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α2-肾上腺素能受体激动剂UK-14,304对大鼠胃底非肾上腺素能非胆碱能抑制性神经传递的调节作用

Modulation of non-adrenergic non-cholinergic inhibitory neurotransmission in rat gastric fundus by the alpha 2-adrenoceptor agonist, UK-14,304.

作者信息

Lefebvre R A, Smits G J

机构信息

Heymans Institute of Pharmacology, University of Gent Medical School, Belgium.

出版信息

Br J Pharmacol. 1992 Sep;107(1):256-61. doi: 10.1111/j.1476-5381.1992.tb14495.x.

DOI:10.1111/j.1476-5381.1992.tb14495.x
PMID:1358387
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1907632/
Abstract
  1. The influence of the alpha 2-adrenoceptor agonist, UK-14,304, on non-adrenergic non-cholinergic (NANC) relaxation induced by electrical field stimulation was investigated in longitudinal muscle strips of the gastric fundus of reserpinized rats. 2. In tissues where tone was raised by 3 x 10(-7) M prostaglandin F2 alpha (PGF2 alpha), the inhibitory effect of 10(-6) M UK-14,304, on the NANC relaxations induced by short train stimulation (40 V, 1 ms, 20 s) was inversely related to the stimulus frequency (1-4-16 Hz). UK-14,304 (10(-6) M) did not influence relaxations induced by administration of exogenous nitric oxide (NO, 2 x 10(-6) M-10(-4) M). The inhibitory effect of UK-14,304 on the electrically induced relaxations was antagonized by 10(-6) M rauwolscine but not by 10(-6) M prazosin. 3. UK-14,304 (10(-6) M) also reduced the amplitude of the sustained NANC relaxation, induced by electrical field stimulation (40 V, 1 ms, 4 Hz) for 5 min. The effect of UK-14,304 was also antagonized by 10(-6) M rauwolscine but not by 10(-6) M prazosin. UK-14,304 (10(-6) M) did not reduce the relaxation induced by 3 x 10(-9) M vasoactive intestinal polypeptide (VIP). 4. These results suggest that the release of the inhibitory NANC neurotransmitter during short train stimulation, thought to be NO, and during sustained stimulation, thought to be VIP, is inhibited by stimulation of presynaptic alpha 2-adrenoceptors in the rat gastric fundus.
摘要
  1. 研究了α2 -肾上腺素能受体激动剂UK - 14,304对利血平化大鼠胃底纵行肌条电场刺激诱导的非肾上腺素能非胆碱能(NANC)舒张的影响。2. 在由3×10(-7)M前列腺素F2α(PGF2α)升高张力的组织中,10(-6)M UK - 14,304对短串刺激(40 V,1 ms,20 s)诱导的NANC舒张的抑制作用与刺激频率(1 - 4 - 16 Hz)呈负相关。UK - 14,304(10(-6)M)不影响外源性一氧化氮(NO,2×10(-6)M - 10(-4)M)给药诱导的舒张。UK - 14,304对电诱导舒张的抑制作用被10(-6)M萝芙辛拮抗,但不被10(-6)M哌唑嗪拮抗。3. UK - 14,304(10(-6)M)也降低了电场刺激(40 V,1 ms,4 Hz)5分钟诱导的持续性NANC舒张的幅度。UK - 14,304的作用也被10(-6)M萝芙辛拮抗,但不被10(-6)M哌唑嗪拮抗。UK - 14,304(10(-6)M)不降低3×10(-9)M血管活性肠肽(VIP)诱导的舒张。4. 这些结果表明,在大鼠胃底,短串刺激期间(认为释放的抑制性NANC神经递质是NO)和持续性刺激期间(认为释放的抑制性NANC神经递质是VIP),突触前α2 -肾上腺素能受体的刺激会抑制抑制性NANC神经递质的释放。

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Inhibition of the excitatory non-adrenergic, non-cholinergic neurotransmission in the guinea pig tracheo-bronchial tree mediated by alpha 2-adrenoceptors.α2肾上腺素能受体介导的豚鼠气管支气管树兴奋性非肾上腺素能、非胆碱能神经传递的抑制作用。
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