Synthesis and Pharmacology of 3-Isoxazolol Amino Acids as Selective Antagonists at Group I Metabotropic Glutamic Acid Receptors. -Amino acids (VIII) as well as the pentyl and heptyl analogues are prepared in order to study the relationship between the structure of the 4-substituents and the pharmacology of these compounds. Amino acids (VIII) are resolved using chiral HPLC. All compounds are tested in receptor binding assays for iGluR activity, in an in vitro electrophysiological model, and in second-messenger assays for mGlu 1 , mGlu 2 , mGlu 4 , and mGlu 5 receptor activity. In addition, compound (VIIIa) is tested for activity against NMDA-induced convulsions in mice.

Ionotropic Excitatory Amino Acid Receptor Ligands. Synthesis and Pharmacology of a New Amino Acid AMPA Antagonist.-One of the prepared title compounds (VIII) is found to be a potent and selective AMPA receptor antagonist.-(MADSEN, ULF; SLOEK, FRANK A.; STENSBOEL, TINE B.; BRAEUNER-OSBORNE, HANS; LUETZHOEFT, HANS-CHRISTIAN H.; POULSEN, MIGUEL V.; ERIKSEN, LISBETH; KROGSGAARD-LARSEN, POVL; Eur.

Structural Determinants for AMPA Agonist Activity of Aryl or Heteroaryl Substituted AMPA Analogues. Synthesis and Pharmacology.-AMPA analogues, containing methoxy-and hydroxyphenyl, as well as pyrazinyl substituents are prepared and evaluated pharmacologically. Key step in the synthesis is the formation of the 3-isoxazolol ring. -(SOERENSEN, ULRICK S.; FALCH, ERIK; STENSBOEL, TINE B.; JAROSZEWSKI, JERZY W.; MADSEN, ULF; KROGSGAARD-LARSEN, POVL; Arch. Pharm. (Weinheim, Ger.) 334 (2001) 2, 62-68; Dep. Med. Chem., R. Dan. Sch. Pharm., DK-2100 Copenhagen, Den.; EN)

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1996 carbamic acid derivatives carbamic acid derivatives (acyclic compounds) P 0480 24 -104 Analogues of Carbacholine: Synthesis and Relationship Between Structure and Affinity for Muscarinic and Nicotinic Acetylcholine Receptors. -A series of acyclic (cf. (V)) and heterocyclic analogues (cf. (XI), ( XVII)) of carbacholine are synthesized and their pharmacological profiles are estimated on the basis of ligand receptor binding studies. -(SOEKILDE, B.; MIKKELSEN, I.; STENSBOEL, T. B.; ANDERSEN, B.; EBDRUP, S.; KROGSGAARD-LARSEN, P.; FALCH, E.; Arch. Pharm. (Weinheim, Ger.) 329 (1996) 2, 95-104; PharmaBiotec Res. Cent., Dep. Med. Chem., Royal Dan. Sch. Pharm., DK-2100 Copenhagen, Den.; EN)