Catecholamine receptors and cyclic AMP formation in the central nervous system: effects of tetrahydroisoquinoline derivatives. |
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Authors: | Y Nimitkitpaisan P Skolnick |
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Institution: | Laboratory of Biopsychosocial Research National Institute of Alcohol Abuse and Alcoholism, ADAMHA 12501 Washington Avenue Rockville, Maryland, 20852, USA |
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Abstract: | The ability of a series of tetrahydroisoquinoline (THIQ) alkaloids to inhibit the binding of radioligands to catecholamine receptors in the CNS has been examined. THP was the most potent inhibitor of 3H] dihydroalprenolol binding to β-adrenergic receptors and of 3H] haloperidol to dopaminergic receptors and was the least potent inhibitor of 3H] WB-4101 binding to α-adrenergic receptors. Other THIQ alkaloids examined such as salsoline, salsolinol, and reticuline were less potent than THP in inhibiting radioligand binding to β-adrenergic and dopaminergic receptors, and more potent than THP in inhibiting radioligand to α-adrenergic receptors. The marked potency of THP in inhibiting radioligand binding to β-adrenergic receptors (IC50 ~ 10?7 M) was confirmed by the potency of this compound in inhibiting (?) isoproternol elicited accumulations of cyclic AMP in brain slice preparations. These data indicate that, if formed during alcohol consumption, THIQ derivatives such as THP may affect catecholamine neurons in the CNS. |
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