Some biological properties of an "irreversible" antagonist of neurohypophyseal hormones, deamino-[Phe(4-BrCH2CONH)2]-oxytocin, and its isosteric analogue, deamino-[Phe(4-CH3CH2CONH)2]-oxytocin. 1978

V Pliska, and P Marbach

The 2-p-bromoacetylaminophenylalanine analogue of deamino-oxytoxin displayed some features of an irreversible inhibitor of oxytocin on rat uterus (long persistence of inhibitory effect, slow wash-out from the tissue). An isosteric analogue with a propionylamino group at the same position was, under similar experimental conditions, also an antagonist of oxytocin, but the features of an irreversible inhibitor were lacking. pA2 values of the two substances are between 6.5 and 6.9. The "irreversibility" of the former compound is concentration dependent and it is concluded that it cannot be entirely caused by a covalent binding of the inhibitor to the uterus receptor for oxytoxin. Like many other similar inhibitors, the substances display only an inefficient in vivo inhibition of the vasopressor effect of lysine vasopressin in rats.

UI MeSH Term Description Entries
D008236 Lypressin The porcine antidiuretic hormone (VASOPRESSINS). It is a cyclic nonapeptide that differs from ARG-VASOPRESSIN by one amino acid, containing a LYSINE at residue 8 instead of an ARGININE. Lys-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE. Lysine Vasopressin,Vasopressin, Lysine,8-Lysine Vasopressin,Diapid,Lys-Vasopressin,Lysyl Vasopressin,Postacton,8 Lysine Vasopressin,Lys Vasopressin,Vasopressin, 8-Lysine,Vasopressin, Lysyl
D008297 Male Males
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D010121 Oxytocin A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION. Ocytocin,Pitocin,Syntocinon
D010909 Pituitary Hormones, Posterior Hormones released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). They include a number of peptides which are formed in the NEURONS in the HYPOTHALAMUS, bound to NEUROPHYSINS, and stored in the nerve terminals in the posterior pituitary. Upon stimulation, these peptides are released into the hypophysial portal vessel blood. Neurohypophyseal Hormones,Pituitrin,Neurohypophyseal Peptides,Posterior Pituitary Hormones
D001794 Blood Pressure PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS. Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
D005260 Female Females
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D014590 Uterine Contraction Contraction of the UTERINE MUSCLE. Myometrial Contraction,Contraction, Myometrial,Contraction, Uterine,Contractions, Myometrial,Contractions, Uterine,Myometrial Contractions,Uterine Contractions
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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