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首页> 外文期刊>Life sciences >Effects of arginine vasopressin and oxytocin on glucagon release from clonal alpha-cell line In-R1-G9: involvement of V1b receptors.
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Effects of arginine vasopressin and oxytocin on glucagon release from clonal alpha-cell line In-R1-G9: involvement of V1b receptors.

机译：精氨酸升压素和催产素对胰高血糖素从克隆α-细胞系In-R1-G9释放的影响：V1b受体的参与。

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摘要

Receptor antagonists were used to determine which receptor mediates the effect of arginine vasopressin (AVP) and oxytocin (OT) on glucagon release from hamster glucagonoma In-R1-G9 cells. Both AVP (10(-9)-10(-6) M) and OT (10(-8)-10(-5) M) increased glucagon release from In-R1-G9 cells in a concentration-dependent manner and AVP was approximately 30-fold more potent than OT in this aspect. The antagonists with potent V1b receptor blocking activity, CL-4-84 (10(-9)-10(-6) M), dP[Tyr(Me)2]AVP and AO-2-44 (10(-8)-10(-6) M), antagonized the effect of both AVP and OT in a concentration-dependent manner. Other receptor antagonists at 10(-6) M failed to block the effect of AVP and OT; these included a highly selective OT-receptor antagonist, L-366,948 and a V1a/V2 receptor antagonist WK-3-6. However, these antagonists at higher concentrations (10(-5) and 10(-4) M) caused inhibition of AVP- and OT-induced glucagon release. The order of antagonistic potency was estimated as CL-4-84 approximately = dP[Tyr(Me)2]AVP approximately = AO-2-44 > WK 3-6 > L366,948. d[D-3-Pal]VP (10(-8)-10(-5) M), a V1b receptor agonist, also increased glucagon release in a concentration-dependent manner, which was antagonized by dP[Tyr(Me)2]AVP (10(-8)-10(-6) M) and CL-4-84 (10(-9)-10(-6) M), but not by WK-3-6 (10(-6) M) or L-366,948 (10(-6) M). Therefore, the stimulatory effects of both OT and AVP on glucagon release may be mediated by V1b receptors, but not by V1a, V2, or OT receptors.
机译：使用受体拮抗剂来确定哪种受体介导精氨酸加压素（AVP）和催产素（OT）对仓鼠胰高血糖素瘤In-R1-G9细胞释放胰高血糖素的作用。 AVP（10（-9）-10（-6）M）和OT（10（-8）-10（-5）M）均以浓度依赖的方式和AVP增加In-R1-G9细胞的胰高血糖素释放在这方面，其效力比OT高约30倍。具有强大的V1b受体阻断活性的拮抗剂，CL-4-84（10（-9）-10（-6）M），dP [Tyr（Me）2] AVP和AO-2-44（10（-8） -10（-6）M），以浓度依赖性方式拮抗AVP和OT的作用。其他在10（-6）M的受体拮抗剂未能阻断AVP和OT的作用。其中包括高度选择性的OT受体拮抗剂L-366,948和V1a / V2受体拮抗剂WK-3-6。但是，这些拮抗剂在较高浓度（10（-5）和10（-4）M）下会抑制AVP和OT诱导的胰高血糖素释放。拮抗效力的顺序估计为CL-4-84大约= dP [Tyr（Me）2] AVP大约= AO-2-44> WK 3-6> L366,948。 d [D-3-Pal] VP（10（-8）-10（-5）M），一种V1b受体激动剂，也以浓度依赖的方式增加了胰高血糖素的释放，这被dP [Tyr（Me）拮抗2] AVP（10（-8）-10（-6）M）和CL-4-84（10（-9）-10（-6）M），但不是WK-3-6（10（- 6）M）或L-366,948（10（-6）M）。因此，OT和AVP对胰高血糖素释放的刺激作用可能是由V1b受体介导的，而不是由V1a，V2或OT受体介导的。

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