The compound N-(5-pyrrolidino-3-pentynyl)-pyrrolidin-2-one or its therapeutically acceptable salts has been found to be a long lasting antagonist to the tremorogenic effects of oxotremorine.

An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist. The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.

The invention relates to novel derivatives of melatonin, to the production of such new derivatives, to labelled forms, and especially radioactively tagged forms of such compounds, to assays for melatonin receptor function based on such radioactively tagged compounds and to pharmaceutical compositions which contain such novel non-labelled compounds. The novel compounds are potent antagonists of melatonin which are of value in human medicine and also in animal husbandry.

The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl option...

The invention concerns a compound of the formula ##STR1## and salts thereof resulting from addition with pharmaceutically acceptable mineral or organic acid, wherein R is an alkylenedioxy group substituted at the 2',3'-position, and R.sub.1 and R.sub.2 are selected from the group consisting of a linear or branched alkyl having 1-4 carbon atoms, a methoxyethyl, or a 2-pyridyl methyl group. The compounds of the present invention are useful in relaxing cardiac or smooth muscle.

A method of suppressing vasoconstriction in a warm-blooded animal which comprises administering to said warm-blooded animal an effective amount of a serotonin antagonist compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen, halo, C.sub.1 -C.sub.5 alkoxy or C.sub.2 -C.sub.6 dialkyl amino; R.sup.2 is hydrogen, halo or C.sub.1 -C.sub.5 alkoxy; R.sup.3 is hydrogen, hydroxy, --O--(CH.sub.2).sub.n --COOH or --O--CO--(CH.sub.2).sub.l --COOH, wherein n is an integer of 1-5, and l is an int...

A novel compound is disclosed for inhibiting the effects of oxytocin in a female mammal. As an analog of oxytocin the compound is named [(S)PMP.sup.1,D-Trp.sup.2,Pen.sup.6,Arg.sup.8 ] oxytocin. This compound can be administered to pregnant women to arrest premature labor while avoiding unwanted side effects due to antagonism of the antidiuretic hormone, vasopressin.

A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: ##STR00001## wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.

The instant invention relates to some tripeptide derivatives having activity against endothelin a process for preparing them, pharmaceutical composition containing the same and their use in prevention or treatment of some diseases associated with endothelin.

A galanin antagonist which is a galanin receptor ligand is described. New peptides, Galanin (1-12)-Pro-Substance P(5-11), Galanin (1-12)-Pro-Bradykinin(2-9), Galanin (1-12)-Pro-Pro-Pro- (Leu.sup.5 -Enkephalin (5-1), Galanin (1-12)-Pro-Lys(.epsilon.-NH-)Pro-(Leu5-Enkephalin (5-1) and functional analogues and functional derivatives thereof are disclosed. The peptides are used in pharmaceutical preparations to treat a disorder in a mammal which depends on the physiological function of galanin at th...