Millan M J, Audinot V, Rivet J M, Gobert A, Vian J, Prost J F, Spedding M, Peglion J L
Psychopharmacology Department, Centre de Recherches de Croissy, Crossy-sur-Seine, France.
Eur J Pharmacol. 1994 Aug 1;260(2-3):R3-5. doi: 10.1016/0014-2999(94)90353-0.
The selective dopamine D3 receptor agonist, 7-OH-DPAT ((+)-7-hydroxy-2-(di-n-propylamino)tetralin) and the novel naphthofurane, S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro- naphtho(2,3b)dihydro,2,3-furane]), bound with high affinity and selectivity to recombinant, human dopamine D3 versus D2 receptors stably transfected into Chinese hamster ovary cells: Ki values = 2 versus 103 nM for 7-OH-DPAT and 13 versus 297 nM for S 14297. In contrast, the putative dopamine D3 receptor antagonist, AJ 76 (cis-(+)-5-methoxy-1-methyl-2-(n- propylamino)tetralin), displayed low affinity and selectivity for dopamine D3 versus D2 sites (70 versus 154 nM). 7-OH-DPAT (0.01-0.16 mg/kg s.c.) provoked hypothermia in rats, an action abolished by S 14297 (0.04-0.63 mg/kg s.c.) and, less potently, by AJ 76 (0.16-2.5 mg/kg s.c.). S 14297 (20.0 mg/kg s.c.) did not modify prolactin secretion. These data suggest that dopamine D3 receptors mediate hypothermia in the rat and that S 14297 acts as a selective antagonist at these sites.
选择性多巴胺D3受体激动剂7-OH-DPAT（（+）-7-羟基-2-（二正丙基氨基）四氢萘）和新型萘并呋喃S 14297（（+）-[7-（N，N-二丙基氨基）-5,6,7,8-四氢萘并（2,3b）二氢呋喃]），对稳定转染到中国仓鼠卵巢细胞中的重组人多巴胺D3受体与D2受体具有高亲和力和选择性：7-OH-DPAT的Ki值为2对103 nM，S 14297的Ki值为13对297 nM。相比之下，假定的多巴胺D3受体拮抗剂AJ 76（顺式-（+）-5-甲氧基-1-甲基-2-（正丙基氨基）四氢萘）对多巴胺D3与D2位点显示出低亲和力和选择性（70对154 nM）。7-OH-DPAT（0.01-0.16 mg/kg皮下注射）可引起大鼠体温过低，S 14297（0.04-0.63 mg/kg皮下注射）可消除该作用，AJ 76（0.16-2.5 mg/kg皮下注射）的作用较弱。S 14297（20.0 mg/kg皮下注射）不改变催乳素分泌。这些数据表明多巴胺D3受体介导大鼠体温过低，并且S 14297在这些位点起选择性拮抗剂的作用。
