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Synthesis and some pharmacological properties of [4-threonine, 7-glycine]oxytocin, [1-(L-2-hydroxy-3-mercaptopropanoic acid), 4-threonine, 7-glycine]oxytocin (hydroxy[Thr4, Gly7]oxytocin), and
Threonine substitution has brought about a substantial enhancement in oxytocic activity and a fivefold enhancement in O/A selectivity in these peptides, which might offer a greater margin of safety than oxytocin in those clinical stiuations in which the latter is currently employed.
The design of effective in vivo antagonists of rat uterus and milk ejection responses to oxytocin.
It is concluded that changes in the 1-position (1-deaminopenicillamine substitution) and the 2- position (2-O-methyltyrosine or 2-phenylalanine substitution) can have additive effects on antagonistic activities.
[1-deaminopenicillamine,4-valine]-8-D-arginine-vasopressin, a highly potent inhibitor of the vasopressor response to arginine-vasopressin.
dPVDAVP with its potent and specific ability to antagonize the vasopressor effects of AVP should be a useful pharmacological tool with which to explore the possible participation of A VP's potent vasoconstrictor properties in cardiovascular regulation in physiological and pathological states.
[1-(beta-mercapto-beta,beta-cyclopentamethylenepropionic acid),4-valine,-8-D-arginine]vasopressin, a potent and selective inhibitor of the vasopressor response to arginine-vasopressin.
d(CH2)5VDAVP is one of the most potent and selective vasopressor antagonists reported to date and should be a useful tool with which to probe the possible role(s) that AVP may play in cardiovascular regulation under normal and pathological conditions.
[1-Deaminopenicillamine,4-threonine]oxytocin, a potent inhibitor of oxytocin.
The substitution of threonine for glutamine in the antagonist [1-deaminopenicilliamine]oxytocin has effected a twofold increase in inhibitory potency, one of the most potent inhibitors of oxytocin known to date.
Synthetic antagonists of in vivo responses by the rat uterus to oxytocin.
Compounds 2-4 are among the most potent in vivo antagonists of oxytocin reported to date and antagonize the actions of Oxytocin on the rat uterus.
Design of neurohypophyseal peptides that exhibit selective agonistic and antagonistic properties.
Analysis of the pharmacological data from over 300 analogs of oxytocin and vasopressin allows the delineation of those structural modifications that can optimize selectivities, and the potential and limitations of this approach for the design of peptides possessing desired agonistic or antagonistic selectivity are discussed.
[1-(L-2-hydroxy-3-mercaptopropanoic acid)] analogues of arginine-vasopressin, [8-D-arginine]vasopressin, and [4-valine,8-D-arginine]vasopressin.
Hydroxy-VDAVP is a highly specific antidiuretic peptids and may be useful in pharmacological studies of antidiuresis.
Studies on the extended active site of papain.
The molecular conformation of cyclotri-β-alanyl
The title compound has been studied by molecular mechanics calculations. There is no single, well defined global minimum energy conformation and the low energy conformations are unrelated to the