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体外介导蟑螂唾液腺腺泡细胞超极化的多巴胺受体的特性研究

Characterization of the dopamine receptor mediating the hyperpolarization of cockroach salivary gland acinar cells in vitro.

作者信息

Evans A M, Green K L

机构信息

Department of Pharmacology, University of Edinburgh.

出版信息

Br J Pharmacol. 1990 Sep;101(1):103-8. doi: 10.1111/j.1476-5381.1990.tb12097.x.

Abstract
  1. Intracellular recordings have been made of the hyperpolarization of cockroach salivary gland cells induced by nerve stimulation and dopamine. 2. The relative potency of a number of dopamine antagonists in inhibiting the dopamine- and nerve-mediated hyperpolarization was studied. SCH23390 (10-50 microM), chlorpromazine (0.1-5 microM), haloperidol (10-100 microM) and metoclopramide (1 mM) inhibited the hyperpolarization. 3. In contrast, domperidone and (+/-)-sulpiride potentiated the hyperpolarization induced by both nerve stimulation and dopamine. 4. Apparent dissociation constants (KDapp) were obtained for the blockade of the dopamine-induced hyperpolarization. The rank order of potency (KDapp in parentheses) was as follows: chlorpromazine (0.2 microM); haloperidol (3.3 microM); SCH23390 (4.1 microM); metoclopramide (265 microM); domperidone and (+/-)-sulpiride (inactive). 5. It is concluded that the receptor subserving the dopamine-induced hyperpolarization of the salivary gland acinar cells is the same as that mediating the secretory response to dopamine. In addition these data support our findings, which suggested that this receptor is similar to the D1 dopamine receptor, but distinct from the D2 receptor found in mammalian systems.
摘要
  1. 已对神经刺激和多巴胺诱导的蟑螂唾液腺细胞超极化进行了细胞内记录。2. 研究了多种多巴胺拮抗剂抑制多巴胺和神经介导的超极化的相对效力。SCH23390(10 - 50微摩尔)、氯丙嗪(0.1 - 5微摩尔)、氟哌啶醇(10 - 100微摩尔)和甲氧氯普胺(1毫摩尔)抑制了超极化。3. 相比之下,多潘立酮和(±)-舒必利增强了神经刺激和多巴胺诱导的超极化。4. 获得了多巴胺诱导的超极化阻断的表观解离常数(KDapp)。效力顺序(括号内为KDapp)如下:氯丙嗪(0.2微摩尔);氟哌啶醇(3.3微摩尔);SCH23390(4.1微摩尔);甲氧氯普胺(265微摩尔);多潘立酮和(±)-舒必利(无活性)。5. 得出的结论是,介导唾液腺腺泡细胞多巴胺诱导的超极化的受体与介导对多巴胺分泌反应的受体相同。此外,这些数据支持了我们的发现,即该受体类似于D1多巴胺受体,但与在哺乳动物系统中发现的D2受体不同。

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