Corticotropin Releasing Activity of Lysine Vasopressin Analogues

A polarographic study of the hydrolysis of [8-lysine]vasopressin and some hormonogens of the vasopressin series with the blood serum of women in the last week of pregnancy was studied. The dependence of hydrolysis on pH (pH optimum: 7.4-7.50, substrate concentration (Km 1.2 . 10-5M), pH stability and thermal stability were determined. The rate of hydrolysis of individual vasopressin analogues decreases in the order: [8-lysine]vasopressin > Nα-glycyl-prolyl[8-lysine]-vasopressin > Nα-leucyl-[8-lysine]vasopressin > Nα-alanyl-[8-lysine]vasopressin > Nα-phenyl alanyl-[8-lysine]vasopressin > Nα-diglycyl-[8-lysine]vasopressin > Nα-prolyl-[8-lysine]vasopressin > Nα-triglycyl-[8-lysine]vasopressin > Nα-sarcosyl-glycyl-[8-lysine]vasopressin. The degree of hydrolysis gradually increases to a multiple with the length of the pregnancy in consequence of the presence of oxytocine. However, vasopressin is also hydrolysed to a small extent with the enzymes from the blood sera of non-pregnant women. Under similar analytical conditions oxytocin was not hydrolysed with the sera of non-pregnant women and therefore oxytocin is a more suitable substrate than vasopressin for polarographic determination of serum oxytocinase.

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Synthesis of two lysine-vasopressin analogues with protracted hormonal activity

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19630747 ◽

1963 ◽

Vol 28 (3) ◽

pp. 747-749 ◽

Cited By ~ 14

Author(s):

M. Zaoral ◽

V. Pliška ◽

K. Řežábek ◽

F. Šorm

Keyword(s):

Hormonal Activity ◽

Lysine Vasopressin ◽

Vasopressin Analogues

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Tryptic splitting of vasopressin analogues containing homologues of lysine or arginine in position 8

Collection of Czechoslovak Chemical Communications ◽

10.1135/cccc19792451 ◽

1979 ◽

Vol 44 (8) ◽

pp. 2451-2454

Author(s):

Anastasia Dimeli ◽

Tomislav Barth

Keyword(s):

Amino Acid ◽

Arginine Vasopressin ◽

Basic Amino Acid ◽

Peptide Bond ◽

Peptide Chain ◽

Side Chain ◽

Lysine Vasopressin ◽

Vasopressin Analogues

Vasopressin analogues containing an amino acid with a shorter side chain in position 8 of the peptide chain were more resistant to tryptic splitting of the peptide bond formed by the basic amino acid and terminal glycine amide. In the lysine vasopressin series, analogues with ornithine or lower homologues of lysine in position 8 were not hydrolyzed. In the arginine vasopressin series, the analogue containing 3-guanidino-2-aminopropionic acid in position 8 was completely resistant to the action of trypsin. The vasopressin analogue with norarginine in position 8 was split at a lower rate than natural arginine vasopressin.

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The Factor VIII Response to Synthetic Vasopressin Analogues in Man

10.1055/s-0039-1689480 ◽

1975 ◽

Author(s):

J. D. Cash ◽

G. Sas

Keyword(s):

Factor Viii ◽

Arginine Vasopressin ◽

Haemophilia A ◽

Healthy Male ◽

Lysine Vasopressin ◽

Parallel Increase ◽

Immunological Assays ◽

Vasopressin Analogues ◽

Therapeutic Possibilities ◽

Future Management

Biological and immunological assays for factor VIII were performed on 6 healthy male volunteers before, during and after the intravenous infusion (10 μg in 15 minutes) of a variety of synthetic vasopressin analogues, which included arginine vasopressin (AVP), lysine vasopressin (LVP), l-Desamino-8-d-arginine vasopressin (DDAVP), vasotocin (VOT), l-Desamino-carb6-8-d-arginine vasopressin (DCAVP), and 1-Desamino-N-methylar-ginine8 vasopressin (DMAVP). No significant changes occurred during or after the administration of VOT and DMAVP. However, AVP, LVP, DDAVP and DCAVP all produced a significant and parallel increase in the biological and immunological levels of factor VIII. These results point to the possibility that vasopressin may play a role in controlling the release and/or synthesis of factor VIII in man, and, as DDAVP and DCAVP are devoid of unpleasant side-effects, indicate new therapeutic possibilities for the future management of patients with mild or moderate haemophilia A.

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EVALUATION OF PITUITARY-ADRENAL FUNCTION IN CHILDREN

Acta Endocrinologica ◽

10.1530/acta.0.0480081 ◽

1965 ◽

Vol 48 (1) ◽

pp. 81-90 ◽

Cited By ~ 9

Author(s):

B. van der Wal ◽

T. Wiegman ◽

J. F. Janssen ◽

A. Delver ◽

D. de Wied

Keyword(s):

Blood Pressure ◽

Body Temperature ◽

Diastolic Blood Pressure ◽

Linear Increase ◽

Significant Rise ◽

Moderate Increase ◽

Specific Stimulus ◽

Lysine Vasopressin ◽

Free Cortisol ◽

Pituitary Adrenal Axis

ABSTRACT The reactivity of the hypothalamico-pituitary-adrenal axis was determined in 48 children, not suffering from any endocrine disorder. The free cortisol (F)- and corticosterone (B) content of plasma was determined in response to ACTH (clinical corticotrophin; A1 peptide), a corticotrophin releaser (lysine vasopressin) and a non specific stimulus (bacterial polysaccharide) as compared to saline. The two ACTH-preparations infused over one hour in a dose of 5 IU per child elicited a marked increase in both F and B. Lysine vasopressin in a dose of 0.5 IU per year of age similarly infused, exhibited a distinct linear increase in the two circulating cortical steroids, although the effect of this octapeptide was smaller than that of the two ACTH-preparations. Blood pressure was also measured during the infusion with vasopressin or saline. The systolic blood pressure was not significantly affected by vasopressin, but a significant rise in diastolic blood pressure was found. No correlation between the increase in diastolic blood pressure and in blood corticoids in response to vasopressin, was found. The intravenous administration of a relatively small amount of pyrifer caused a moderate increase in circulating F which was significant only at 4 and 6 hours after the injection of the pyrogen. The B content did not increase significantly above that of saline treated control children, presumably because of the relatively weak corticotrophic activity of the pyrogen under these conditions. A positive linear relation between body temperature and time was found. No correlation between increase in body temperature and increase in circulating F could be demonstrated.

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IMPAIRMENT OF THE PITUITARY-ADRENAL AXIS FOLLOWING PROLONGED THERAPY WITH CORTICOTROPHIN

Acta Endocrinologica ◽

10.1530/acta.0.0650608 ◽

1970 ◽

Vol 65 (4) ◽

pp. 608-616 ◽

Cited By ~ 5

Author(s):

M. J. Levell ◽

S. R. Stitch ◽

M. J. Noronha

Keyword(s):

Multiple Sclerosis ◽

Adrenal Function ◽

Withdrawal Symptoms ◽

Prolonged Therapy ◽

Adrenal Axis ◽

Lysine Vasopressin ◽

Subsequent Response ◽

Pituitary Adrenal Axis

ABSTRACT Pituitary-adrenal function was tested in a group of 33 patients with multiple sclerosis who had been treated with corticotrophin for at least 1 year. Assessment was made by measuring the change in the plasma 11-hydroxycorticosteroid concentration following lysine vasopressin (LVP) administration. Ten patients showed abnormally small increases after LVP. Two of the 5 patients with the smallest increases still showed impairment 8 months later. The patients with no withdrawal symptoms had normal or nearly normal increases following LVP. There was an association between the concentration of 11-hydroxycorticosteroids immediately after withdrawal of ACTH and the subsequent response to LVP.

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EFFECTS OF ARGININE-, LYSINE- AND LEUCINE-VASOPRESSIN ON URINARY OSMOLALITY AND RATE OF URINE FLOW IN HYDRATED RATS AND DOGS

Acta Endocrinologica ◽

10.1530/acta.0.xxxii0134 ◽

1959 ◽

Vol XXXII (I) ◽

pp. 134-141 ◽

Cited By ~ 10

Author(s):

Niels A. Thorn

Keyword(s):

Arginine Vasopressin ◽

Urine Osmolality ◽

Urine Flow ◽

The Other ◽

Maximum Increase ◽

Urinary Osmolality ◽

Lysine Vasopressin

ABSTRACT Arginine-, lysine- and leucine-vasopressin, injected i. v. into hydrated rats or dogs caused different patterns of response in that urine osmolality fell much more slowly after the maximum increase following arginine-vasopressin, than after the other two preparations. Using 3 different parameters for antidiuretic response, arginine-vasopressin was somewhat more potent than leucine-vasopressin in both rats and dogs, considerably more potent than lysine-vasopressin in rats, and much more so in dogs.

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