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- W2044025009 abstract "Several new clonidine analogs were synthesized and their ability to inhibit [ 3 H] phentolamine binding to human platelet α 2 -adrenergic receptors was tested. The order of potency and calculated dissociation constants for clonidine and its analogs were as follows: clonidine (0.020 ± 0.005 μ M) > p -aminoclonidine (0.100 ± 0.010 μ M) > hydroxy-phenacetyl-aminoclonidine (0.20 ± 0.03 μ M) > p -dansyl clonidine (1.00 ± 0.20 μ M) > t -boc-tyrosine clonidine (1.80 ± 0.60 μ M). Thus, p -amino substitution reduces α 2 -adrenergic affinity in the platelet system. The effects of clonidine and its p -amino analogs on platelet adenylate cyclase were also evaluated. This enzyme is inhibited by epinephrine acting via α 2 -adrenergic receptors. Both clonidine and p -aminoclonidine cause slight inhibition of basal adenylate cyclase and reverse the inhibition induced by epinephrine. These observations indicate that clonidine is a partial agonist for platelet α 2 -adrenergic receptors." @default.
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- W2044025009 date "1982-02-25" @default.
- W2044025009 modified "2023-09-23" @default.
- W2044025009 title "Interaction of clonidine and clonidine analogs with human platelet α2-adrenergic receptors" @default.
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- W2044025009 doi "https://doi.org/10.1016/0304-4165(82)90145-3" @default.
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