| Literature DB >> 11412984 |
B Ebert1, M Mortensen, S A Thompson, J Kehler, K A Wafford, P Krogsgaard-Larsen.
Abstract
The potency and efficacy of a series of bioisosterically modified GABA analogues were determined electrophysiologically using heteromeric GABA(A) receptors expressed in Xenopus oocytes. These agonist parameters were shown to be strongly dependent on the receptor subunit combination. On the other hand, the antagonist potencies of the classical GABA(A) antagonists SR 95531 (7) and BMC (8) and also of 5g and the phosphinic acid bioisosteres of 5a, compounds 5f and 6, were essentially independent of the receptor subunit combinations.Entities:
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Year: 2001 PMID： 11412984 DOI： 10.1016/s0960-894x(01)00184-6
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823