Hydro-osmotic activity of "carba' analogues of oxytocin and [8-arginine] vasopressin on frog (Rana esculenta) bladder.
The biological potency of neurohypophysial hormone analogues in stimulating water transport across the frog bladder (Rana esculenta) was estimated from the pD2 (negative logarithm of the peptide concentration eliciting 50% of its maximal hydroosmotic effect) and from the maximal response. Most analogues elicited maximal responses similar to those of the natural hormones. Both replacement of sulfur by a methylene group in the disulfide bridge and omission of the terminal amino group in oxytocin reduced hydroosmotic activity; carba substitution in oxytocin led to a greater drop in pD2 than the same substitution in deamino-oxytocin. On the contrary, the effects of substituting phenylalanine for tyrosine and of omitting the amino group were almost additive. Elimination of the carboxyl-terminal tripeptide sequence considerably reduced hydroosmotic potency; pressinamide was inactive up to 3 mug/ml. The highly potent antidiuretic peptides, deamino-[D-Arg8]vasopressin and deamino-6-carba-]D-Arg8]vasopressin, were weakly active in the hydroosmotic assay.
D000595:Amino Acid Sequence; D000818:Animals; D001127:Arginine Vasopressin / Q000031:analogs & derivatives / Q000494:pharmacology*; D002463:Cell Membrane Permeability / Q000187:drug effects*; D066298:In Vitro Techniques; D010121:Oxytocin / Q000031:analogs & derivatives / Q000494:pharmacology*; D010443:Peptide Chain Termination, Translational; D011893:Rana esculenta; D001743:Urinary Bladder / Q000187:drug effects*; D014667:Vasopressins / Q000031:analogs & derivatives*
D014667:Vasopressins; D001127:Arginine Vasopressin; D010121:Oxytocin