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溴隐亭和喹吡罗在鸡松果体中的α-2肾上腺素能活性。对褪黑素合成及[3H]萝芙辛结合的影响。

Alpha-2 adrenergic activity of bromocriptine and quinpirole in chicken pineal gland. Effects on melatonin synthesis and [3H]rauwolscine binding.

作者信息

Zawilska J, Iuvone P M

机构信息

Emory University School of Medicine, Department of Pharmacology, Atlanta, Georgia.

出版信息

J Pharmacol Exp Ther. 1990 Dec;255(3):1047-52.

PMID:1979809
Abstract

In the pineal gland and retina of chickens, serotonin N-acetyl-transferase (NAT) activity and melatonin content are modulated by different receptors, alpha-2 adrenergic receptors in pineal gland and D2-dopamine receptors in retina. The effect of two D2-dopamine receptor agonists, bromocriptine and quinpirole (LY 171555), on melatonin synthesis in these tissues was investigated. Systemic administrations of bromocriptine and quinpirole decreased nocturnal NAT activity and melatonin content of both pineal gland and retina. Bromocriptine was equipotent in the two tissues, whereas quinpirole was approximately 100-fold more potent in retina than in pineal gland. In pineal gland, the suppressive effects of bromocriptine and quinpirole on NAT activity were blocked by yohimbine, a selective alpha-2 adrenergic receptor antagonist, but not by spiperone, a D2-dopamine receptor antagonist. In contrast, bromocriptine- and quinpirole-induced decreases of the enzyme activity in retina were antagonized by spiperone, and not affected by yohimbine. The nocturnal increase of NAT activity of pineal glands in vitro was inhibited with an order of potency clonidine greater than bromocriptine greater than quinpirole. Additionally, bromocriptine and quinpirole displaced the specific binding of [3H]rauwolscine, an alpha-2 adrenergic receptor antagonist, to membranes from chicken pineal gland, with potencies comparable to those observed for inhibition of NAT activity in vitro. It is suggested that bromocriptine and quinpirole, in addition to their D2-dopaminergic activity, can stimulate alpha-2 adrenergic receptors in pineal gland of chicken.

摘要

在鸡的松果体和视网膜中,血清素N - 乙酰转移酶(NAT)活性和褪黑素含量受不同受体调节,松果体中是α - 2肾上腺素能受体,视网膜中是D2 - 多巴胺受体。研究了两种D2 - 多巴胺受体激动剂溴隐亭和喹吡罗(LY 171555)对这些组织中褪黑素合成的影响。全身性给予溴隐亭和喹吡罗可降低松果体和视网膜的夜间NAT活性及褪黑素含量。溴隐亭在这两种组织中的作用效力相同,而喹吡罗在视网膜中的效力比在松果体中约强100倍。在松果体中,溴隐亭和喹吡罗对NAT活性的抑制作用可被选择性α - 2肾上腺素能受体拮抗剂育亨宾阻断,但不能被D2 - 多巴胺受体拮抗剂螺哌隆阻断。相反,溴隐亭和喹吡罗诱导的视网膜中酶活性降低可被螺哌隆拮抗,且不受育亨宾影响。体外实验中,松果体NAT活性的夜间增加受到抑制,其效力顺序为可乐定大于溴隐亭大于喹吡罗。此外,溴隐亭和喹吡罗可取代α - 2肾上腺素能受体拮抗剂[3H]萝芙木碱与鸡松果体膜的特异性结合,其效力与体外抑制NAT活性时观察到的效力相当。提示溴隐亭和喹吡罗除具有D2 - 多巴胺能活性外,还可刺激鸡松果体中的α - 2肾上腺素能受体。

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