Ichihara K, Kamei H, Okumura K, Mizukoshi K, Nagasaka M
New Drug Research Laboratories, Maruko Seiyaku Co., Ltd., Kasugai, Japan.
Methods Find Exp Clin Pharmacol. 1998 Sep;20(7):561-6. doi: 10.1358/mf.1998.20.7.485719.
BAM-1120, an ergoline derivative, has been found to display a relatively high affinity for dopamine D2-like receptor subtypes in a preliminary binding study. This study investigated whether BAM-1120 acts as a dopamine receptor agonist on prolactin-secreting and motor functions. BAM-1120 suppressed hyperprolactinemia induced by pretreatment with reserpine or estradiol in female rats. Furthermore, BAM-1120 was able to shrink a prolactin-secreting pituitary tumor (prolactinoma) in the estradiol-treated female rats. BAM-1120 induced rotations contralateral to the lesion side in rats with unilateral 6-hydroxydopamine-induced lesions of nigrostriatal dopamine pathway at a dose that was at least 30-fold higher than that required for the inhibition of prolactin secretion. These findings suggest that BAM-1120 is characterized as a putative dopamine D2-like receptor agonist that possesses a preference of inhibiting prolactin secretion over activating motor behaviors.
BAM - 1120是一种麦角灵衍生物，在初步结合研究中发现它对多巴胺D2样受体亚型表现出相对较高的亲和力。本研究调查了BAM - 1120是否作为多巴胺受体激动剂作用于催乳素分泌和运动功能。BAM - 1120抑制了雌性大鼠中由利血平或雌二醇预处理诱导的高催乳素血症。此外，BAM - 1120能够使经雌二醇处理的雌性大鼠中分泌催乳素的垂体肿瘤（催乳素瘤）缩小。在单侧6 - 羟基多巴胺诱导黑质纹状体多巴胺通路损伤的大鼠中，BAM - 1120诱导与损伤侧相反方向的旋转，其剂量比抑制催乳素分泌所需剂量至少高30倍。这些发现表明，BAM - 1120被表征为一种假定的多巴胺D2样受体激动剂，它在抑制催乳素分泌方面比激活运动行为更具偏好性。
