✦ LIBER ✦

Selectivity of agonists and antagonists at D2dopamine receptors compared to D1 and S2receptors

✍ Scribed by Dr. Philip Seeman; Dimitri E. Grigoriadis; Hyman B. Niznik

Publisher: John Wiley and Sons
Year: 1986
Tongue: English
Weight: 332 KB
Volume: 9
Category: Article
ISSN: 0272-4391
DOI: 10.1002/ddr.430090108

No coin nor oath required. For personal study only.

✦ Synopsis

Seeman, P., D.E. Grigoriadis, and H.B. Niznik: Selectivity of agonists and antagonists at D2 dopamine receptors compared to D, and S2 receptors. Drug Dev. Res. 9:63-69,

1986.

The common dopamine agonists (dopamine, apomorphine, ADTN, and N-propylnorapomorphine) are not selective for either D, or D2 dopamine receptors, affecting both simultaneously. SK&F 38393 is selective for D,, while bromocriptine and (-)-LY-171555 are selective for D2. The neuroleptic with the highest D2/S2 selectivity is eticlopride with an affinity 3,200-fold higher for the D2 dopamine receptor compared to the S2 serotonin receptor. Such selective neuroleptics may be clinically useful and may also help in measuring the elevated D2 density in vivo by positron emission tomography in the brains of schizophrenics.

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