LH-RH-Peptides as contraceptives

DETAILED DESCRIPTION What is claimed is: 1.
The method of inducing a contraceptive effect in a male of female patient which comprises parenterally administering to said patient, over a period of at least four days, a daily dose from 0.
05 to 1.
0 micrograms per kilogram of body weight of a peptide of the formula Glu-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-NHC.
sub.
2 H.
sub.
5 wherein X is D-serine-tert.
butyl ether or D-glutamic acid .
delta.
-cyclohexyl amide.
2.
The method of inducing a contraceptive effect in a male or female patient which comprises intranasally administering to said patient, over a period of at least four days, a daily dose from 2 to 40 micrograms per kilogram of body weight of a peptide of the formula Glu-His-Trp-Ser-Tyr-X-Leu-Arg-Pro-NHC.
sub.
2 H.
sub.
5, wherein X is D-serine-tert.
butyl ether or D-glutamic acid .
delta.
-cyclohexyl amide.




Description:
This invention relates to the use of peptides of the formula ##STR2## in which X denotes D-serine-tert.
butyl ether or D-glutamic acid .
gamma.
-cyclohexylamide as contraceptives.
The aforementioned compounds are prepared by the processes disclosed in U.
S.
Pat.
No.
4,024,248 and U.
S.
Pat.
No.
4,118,483.
In test persons a single dose of 1.
4 to 20 mcg (corresponding to 20 to 300 ng/kg) administered intravenously (i.
v.
), subcutaneously (s.
c.
) or by the intramuscular route (i.
m.
) or of 50 to 1,000 mcg (corresponding to 100 to 5,000 ng/kg) administered intranasally (i.
n.
) causes the secretion of gonadotrophic hormones from the anterior lobe of the pituitary gland.
It has now been found that repeated doses of more than 2.
5 mcg i.
v.
, s.
c.
or i.
m.
(daily dose) or over about 100 mcg i.
n.
over a period of at least 4 days do not increase the effect but, surprisingly, that the effect is reversed so that the aforesaid compounds can be used as contraceptives when administered in appropriate doses to male and female mammals.
The mechanism of this effect may be explained as follows: The compounds administered have a strong effect on the release of gonadotrophins from the pituitary gland and also stimulate the synthesis of these hormones