Chapman R W, Hey J A, Rizzo C A, Bolser D C
Schering-Plough Research Institutes, Kennleworth, NJ 07033.
Trends Pharmacol Sci. 1993 Jan;14(1):26-9. doi: 10.1016/0165-6147(93)90110-6.
gamma-Aminobutyric acid (GABA), an important inhibitory neurotransmitter in the mammalian CNS, is also found in peripheral tissues, including the lung. Recent pharmacological studies using selective ligands for GABAA and GABAB receptors demonstrate that of these two, the GABAB receptor is the important receptor subtype controlling lung functions. GABAB agonists inhibit a variety of responses in the airways, including neuronally induced cholinergic- and tachykinin-mediated smooth muscle contraction, microvascular leakage, anaphylactic bronchospasm and cough. Because these conditions are seen in certain respiratory diseases, such as asthma, a selective GABAB agonist may have therapeutic potential for the treatment of this respiratory disorder.
γ-氨基丁酸(GABA)是哺乳动物中枢神经系统中一种重要的抑制性神经递质,在包括肺在内的外周组织中也有发现。最近使用GABAA和GABAB受体选择性配体的药理学研究表明,在这两种受体中,GABAB受体是控制肺功能的重要受体亚型。GABAB激动剂可抑制气道中的多种反应,包括神经元诱导的胆碱能和速激肽介导的平滑肌收缩、微血管渗漏、过敏性支气管痉挛和咳嗽。由于这些情况见于某些呼吸系统疾病,如哮喘,选择性GABAB激动剂可能具有治疗这种呼吸系统疾病的潜力。