Schoepp D D, Johnson B G, True R A, Monn J A
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285.
Eur J Pharmacol. 1991 Aug 14;207(4):351-3. doi: 10.1016/0922-4106(91)90010-f.
(1S,3R)-1-Aminocyclopentane-1,3-dicarboxylic acid (1S,3R-ACPD) and (1R,3S)-1-aminocyclopentane-1,3-dicarboxylic acid (1R,3S-ACPD) were characterized for potency, efficacy, and selectivity at metabotropic excitatory amino acid receptors. 1S,3R-ACPD stimulated [3H]phosphoinositide hydrolysis in slices of the neonatal and adult rat hippocampus with full efficacy and twice the potency relative to what has been shown for (+/-)-trans-ACPD. 1S,3R-ACPD was up to 30 times more potent in activating metabotropic excitatory amino acid receptors, compared to its affinity for [3H]CGS19755 binding to NMDA receptors. In contrast, 1R,3S-ACPD was much less potent, efficacious, and selective than 1S,3R-ACPD. Although 1S,3R-ACPD is not specific, it is a most selective and efficacious agonist at metabotropic excitatory amino acid receptors.
对（1S,3R）-1-氨基环戊烷-1,3-二羧酸（1S,3R-ACPD）和（1R,3S）-1-氨基环戊烷-1,3-二羧酸（1R,3S-ACPD）在代谢型兴奋性氨基酸受体上的效力、效能和选择性进行了表征。1S,3R-ACPD在新生和成年大鼠海马切片中刺激[3H]磷酸肌醇水解，效能完全，效力是（±）-反式-ACPD的两倍。与它对[3H]CGS19755结合NMDA受体的亲和力相比，1S,3R-ACPD激活代谢型兴奋性氨基酸受体的效力高达30倍。相比之下，1R,3S-ACPD的效力、效能和选择性比1S,3R-ACPD低得多。虽然1S,3R-ACPD不具有特异性，但它是代谢型兴奋性氨基酸受体上最具选择性和效能的激动剂。
