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Details for Patent: 5,990,128

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Details for Patent: 5,990,128

Title: .alpha..sub.1C specific compounds to treat benign prostatic hyperplasia
Abstract:This invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of an .alpha..sub.1C antagonist which (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 .alpha..sub.1C antagonist 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 .alpha..sub.1C antagonist binds to such .alpha..sub.1C adrenergic receptor. The invention further provides a method of inhibiting contraction of a prostate tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of an .alpha..sub.1C antagonist which (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 .alpha..sub.1C antagonist 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 .alpha..sub.1C antagonist binds to such .alpha..sub.1C adrenergic receptor.
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. (Pennington, NJ)
Assignee: Synaptic Pharmaceutical Corporation (Paramus, NJ)
Filing Date:Nov 22, 1996
Application Number:08/722,190
Claims:1. A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of an antagonist which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 691-fold higher than the binding affinity with which the antagonist binds to a human .alpha..sub.1B adrenergic receptor.

2. A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of an antagonist which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 1089-fold higher than the binding affinity with which the antagonist binds to a human .alpha..sub.1A adrenergic receptor.

3. The method of claim 1, wherein the binding affinity of the antagonist is at least 91-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.1A adrenergic receptor.

4. The method of claim 2, wherein the binding affinity of the antagonist is at least 28-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for any human .alpha..sub.2 adrenergic receptor.

5. The method of claim 1, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is (I) at least 91-fold higher than it is for the human .alpha..sub.1A adrenergic receptor, (ii) at least 65-fold higher than it is for the human histamine H.sub.1 receptor, and (iii) at least 229-fold higher than it is for the human .alpha..sub.2 adrenergic receptor.

6. The method of claim 1, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is at least 41-fold higher than it is for any calcium channel.

7. The method of claim 1, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is at least 234-fold higher than it is for a human histamine H.sub.2 receptor.

8. The method of claim 1, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is at least 30-fold higher than it is for a human serotonin receptor.

9. The method of claim 1 or 2, wherein the antagonist does not cause an orthostatis fall in blood pressure.

10. The method of claim 9, wherein the antagonist additionally does not cause an orthostatic fall in blood pressure in rats at a dosage of 10 micrograms of antagonist per kilogram of rat.

11. A method of inhibiting contraction of prostatic tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of an antagonist which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 691-fold higher than the binding affinity with which the antagonist binds to a human .alpha..sub.1B adrenergic receptor.

12. A method of inhibiting contraction of prostatic tissue which comprises contacting the prostate tissue with an effective contraction-inhibiting amount of an antagonist which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 1089-fold higher than the binding affinity with which the antagonist binds to a human .alpha..sub.1A adrenergic receptor.

13. The method of claim 11, wherein the binding affinity of the antagonist is at least 91-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for any human .alpha..sub.1A adrenergic receptor.

14. The method of claim 12, wherein the binding affinity of the antagonist is at least 28-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.2 adrenergic receptor.

15. The method of claim 11, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is (I) at least 91-fold higher than it is for the human .alpha..sub.1A adreriergic receptor, (ii) at least 65-fold higher than it is for the human histamine H.sub.1 receptor, and (iii) at least 229-fold higher than it is for the human .alpha..sub.2 adrenergic receptor.

16. The method of claim 11, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is at least 41-fold higher than it is for any calcium channel.

17. The method of claim 11, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is at least 234-fold higher than it is for a human histamine H.sub.2 receptor.

18. The method of claim 11, wherein the binding affinity of the antagonist for the human .alpha..sub.1C adrenergic receptor is at least 30-fold higher than it is for a human serotonin receptor.

19. The method of claim 11 or 12, wherein the antagonist does not cause an orthostatic fall in blood pressure.

20. The method of claim 19, wherein the antagonist additionally does not cause an orthostatic fall in blood pressure in rats at a dosage of 10 micrograms of antagonist per kilogram of rat.
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