摘要:
A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.
摘要:
A method is disclosed for the treatment of neuropsychopharmacological disorders which are associated with or result from excessive activation of the N-methyl-D-aspartate receptor complex, which method comprises administering an effective neuropsychopharmacological disorder-treating amount of a compound possessing partial agonist properties for the strychnine insensitive glycine modulatory sites of N-methyl-D-aspartate receptors. Exemplary of partial agonists which are useful in the method of the invention are 1-aminocyclopropanecarboxylic acid, and associated derivates thereof. Novel injectable pharmaceutical compositions are also disclosed.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is CH.dbd.CY--C(CH.sub.3).dbd.CHX wherein X and Y are different and each is of the formula ##STR2## wherein R' and R" independently are H or alkyl of C.sub.1-6 and R.sub.1 includes all possible geometric isomers are demonstrated effective in treating inflammation, both topically and internally. The mechanism appears to be the inhibition of phospholipase A.sub.2 enzymes.