Demeneix B A, Desaulles E, Feltz P, Loeffler J P
Br J Pharmacol. 1984 May;82(1):183-90. doi: 10.1111/j.1476-5381.1984.tb16457.x.
We have studied the effects of selective GABAA and GABAB agonists on alpha-melanophore stimulating hormone (alpha MSH) release from intact rat neurointermediate lobes (NIL) in vitro. Agonist effects were tested against either basal alpha MSH output or BaCl2 (5 mM)-evoked release. GABA (50 microM) produced a biphasic effect on basal release, with an enhancement followed by inhibition of release. The enhancement but not the inhibition was blocked by bicuculline methiodide (100 microM). Baclofen (10 microM), a specific GABAB agonist, reduced the basal and Ba2+-evoked hormonal release in a stereospecific manner. (-)-Baclofen (5 microM) was active whereas the (+)-isomer was inactive at the same concentration. Isoguvacine (50 microM) a specific GABAA agonist, potentiated the Ba2+-evoked release of alpha MSH. GABA (50 microM) mimicked this effect, and its action was antagonized by bicuculline methiodide (200 microM). The results suggest that both GABAA and GABAB receptors are present on the endocrine cells of the intermediate lobe.
我们研究了选择性GABAA和GABAB激动剂对体外完整大鼠神经中间叶(NIL)中α-黑素细胞刺激激素(αMSH)释放的影响。针对基础αMSH输出或BaCl2(5 mM)诱发的释放测试激动剂作用。GABA(50 μM)对基础释放产生双相作用,先是增强释放,随后抑制释放。增强作用而非抑制作用被甲硫酸荷包牡丹碱(100 μM)阻断。巴氯芬(10 μM),一种特异性GABAB激动剂,以立体特异性方式降低基础和Ba2 +诱发的激素释放。(-)-巴氯芬(5 μM)有活性,而(+)-异构体在相同浓度下无活性。异谷氨酰胺(50 μM),一种特异性GABAA激动剂,增强Ba2 +诱发的αMSH释放。GABA(50 μM)模拟了这种作用,其作用被甲硫酸荷包牡丹碱(200 μM)拮抗。结果表明,GABAA和GABAB受体均存在于中间叶的内分泌细胞上。