EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT1A receptor agonistic properties
EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT1A receptor agonistic properties
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DOI：
10.1016/s0014-2999(96)00999-5
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发表时间：
1997-03-19
影响因子：
5
通讯作者：
Ziegler, H
中科院分区：
文献类型：
--
作者：
Bartoszyk, GD;Hegenbart, R;Ziegler, H
5-HT1A 受体激动剂 8-羟基-(二正丙氨基)四氢萘 (8-OH-DPAT；0.55 mg/kg s.c.) 和 5-HT（5-羟色胺、血清素）再摄取抑制剂/5-HT1A 受体配体5-{4-[4-(5-氰基-3-吲哚基)-丁基]-1-哌嗪基}-苯并呋喃-2-甲酰胺（EMD 68843；55 mg/kg 口服）抑制大鼠超声发声，该作用可被 5-HT1A 受体拮抗剂拮抗N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]-乙基]-N-(2-吡啶基)-环己甲酰胺（WAY 100635；1.0 mg/kg s.c.）。 8-OH-DPAT 降低大鼠体温，这一作用也被 WAY 100635 拮抗，而 EMD 68843 本身既不影响体温，也不与 8-OH-DPAT 或 WAY 100635 相互作用。选择性 5-HT 再摄取抑制剂氟西汀（口服 100 mg/kg）对超声发声或体温没有影响。因此，EMD 68843 被认为是一种对突触前 5-HT1A 受体具有选择性的 5-HT1A 受体激动剂。 (C) 1997 Elsevier Science B.V.
The 5-HT1A receptor agonist 8-hydroxy-(di-n-propylamino)tetralin (8-OH-DPAT; 0.55 mg/kg s.c.) and the 5-HT (5-hydroxytryptamine, serotonin) reuptake inhibitor/5-HT1A receptor ligand 5-{4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl}-benzofuran-2-carboxamide (EMD 68843; 55 mg/kg p.o.) inhibited ultrasonic vocalization in rats, an effect which was antagonized by the 5-HT1A receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]-ethyl]-N-(2-pyridyl)-cyclohexancarboxamide(WAY 100635; 1.0 mg/kg s.c.). 8-OH-DPAT decreased body temperature in rats, an effect which was also antagonized by WAY 100635, whereas EMD 68843 neither affected body temperature by itself nor interacted with 8-OH-DPAT or WAY 100635. The selective 5-HT reuptake inhibitor fluoxetine (100 mg/kg p.o.) had no effect on ultrasonic vocalization or body temperature. Therefore EMD 68843 is suggested to be a 5-HT1A receptor agonist selective for presynaptic 5-HT1A receptors. (C) 1997 Elsevier Science B.V.