Park Sun Young, Shin Chang Yell, Song Hyun Ju, Min Young Sil, La Hyen O, Lee Jun Woo, Kim Do Young, Je Hyun Dong, Sohn Uy Dong
Department of Pharmacology, College of Pharmacy, Chung Ang University, Seoul 156-756, Korea.
Arch Pharm Res. 2006 May;29(5):400-4. doi: 10.1007/BF02968590.
This study examined the effect of Gamma-Amino butyric acid (GABA) and selective GABA receptor related drugs on the electrically stimulated relaxation in the lower esophageal sphincter muscle (LES) of a cat. Tetrodotoxin (10(-6) M) suppressed the electrically stimulated (0.5-5 Hz) relaxation of the LES. However, guanethidine (10(-6) M) and atropine (10(-6) M) had no effect indicating that the relaxations were neurally mediated via the nonadrenergic and noncholinergic (NANC) pathways. NG-nitro-L-arginine methyl ester (10(-4) M, L-NAME) also inhibited the relaxant response but did not completely abolish the electrically stimulated relaxation with 60 % inhibition, which suggests the involvement of nitric oxide as an inhibitory transmitter. This study examined the role of GABA, an inhibitory neurotransmitter, on neurally mediated LES relaxation. GABA (10(-3)-10(-5) M, non selective receptor agonist), muscimol (10(-3)-10(-5) M, GABA-A agonist), and baclofen (10(-3)-10(-5) M, GABA-B agonist) had no significant effect on the electrically stimulated relaxation. Moreover, bicuculline (10(-5) M, GABA-A antagonist) and phaclofen (10(-5) M, GABA-B antagonist) had no inhibitory effect on the electrically stimulated relaxation. This suggests that GABA and the GABA receptor are not involved in the electrically stimulated NANC relaxation in the cat LES.
本研究检测了γ-氨基丁酸(GABA)及选择性GABA受体相关药物对猫食管下括约肌(LES)电刺激舒张的影响。河豚毒素(10⁻⁶ M)抑制了LES的电刺激(0.5 - 5 Hz)舒张。然而,胍乙啶(10⁻⁶ M)和阿托品(10⁻⁶ M)无此作用,这表明该舒张是通过非肾上腺素能和非胆碱能(NANC)途径经神经介导的。N⁰-硝基-L-精氨酸甲酯(10⁻⁴ M,L-NAME)也抑制了舒张反应,但未完全消除电刺激舒张,抑制率为60%,这提示一氧化氮作为一种抑制性递质参与其中。本研究检测了抑制性神经递质GABA在神经介导的LES舒张中的作用。GABA(10⁻³ - 10⁻⁵ M,非选择性受体激动剂)、蝇蕈醇(10⁻³ - 10⁻⁵ M,GABA-A激动剂)和巴氯芬(10⁻³ - 10⁻⁵ M,GABA-B激动剂)对电刺激舒张无显著影响。此外,荷包牡丹碱(10⁻⁵ M,GABA-A拮抗剂)和法氯芬(10⁻⁵ M,GABA-B拮抗剂)对电刺激舒张无抑制作用。这表明GABA和GABA受体不参与猫LES的电刺激NANC舒张。