Valchár M, Vrsecká M, Krejcí I, Dlabac A
Eur J Pharmacol. 1987 Apr 7;136(1):97-101. doi: 10.1016/0014-2999(87)90784-9.
The binding properties of [3H]terguride were studied in various regions of the rat brain. The highest density of [3H]terguride binding sites was found in the striatum and tuberculum olfactorium. In the striatum, the binding was saturable, stereoselective and of a high affinity. There was a good correlation between the inhibition of [3H]terguride and [3H]spiperone bindings by various dopaminergic agents. Drugs with affinity to another type of receptors did not displace [3H]terguride binding in the striatum; only SCH 23390 was effective. The experiments indicate a certain affinity of the ligand to D-1 receptors. Nevertheless, [3H]terguride appears to have an affinity to D-2 receptors in the striatum and, thanks to its dopamine agonistic/antagonistic profile, would be useful in the further study of dopamine receptors.
研究了[3H]泰必利在大鼠脑不同区域的结合特性。在纹状体和嗅结节中发现[3H]泰必利结合位点密度最高。在纹状体中，结合具有饱和性、立体选择性且亲和力高。各种多巴胺能药物对[3H]泰必利和[3H]螺哌隆结合的抑制之间存在良好的相关性。对另一类受体有亲和力的药物不会取代纹状体中[3H]泰必利的结合；只有SCH 23390有效。实验表明该配体对D-1受体有一定亲和力。然而，[3H]泰必利似乎对纹状体中的D-2受体也有亲和力，并且由于其多巴胺激动/拮抗特性，将有助于多巴胺受体的进一步研究。
