Abstract
1,2,3,4-Tetrahydropyrazino[1,2-a]indoles are described as a novel class of I(2) imidazoline receptor ligands. In particular, 8-methoxy-1,2,3,4-tetrahydropyrazino[1,2-a]indole (8-OMe THPI; 3c) binds with high affinity at I(2) imidazoline receptors (K(i)=6.2 nM) and with exceptional (> or =1000-fold) selectivity relative to its affinity for I(1) imidazoline receptors, alpha(2)adrenergic receptors, and 5-HT(2A) and 5-HT(2C) serotonin receptors.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Binding, Competitive
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Carbolines / metabolism
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Imidazoline Receptors
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Indoles / chemistry
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Indoles / metabolism*
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Ligands
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Molecular Structure
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Pyrazines / chemistry
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Pyrazines / metabolism*
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Receptor, Serotonin, 5-HT2A / metabolism
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Receptor, Serotonin, 5-HT2C / metabolism
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Receptors, Adrenergic, alpha-2 / metabolism
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Receptors, Drug / metabolism*
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Structure-Activity Relationship
Substances
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1,2,3,4-Tetrahydropyrazino(1,2-a)indole
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8-methoxy-1,2,3,4-tetrahydropyrazino(1,2-a)indole
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Carbolines
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Imidazoline Receptors
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Indoles
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Ligands
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Pyrazines
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Receptor, Serotonin, 5-HT2A
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Receptor, Serotonin, 5-HT2C
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Receptors, Adrenergic, alpha-2
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Receptors, Drug