Dopamine receptor blockade and the neuroleptics, a crystallographic study
AS Horn, ML Post, O Kennard - Journal of Pharmacy and …, 1975 - Wiley Online Library
AS Horn, ML Post, O Kennard
Journal of Pharmacy and Pharmacology, 1975•Wiley Online LibraryThe X‐ray structures of 12 drugs of the tricyclic class having varying pharmacological
profiles have been examined in detail in an attempt to rationalize the known structure‐
activity relations of neuroleptic drugs with respect to their ability to block dopamine receptors
in the brain. Further evidence is presented in support of the theory that the neuroleptics are
able to block dopamine receptors because of a conformational complementarity between
certain portions of these drugs and dopamine.
profiles have been examined in detail in an attempt to rationalize the known structure‐
activity relations of neuroleptic drugs with respect to their ability to block dopamine receptors
in the brain. Further evidence is presented in support of the theory that the neuroleptics are
able to block dopamine receptors because of a conformational complementarity between
certain portions of these drugs and dopamine.
The X‐ray structures of 12 drugs of the tricyclic class having varying pharmacological profiles have been examined in detail in an attempt to rationalize the known structure‐activity relations of neuroleptic drugs with respect to their ability to block dopamine receptors in the brain. Further evidence is presented in support of the theory that the neuroleptics are able to block dopamine receptors because of a conformational complementarity between certain portions of these drugs and dopamine.
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