(6a.alpha.,10a.alpha.,11a.alpha.)-2-(2-Pyridinyl)-1,3,4,6,6a,7,8,9,10,10 a,11,11a-dodecahydro-2H-pyrazino]1,2-b]isoquinoline and derivatives
AssigneeMerck & Co., Inc.
InventorsJoel R. Huff, Stella W. King, Walfred S. Saari
Life of this patent
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Abstract
(6a.alpha.,10a.alpha.,11a.alpha.)-2-(2-pyridinyl)-1,3,4,6,6a,7,8,9,10,10a,1 1,11a-dodecahydro-2H-pyrazino[1,2-b]isoquinoline and derivatives or acid addition salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressant agents and for treating sedation caused by antihypertensive therapy.
Claims9
A method of selectively antagonizing .alpha..sub.2 -adrenergic receptors in a patient in need of such treatment which comprises the administration of an effective amount of a compound of structural formula:
- ##STR4## or a pharmaceutically acceptable salt thereof wherein R is
- (1) hydrogen,
- (2) halo,
- (3) C.sub.1-4 alkyl,
- (4) cyano,
- (5) C.sub.1-4 alkoxy,
- (6) trifluoromethyl, or
- (7) nitro.
A compound of structural formula:
- ##STR5## or a pharmaceutically acceptable salt thereof, wherein R is
- (1) hydrogen,
- (2) halo,
- (3) C.sub.1-4 alkyl,
- (4) cyano,
- (5) C.sub.1-4 alkoxy,
- (6) trifluoromethyl, or
- (7) nitro.
A selective .alpha..sub.2 -adrenergic receptor antagonist pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an effective .alpha..sub.2 -adrenergic receptor antagonist amount of a compound of structural formula:
- ##STR6## or a pharmaceutically acceptable salt thereof wherein R is
- (1) hydrogen,
- (2) halo,
- (3) C.sub.1-4 alkyl,
- (4) cyano,
- (5) C.sub.1-4 alkoxy,
- (6) trifluoromethyl, or
- (7) nitro.
Dependencies are inferred from the claim text.