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Details for Patent: 5,578,611

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Details for Patent: 5,578,611

Title: Use of .alpha.-1C specific compounds to treat benign prostatic hyperplasia
Abstract:The subject invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, a human histamine H.sub.1 receptor and .alpha..sub.2 adrenergic receptor. The subject invention also provides a method of inhibiting contraction of prostate tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of such compound.
Inventor(s): Gluchowski; Charles (Wayne, NJ), Forray; Carlos C. (Paramus, NJ), Chiu; George (Bridgewater, NJ), Branchek; Theresa A. (Teaneck, NJ), Wetzel; John M. (Elmwood Park, NJ), Hartig; Paul R. (Kinnelon, NJ)
Assignee: Synaptic Pharmaceutical Corporation (Paramus, NJ)
Filing Date:Apr 13, 1994
Application Number:08/228,932
Claims:1. A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which:

a. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 20-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor; and

b. binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 20-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

2. The method of claim 1, wherein the compound (a) binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 50-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and (b) binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 50-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

3. The method of claim 2, wherein the compound (a) binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 100-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and (b) binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

4. The method of claim 3, wherein the compound (a) binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 300-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and (b) binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 300-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

5. The method of claim 1, 2, 3 or 4, wherein the compound additionally binds to a calcium channel with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

6. The method of claim 1, 2, 3 or 4, wherein the compound binds to a calcium channel with a binding affinity which is greater than 20-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

7. The method of claim 1, 2, 3 or 4, wherein the compound binds to a calcium channel with a binding affinity which is greater than 50-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

8. The method of claim 1, 2, 3 or 4, wherein the compound binds to a calcium channel with a binding affinity which is greater than 100-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

9. The method of claim 1, 2, 3 or 4, wherein the compound binds to a calcium channel with a binding affinity which is greater than 300-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

10. The method of claim 1, 2, 3 or 4, wherein the compound additionally binds to a human dopamine D.sub.2 or human H.sub.2 receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

11. The method of claim 1, 2, 3 or 4, wherein the compound binds to a human dopamine D.sub.2 or human H.sub.2 receptor with a binding affinity which is greater than 20-fold lower than the binding affinity with the compound binds to the .alpha..sub.1C adrenergic receptor.

12. The method of claim 1, 2, 3 or 4, wherein the compound binds to a human dopamine D.sub.2 or human H.sub.2 receptor with a binding affinity which is greater than 50-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

13. The method of claim 1, 2, 3 or 4, wherein the compound binds to a human dopamine D.sub.2 or human H.sub.2 receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

14. The method of claim 1, 2, 3 or 4, wherein the compound binds to a human dopamine D.sub.2 or human H.sub.2 receptor with a binding affinity which is greater than 300-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

15. The method of claim 1, 2, 3 or 4, wherein the compound additionally binds to any serotonin receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

16. The method of claim 1, 2, 3 or 4, wherein the compound binds to any serotonin receptor with a binding affinity which is greater than 20-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

17. The method of claim 1, 2, 3 or 4, wherein the compound binds to any serotonin receptor with a binding affinity which is greater than 50-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

18. The method of claim 1, 2, 3 or 4, wherein the compound binds to any serotonin receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

19. The method of claim 1, 2, 3 or 4, wherein the compound binds to any serotonin receptor with a binding affinity which is greater than 300-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

20. The method of claim 1, 2, 3 or 4, wherein the compound additionally binds to a dopamine D.sub.3, D.sub.4, or D.sub.5 receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

21. The method of claim 1, 2, 3 or 4, wherein the compound binds to a dopamine D.sub.3, D.sub.4, or D.sub.5 receptor with a binding affinity which is greater than 20-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

22. The method of claim 1, 2, 3 or 4, wherein the compound binds to a dopamine D.sub.3, D.sub.4, or D.sub.5 receptor with a binding affinity which is greater than 50-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

23. The method of claim 1, 2, 3 or 4, wherein the compound binds to a dopamine D.sub.3, D.sub.4, or D.sub.5 receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

24. The method of claim 1, 2, 3 or 4, wherein the compound binds to a dopamine D.sub.3, D.sub.4, or D.sub.5 receptor with a binding affinity which is greater than 300-fold lower than the binding affinity with which the compound binds to the .alpha..sub.1C adrenergic receptor.

25. A method of claims 1, 2, 3 or 4, wherein the compound additionally does not cause an orthostatic fall in blood pressure at dosages effective to alleviate benign prostatic hyperplasia.

26. The method of claim 25, wherein the compound additionally does not cause an orthostatic fall in blood pressure in rats at a dosage of 10 micrograms of compound per kilogram of rat.

27. The method of claim 1, wherein the compound has the structure: ##STR5##

28. The method of claim 1 or 2, wherein the compound has the structure: ##STR6##

29. The method of claim 1, wherein the compound has the structure: ##STR7##

30. The method of claim 1, wherein the compound has the structure: ##STR8##

31. A method of inhibiting contraction of prostate tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of a compound which:

a. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 20-fold higher than the binding affinity with which the compound binds to a human adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor; and

b. binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 20-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

32. The method of claim 31, wherein the compound (a) binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 50-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and (b) binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 50-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

33. The method of claim 32, wherein the compound (a) binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 100-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and (b) binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 100-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

34. The method of claim 33, wherein the compound (a) binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than 300-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and (b) binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than 300-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor.

35. A method of claim 31, wherein the compound additionally does not cause an orthostatic fall in blood pressure at dosages effective to alleviate benign prostatic hyperplasia.

36. The method of claim 35, wherein the compound additionally does not cause an orthostatic fall in blood pressure in rats at a dosage of 10 micrograms of compound per kilogram of rat.
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