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Synthesis of conformationally-constrained antagonists of LHRH

✍ Scribed by Roger W. Roeske; Zhenping Tian; Patrick Edwards; Tanya Hrinyo-Pavlina; Nisheth Chaturvedi; Maria Kowalczuk; Robert P. Millar; Colleen Shapiro; Kenneth D. Kopple

Book ID
115844762
Publisher
Elsevier Science
Year
1992
Tongue
English
Weight
36 KB
Volume
46
Category
Article
ISSN
0010-7824

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Synthesis of conformationally-constraine
Synthesis of conformationally-constrained stereospecific analogs of glutamic acid as antagonists of metabotropic receptors
✍ FrΓ©dΓ©rique Tellier; Francine Acher; Isabelle Brabet; Jean-Philippe Pin; JoΓ«l Boc πŸ“‚ Article πŸ“… 1995 πŸ› Elsevier Science 🌐 English βš– 332 KB

Rigid analogs of ACPD have been synthesized to mimick different potential conformations of ACPD in aqueous solution. One of them, (+)-ABHD-I is a competitive antagonist at mGluRla receptor with a KB value of 300 laM. Glutamic acid is a major excitatory amino acid and neurotransmitter in the central