Kemp M C, Jane D E, Tse H W, Roberts P J
Department of Pharmacology, School of Medical Sciences, University of Bristol, UK.
Eur J Pharmacol. 1996 Aug 1;309(1):79-85. doi: 10.1016/0014-2999(96)00314-7.
A number of potential Group 2 and Group 3 metabotropic glutamate receptor (mGlu receptor) agonists were investigated in adult rat brain cerebrocortical slices. The rank order of their potency in inhibiting forskolin-stimulated adenylyl cyclase was found to be: (S)-2-amino-2-methyl-4-phosphonobutyric acid (MAP4) > (2S,1'S,2'S)-2-(2-carboxycyclopropyl)glycine (L-CCG-I) > (1S,3S)-1-aminocyclopentane-1,3-dicarboxylic acid (1S,3S-ACPD) > (1S,3R)-1-aminocyclopentane-1, 3-dicarboxylic acid (1S,3R)-ACPD) > (2S,1'R,2'R,3'R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV) > (S) -2-methylglutamate ((S)-MG) > L-glutamate > (2S,1'S, 2'S)-2-(2-carboxycyclopropyl)alanine (MCCG) > L-2-amino-4-phosphonobutyric acid (L-AP4) > L-serine-O-phosphate (SOP). The finding that (S)-2-amino-2-methyl-4-phosphonobutyric acid was the most potent agonist at these metabotropic glutamate receptors is in contrast to its observed potent mGlu receptor antagonist action in the neonatal rat spinal cord.
在成年大鼠脑皮质切片中研究了多种潜在的第2组和第3组代谢型谷氨酸受体（mGlu受体）激动剂。发现它们抑制福斯高林刺激的腺苷酸环化酶的效力顺序为：(S)-2-氨基-2-甲基-4-膦酰丁酸（MAP4）>(2S,1'S,2'S)-2-(2-羧基环丙基)甘氨酸（L-CCG-I）>(1S,3S)-1-氨基环戊烷-1,3-二羧酸（1S,3S-ACPD）>(1S,3R)-1-氨基环戊烷-1,3-二羧酸（1S,3R)-ACPD）>(2S,1'R,2'R,3'R)-2-(2,3-二羧基环丙基)甘氨酸（DCG-IV）>(S)-2-甲基谷氨酸（(S)-MG）>L-谷氨酸>(2S,1'S,2'S)-2-(2-羧基环丙基)丙氨酸（MCCG）>L-2-氨基-4-膦酰丁酸（L-AP4）>L-丝氨酸-O-磷酸（SOP）。(S)-2-氨基-2-甲基-4-膦酰丁酸在这些代谢型谷氨酸受体上是最有效的激动剂，这一发现与其在新生大鼠脊髓中观察到的强效mGlu受体拮抗剂作用形成对比。
