Davidson C, Stamford J A
Anaesthetics Unit (Neurotransmission Laboratory), London Hospital Medical College, Royal London Hospital, Whitechapel.
Br J Pharmacol. 1995 Mar;114(6):1107-9. doi: 10.1111/j.1476-5381.1995.tb13321.x.
Electrically stimulated 5-hydroxytryptamine (5-HT) release was monitored in slices of rat dorsal raphé nucleus (DRN) by fast cyclic voltammetry. Pseudo-single pulse stimulations (5 pulses at 100 Hz) were used to enable the effect of various receptor agonists to be seen without competition from endogenously released transmitter. The selective 5-HT1A receptor agonist, (+)-8-OH-DPAT (1.0 microM) decreased stimulated 5-HT release to 31 +/- 3% of controls. This decrease was inhibited by the 5-HT1A receptor antagonists, (+)-WAY-100135 (1.0 microM) and WAY-100635 (0.1 microM) but not by the 5-HT1D/B antagonist, GR127935 (0.05 microM). The selective 5-HT1B receptor agonist, CP-93129 (0.3 microM) decreased stimulated 5-HT release to 61 +/- 4% of control. This effect was antagonized by the 5-HT1B receptor antagonist, isamoltane (0.5 microM) but not by (+)-WAY-100135. The 5-HT1D agonist, sumatriptan (0.5 microM) decreased stimulated 5-HT release to 52 +/- 2% of controls. This decrease was blocked by GR-127935 but not by WAY-100635. These results suggest that 5-HT release in the rat DRN is under the control of 5-HT1A, 5-HT1B and 5-HT1D autoreceptors.
采用快速循环伏安法监测大鼠中缝背核(DRN)切片中电刺激诱导的5-羟色胺(5-HT)释放。使用伪单脉冲刺激(100Hz的5个脉冲),以便在不存在内源性释放递质竞争的情况下观察各种受体激动剂的作用。选择性5-HT1A受体激动剂(+)-8-OH-DPAT(1.0微摩尔)可使刺激诱导的5-HT释放降至对照的31±3%。5-HT1A受体拮抗剂(+)-WAY-100135(1.0微摩尔)和WAY-100635(0.1微摩尔)可抑制这种降低,但5-HT1D/B拮抗剂GR127935(0.05微摩尔)则不能。选择性5-HT1B受体激动剂CP-93129(0.3微摩尔)可使刺激诱导的5-HT释放降至对照的61±4%。5-HT1B受体拮抗剂异美坦(0.5微摩尔)可拮抗这种作用,但(+)-WAY-100135则不能。5-HT1D激动剂舒马曲坦(0.5微摩尔)可使刺激诱导的5-HT释放降至对照的52±2%。这种降低被GR-127935阻断,但未被WAY-100635阻断。这些结果表明,大鼠DRN中的5-HT释放受5-HT1A、5-HT1B和5-HT1D自身受体的控制。