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1. (WO1991009055) ACYLATED BRADYKININ ANTAGONISTS AND USES THEREFOR
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CLAIMS

1. An acylated bradykinin analog which is a
peptide having an N-terminus acyl group
represented by the formula:



X-C-,
wherein X is an organic substituent having at least one carbon atom.

An acylated bradykinin analog of Claim 1 which is a modified acylated bradykinin analog which differs from the acylated bradykinin analog by at least one amino acid.

3. An acylated bradykinin analog of Claim 2
selected from the group consisting of:


X-C Arg-Pro-Hyp-Gly-Thi-Ser-DPhe-Thi-Arg,



X-C-D-Arg-Arg-Hyp-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg,
I
X-C-Lys-Lys-Arg-Pro-Pro-Gly-Thi-Ser-D-Phe-Thi-Arg,



X-C-Arg-Pro-Pro-Gly-Thi-Ser-DPhe-Thi-Arg and



X-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg.



4. A bradykinin analog of Claim 1 wherein X-C- is selected from the group consisting of:



CH3-C-, CH3-CH2-C- and CH2-C-.


5. An acylated bradykinin analog having the
formula:



X-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi- Arg,

wherein X is an organic substituent having at
least one carbon atom.

6. An acylated bradykinin analog of Claim 5
wherein X is an organic substituent selected
from the group consisting of: saturated cyclic compounds, unsaturated cyclic compounds, cyclic aromatic compounds, saturated heterocyclic
compounds, unsaturated heterocyclic compounds and aromatic heterocyclic compounds..

7. An acylated bradykin analog having the
following formula:

CH

3-CH2-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg.

An acylated bradykinin analog of Claim 7 which
is a bradykinin antagonist.

9. An acylated bradykinin analog having the
formula:


CH2 -C -D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg .

10. An acylated bradykinin analog of Claim 9 which
is a bradykinin antagonist.

11. A method of antagonizing the effects of
bradykinin in an individual, comprising
administering to the individual an acylated
bradykinin analog.

12. A method of Claim 11 wherein the acylated
bradykinin analog has the formula:



X-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg,

wherein X is an organic substituent containing
at least one carbon atoms.

13. A method of Claim 12 wherein the acylated
bradykinin analog is selected from the group
consisting of:



CH 2-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg.


and



CH3-CH2-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg

14. A method for reducing or inhibiting the vasodepressor response in an individual, comprising administering to the individual an amount
sufficient to reduce or inhibit the
vasodepressor response by an acylated
bradykinin analog having the following formula:



X-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg,

wherein X is an organic substituent containing at least one carbon atom.

15. A method of Claim 14 wherein the amount of the acylated bradykinin analog administered is from about 3 to about 15 mg per dose.

16. A method for reducing, ameliorating or
eliminating a bradykinin-mediated disorder in an individual, comprising administering to the individual an amount sufficient to reduce,
ameliorate or eliminate the symptoms of the
disorder by an acylated bradykinin analog
having the following general formula:



X-C-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg,

wherein X is an organic substituent containing at least one carbon atom.

17. A method of Claim 16 wherein the amount
administered is from about 3 to about 15 mg per dose.

18. A method of Claim 17 wherein the bradykinin- mediated disorder is selected from the group consisting of: angina, sympathetic discharge, cardiac arrythmia, diabetic neuropathy,
ischemic heart disease, burn pain, bronchial asthma, allergic rhinitis, toxic shock,
circulatory collapse, oro-facial pain,
trigeminal neuralgia, migraine and inflammatory bowel disease.