The binding sites of 8-[H-3]hydroxy-2-(di-n-propylamino)tetralin ([H-3
]DPAT) were characterized in the retina of goldfish in order to evalua
te the selectivity of the ligand for serotonin(1A) (5HT(1A)) receptors
. Specificity of the binding was performed in the presence of serotone
rgic and dopaminergic agonists and antagonists. Buspirone, spiroxatrin
e and 5-methoxy-N,N-dimethyltryptamine were potent inhibitors, followe
d by propranolol, citalopram, imipramine and desipramine. Serotonin wa
s not a potent inhibitor, and its interaction with the binding sites o
f [H-3]DPAT was complex. Nomifensine displayed an important inhibition
, however, other dopamine uptake blockers, such as bupropion and GBR-1
2909, were less potent. Haloperidol was also a good inhibitor, but the
D-1 receptor agonist, SKF-38393, the D-2 receptor antagonist, sulpiri
de, and dopamine did not inhibit the binding. GppNHp inhibited the bin
ding in the micromolar range. The analysis of saturation experiments b
y isotopic dilution, using buspirone to determine nonspecific binding,
revealed two sites. The number of binding sites defined by buspirone
were higher than the ones defined by nomifensine. The specific binding
, using buspirone for definition, was reduced by the intraocular injec
tion of 6-hydroxydopamine. This investigation demonstrates that [H-3]D
PAT labels 5HT(1A) receptors in goldfish retina, but also interacts wi
th a non-5HT receptor site. These receptors seem to be localized in do
paminergic neurons.