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Selectivity of agonists and antagonists at D 2 dopamine receptors compared to D 1 and S 2 receptors
Author(s) -
Seeman Philip,
Grigoriadis Dimitri E.,
Niznik Hyman B.
Publication year - 1986
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430090108
Subject(s) - bromocriptine , dopamine , chemistry , apomorphine , eticlopride , dopamine receptor , 5 ht receptor , receptor , dopamine receptor d3 , endogenous agonist , dopamine receptor d2 , agonist , endocrinology , medicine , pharmacology , serotonin , sch 23390 , dopamine receptor d1 , biochemistry , hormone , prolactin
The common dopamine agonists (dopamine, apomorphine, ADTN, and N‐propylnorapomorphine) are not selective D 1 or D 2 dopamine receptors, affecting both simultaneously. SK&F 38393 is selective for D 1 , while bromocriptine and (D 2 )D 2 LYD 2 171555 are selective for D 2 . The neuroleptic with the highest D 2 /S 2 selectivity is eticlopride with an affinity 3,200‐fold higher for the D 2 dopamine receptor compared to the S 2 serotonin receptor. Such selective neuroleptics may be clinically useful and may also help in measuring the elevated D 2 density in vivo by positron emission tomography in the brains of schizophrensis.