Agonists •
WAY-100635: potent full
agonist, with 5-HT1A antagonistic component •
A-412,997: full agonist, > 100-fold selective over a panel of seventy different receptors and ion channels •
ABT-724 - developed for treatment of erectile dysfunction •
ABT-670 - better oral bioavailability than ABT-724 • FAUC 316: partial agonist, > 8600-fold selective over other dopamine receptor subtypes • FAUC 299: partial agonist • PIP3EA: partial agonist •
Flibanserin - partial agonist •
PD-168,077 - D4 selective but also binds to α1A, α2C and 5HT1A •
CP-226,269 - D4 selective but also binds to D2, D3, α2A, α2C and
5HT1A •
Ro10-5824 – partial agonist •
Roxindole – D4 selective but also D2 and D3 autoreceptor agonist, 5HT1A receptor agonist,
serotonin reuptake inhibitor) •
Apomorphine – D4 selective but also D2 and D3 agonist, α-
adrenergic and
serotonergic weak antagonist •
Nuciferine - D4 full selective but also partial D2 and D5 agonist
Antagonists • A-381393: potent, subtype selective antagonist (>2700-fold) • FAUC 213 • L-750,667 • ML-398 • S 18126 - also
σ1 affinity •
Fananserin – mixed 5-HT2A / D4 antagonist •
Buspirone, an anxiolytic •
Clozapine - atypical antipsychotic with relative D4 and 5HT2A selectivity over D2 •
Olanzapine - an atypical antipsychotic •
Pipamperone - sedative antipsychotic with relative D4 and 5HT2A selectivity over D2
Inverse agonists • FAUC F41:
inverse agonist, subtype selectivity of more than 3 orders of magnitude over D2 and D3 == In popular culture ==