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可卡因与妊娠子宫肌层中的β-肾上腺素能受体功能

Cocaine and beta-adrenergic receptor function in pregnant myometrium.

作者信息

Wang F L, Dombrowski M P, Hurd W W

机构信息

Department of Obstetrics and Gynecology, University of Michigan Medical Center, Ann Arbor, Michigan, USA.

出版信息

Am J Obstet Gynecol. 1996 Dec;175(6):1651-3. doi: 10.1016/s0002-9378(96)70120-5.

DOI:10.1016/s0002-9378(96)70120-5
PMID:8987955
Abstract

OBJECTIVE

Our purpose was to evaluate the in vitro effect of cocaine on beta-adrenergic receptor function in pregnant human myometrium.

STUDY DESIGN

Myometrium was obtained from 25 pregnant women at term who were undergoing cesarean section but who were not in labor. Membrane preparations were assayed for cyclic adenosine monophosphate production after exposure to isoproterenol, sodium fluoride, or forskolin in the presence and absence of either cocaine or benzoylecgonine, a major metabolite of cocaine.

RESULTS

Cocaine inhibited isoproterenol-induced cyclic adenosine monophosphate production in concentrations as low as 10(-8) mol/L but had no effect on cyclic adenosine monophosphate production induced by sodium fluoride or forskolin. Benzoylecgonine (10(-4) mol/L) had no effect on isoproterenol-induced cyclic adenosine monophosphate production.

CONCLUSION

Cocaine is a beta-adrenergic receptor antagonist in human myometrium at concentrations as low as 10(-8) mol/L. This acute effect of cocaine may result in increased uterine contractility with adrenergic stimulation, potentially leading to increased uterine activity associated with acute cocaine use.

摘要

目的

我们的目的是评估可卡因对妊娠人类子宫肌层β-肾上腺素能受体功能的体外作用。

研究设计

从25名足月行剖宫产但未临产的孕妇获取子宫肌层。在存在和不存在可卡因或苯甲酰爱康宁(可卡因的主要代谢产物)的情况下,将膜制剂暴露于异丙肾上腺素、氟化钠或福斯高林后,检测环磷酸腺苷的产生。

结果

可卡因在低至10^(-8)摩尔/升的浓度下即可抑制异丙肾上腺素诱导的环磷酸腺苷产生,但对氟化钠或福斯高林诱导的环磷酸腺苷产生无影响。苯甲酰爱康宁(10^(-4)摩尔/升)对异丙肾上腺素诱导的环磷酸腺苷产生无影响。

结论

可卡因在低至10^(-8)摩尔/升的浓度下是人类子宫肌层中的β-肾上腺素能受体拮抗剂。可卡因的这种急性作用可能导致肾上腺素能刺激时子宫收缩性增加,潜在地导致与急性可卡因使用相关的子宫活动增加。

相似文献

1
Cocaine and beta-adrenergic receptor function in pregnant myometrium.可卡因与妊娠子宫肌层中的β-肾上腺素能受体功能
Am J Obstet Gynecol. 1996 Dec;175(6):1651-3. doi: 10.1016/s0002-9378(96)70120-5.
2
Cocaine selectively inhibits beta-adrenergic receptor binding in pregnant human myometrium.可卡因选择性抑制妊娠子宫肌层中的β-肾上腺素能受体结合。
Am J Obstet Gynecol. 1993 Sep;169(3):644-9. doi: 10.1016/0002-9378(93)90637-x.
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Cocaine downregulates beta-adrenergic receptors in pregnant sheep myometrium.可卡因会下调怀孕绵羊子宫肌层中的β-肾上腺素能受体。
Reprod Toxicol. 1996 Mar-Apr;10(2):119-23. doi: 10.1016/0890-6238(95)02053-5.
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Decrease in myometrial beta-adrenergic receptors with prenatal cocaine use.产前使用可卡因导致子宫肌层β-肾上腺素能受体减少。
Obstet Gynecol. 1995 Mar;85(3):357-60. doi: 10.1016/0029-7844(94)00424-C.
5
Cocaine augments contractility of the pregnant human uterus by both adrenergic and nonadrenergic mechanisms.可卡因通过肾上腺素能和非肾上腺素能机制增强妊娠人类子宫的收缩力。
Am J Obstet Gynecol. 1998 May;178(5):1077-81. doi: 10.1016/s0002-9378(98)70551-4.
6
A re-evaluated role for cyclic AMP in uterine relaxation. Differential effect of isoproterenol and forskolin.
J Pharmacol Exp Ther. 1986 Oct;239(1):236-42.
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Failure to demonstrate decreased beta-adrenergic receptor concentration or decreased agonist efficacy in term or preterm human parturition.在足月或早产的人类分娩中,未能证实β-肾上腺素能受体浓度降低或激动剂效力降低。
Am J Obstet Gynecol. 1986 Feb;154(2):450-6. doi: 10.1016/0002-9378(86)90689-7.
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Forskolin: unique diterpene activator of adenylate cyclase in pregnant and nonpregnant guinea pig myometrial membranes.福司可林:怀孕和未怀孕豚鼠子宫肌层膜中腺苷酸环化酶的独特二萜激活剂。
Am J Obstet Gynecol. 1986 Dec;155(6):1202-8. doi: 10.1016/0002-9378(86)90145-6.
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Estrogen reduces beta-adrenoceptor-mediated cAMP production and the concentration of the guanyl nucleotide-regulatory protein, Gs, in rabbit myometrium.雌激素可降低兔子宫肌层中β-肾上腺素能受体介导的环磷酸腺苷(cAMP)生成以及鸟苷酸调节蛋白Gs的浓度。
Mol Pharmacol. 1988 Apr;33(4):389-95.
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Disappearance of beta-adrenergic response of human myometrial adenylate cyclase at the end of pregnancy.妊娠末期人子宫肌层腺苷酸环化酶β-肾上腺素能反应消失。
J Clin Endocrinol Metab. 1989 Jul;69(1):1-6. doi: 10.1210/jcem-69-1-1.

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