Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-04-13
1996-11-26
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514654, A61K 31445, A61K 31135
Patent
active
055786111
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.
REFERENCES:
patent: 4975440 (1990-12-01), Flockerzi et al.
patent: 4994461 (1991-02-01), Ulrich
patent: 5403847 (1995-04-01), Gluchowski et al.
Lomasney, J. W., et al., "molecular Cloning and Expression of the cDNA for the Alpha.sub.1A -Adrenergic Receptor," Journal of Biological Chemistry, 266, 6365-6369 (1991).
Lepor, H., et al., "A Dose Titration Study Evaluating Terazosin, A Selective, Once-A-Day Alpha 1-Blocker for the Treatment of Symptomatic Benign Prostatic Hyperlasia," Journal of Urology, 144, 1393-1398 (1990).
Gup, D., et al., "Autonomic Receptors in Human Prostate Adenomas," Journal of Urology, 143, 179-185 (1990).
Lepor, H., et al., "The Effect of Electrocautery on Neurotransmitter Receptor Binding Assays in the Canine Prostate," Medline Abstracts, 88317114 (1988).
Lepor, H., et al., "The Alpha Adrenergic Binding Properties of Terazosin in the Human Prostate Adenoma and Canine Brain," Medline Abstracts, 88317113 (1988).
Ramarao, C. S., et al., "Genomic Organization and Expression of the Human Alpha.sub.1B -Adrenergic Receptor," J. Biol. Chem., 267, 21936-21944 (1992).
I. Marshall, et al., Abstract No. C97 of an oral presentation given during a Sep. 9-11 Meeting of the British Pharmacological Society (1992).
Archibald, J. L., et al., "Antihypertensive Ureidopiperidines," Journal of Medicinal Chemistry, 23, 857-861 (1980).
Boer, R., et al., "(+)-Niguldipine binds with very high affinity to Ca.sup.2+ channels and to a subtype of .varies.-adrenoreceptors," European Journal of Pharmacology--Molecular Pharmacology Section, 172, 131-145 (1989).
Forray, C., et al., "The .varies..sub.1 -Adrenergic Receptor that Mediates Smooth Muscle Contraction in Human Prostate Has the Pharmacological Properties of Cloned Human .varies..sub.1C Subtype," Molecular Pharmacology, 45, 703-708 (1994).
Forray, C., Chiu, G., et al., "Effects of Novel Alpha-1C Adrenergic Receptor Antagonists on the Contraction of Human Prostate Smooth Muscle", American Urological Association Eighty-ninth Annual Meeting, May 14-19, 1994, The Journal of Urology, Association Eighty-ninth Annual Meeting, May 14-19, 1994, The Journal of Urology, 151(5), Abstract #159 (May 1994).
Forray, C., Bard, J. A., et al., "Comparison of the Pharmacological Properties of the Cloned Bovine, Human, and Ray .varies..sub.1C -Adrenergic Receptors," The FASEB Journal, 8(4), Abstract #2042 (1994).
Gong, G., et al., ".varies..sub.1C -Adrenergic Antagonists and Orthostatic Hypotension in the Rat," The FASEB Journal, 8(4), Abstract #2043 (1994).
Lepor, H., et al., "Localization of Alpha.sub.1C Adrenoceptor (.varies..sub.1C AR) Subtypes in the Human Prostate," American Urological Association Eighty-ninth Annual Meeting, May 14-19, 1994, The Journal of Urology, 151(15), Abstract #614 (May 1994).
Hieble, J. P., et al., "In vitro characterization of the .varies.hd 1-adrenoreceptors in human prostate," European Journal of Pharmacology, 107, 111-117 (1985).
Perez, J. L., et al., "Is the .varies..sub.1C -Adrenergic Receptor the .varies..sub.1A -Subtype?" The FASEB Journal, 8(4), Abstract #2041 (1994).
Tang, R., et al., "Localization of Alpha 1C Adrenoceptor (.varies.1C AR) Subtypes in the Human Prostatic Tissue," The FASEB Journal, 8(5), Abstract #5070 (1994).
Wetzel, J. M., et al., "Structural and Functional Studies of the Human .varies..sub.1C Adrenergic Receptor: The Orientation of Transmembrane Helix 5," The FASEB Journal, 8(4) Abstract #2182 (1994).
Yamada, S., et al., ".varies..sub.1A -Adrenergic Receptors in Human Prostate: Characterization and Alteration in Benign Prostatic Hypertrophy," Journal of Pharmacology and Experimental Therapeutics, 242, 326-330 (1987).
Branchek Theresa A.
Chiu George
Forray Carlos C.
Gluchowski Charles
Hartig Paul R.
Cintins Marianne M.
Jarvis William R. A.
Synaptic Pharmaceutical Corporation
White John P.
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