Leu5]enkephalin (DADL) concentrations. 2. Meptazinol and DADL lowered [3H]DAGO to similar extents in most brain regions studied. The greatest levels of inhibition were observed in the periaqueductal gray, interpeduncular nucleus, thalamus, hypothalamus, and hippocampus. Low levels of inhibition were found in the temporal and frontal cortex. The correlation between the inhibition of [3H]DAGO binding by meptazinol and that by DADL was high (r = 0.83), consistent with the binding of meptazinol to mu 1 sites.

美普他酚是一种有趣的阿片类药物，能产生纳洛酮可逆性镇痛作用，对心血管和呼吸系统影响较小。近期研究表明，μ1阿片受体介导美普他酚的镇痛作用。我们使用计算机自动放射照相减法技术，研究了美普他酚敏感的[3H][D-丙氨酸2，甲硫氨酸苯丙氨酸4，甘氨酸（醇）5]脑啡肽（DAGO）结合的区域分布，并将其与通过低浓度[D-丙氨酸2，D-亮氨酸5]脑啡肽（DADL）竞争测定的μ1结合分布进行比较。2. 在大多数研究的脑区中，美普他酚和DADL降低[3H]DAGO的程度相似。在导水管周围灰质、脚间核、丘脑、下丘脑和海马体中观察到最大程度的抑制。在颞叶和额叶皮质中发现抑制水平较低。美普他酚对[3H]DAGO结合的抑制与DADL的抑制之间的相关性很高（r = 0.83），这与美普他酚与μ1位点的结合一致。