Abstract：
:Flibanserin has been reported to be an agonist at 5-HT1A-receptors and an antagonist at 5-HT2A receptors, with higher affinity for 5-HT1A receptors. Despite the fact that less receptor occupation is required by full agonists than by antagonists to exert their effects, flibanserin was shown to exert 5-HT2A antagonism at doses (4-5 mg kg-1) that are lower or equal to those required to stimulate 5-HT1A receptors. In order to understand this phenomenon, the interaction of flibanserin with 5-HT1A and 5-HT2A receptors was evaluated in ex vivo binding studies. This interaction was evaluated in the prefrontal cortex, hippocampus and midbrain by using [3H]8-OH-DPAT and [3H]ketanserin to label 5-HT1A and 5-HT2A receptors, respectively. Flibanserin was given at 1, 10 and 30 mg kg-1 intraperitoneally. The dose of 1 mg kg-1 displaced both radioligands preferentially in the frontal cortex. The doses of 10 and 30 mg kg-1 reduced the binding of both radioligands in all the three brain regions non-selectively by about 50% and 70%, respectively. The displacement was maximal after 0.5 h and was reduced or not evident after 3 h. We conclude that 5-HT2 antagonism brought about by low doses of flibanserin may reflect functional mechanisms more than receptor-mediated effects.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Scandroglio A,Monferini E,Borsini Fdoi
10.1006/phrs.2000.0762keywords:
subject
Has Abstractpub_date
2001-02-01 00:00:00pages
179-83issue
2eissn
1043-6618issn
1096-1186pii
S1043-6618(00)90762-Xjournal_volume
43pub_type
杂志文章abstract：OBJECTIVE:The vasorelaxant effect of 2-arachidonoylglycerol (2-AG) has been well characterised in animals. 2-AG is present in human vascular cells and is up-regulated in cardiovascular pathophysiology. However, the acute vascular actions of 2-AG have not been explored in humans. APPROACH:Mesenteric arteries were obtai...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2014.02.001
更新日期：2014-03-01 00:00:00
abstract：:Epidemiological, clinical and animal studies revealed that sex differences exist in the manifestation and outcome of cardiovascular disease (CVD). The underlying molecular mechanisms implicated in these sex differences are not fully understood. The reasons for sex differences in CVD are definitely multifactorial, but ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.01.019
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abstract：:Lupeol is a natural triterpenoid that widely exists in edible fruits and vegetables, and medicinal plants. In the last decade, a plethora of studies on the pharmacological activities of lupeol have been conducted and have demonstrated that lupeol possesses an extensive range of pharmacological activities such as antic...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
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abstract：BACKGROUND AND OBJECTIVES:Thymidylate synthase (TS) expression levels appear to be related to response to 5-fluorouracil-(5-FU)-based chemotherapy in colorectal cancer (CRC) patients. Three polymorphisms have been proposed as modulators of TS expression: a tandemly repeated sequence (2R/3R) in the 5' UTR, a SNP (G>C) w...
journal_title：Pharmacological research
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abstract：:Oxylipins (OXLs) are bioactive molecules generated by the oxidation of fatty acids that promote the resolution of acute inflammation and prevent chronic inflammatory processes through molecular mechanisms that are not well known. We have previously reported the anti-inflammatory activity of microalgae-derived OXLs and...
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journal_title：Pharmacological research
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doi：10.1016/j.phrs.2004.07.002
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doi：10.1016/j.phrs.2005.12.003
更新日期：2006-03-01 00:00:00
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journal_title：Pharmacological research
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doi：10.1016/s1043-6618(05)80067-2
更新日期：1992-01-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.phrs.2016.05.001
更新日期：2016-09-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1998.0442
更新日期：1999-04-01 00:00:00
abstract：:The EEG and behavioural changes induced by the administration of polyamines (spermine and spermidine) were studied in rabbit. Spermine and spermidine were administered at different doses (200 and 400 micrograms) into the mesencephalic ventricle (i.c.v.) both as a bolus and in constant perfusion (60 min duration). We a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(90)90754-2
更新日期：1990-07-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.02.008
更新日期：2016-04-01 00:00:00
abstract：:The effects of the angiotensin-converting enzyme (ACE) inhibitor monopril and the angiotensin II receptor blocker losartan on serum glucose, protein levels and some serum lipid components were compared in normal and diabetic rats receiving oral antidiabetic drugs 'repaglinide or gliclazide'. The two antihypertensive a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2003.12.019
更新日期：2004-08-01 00:00:00
abstract：:Accumulation of amyloid-β peptides (Aβ) within brain is a major pathogenic hallmark of Alzheimer's disease (AD). Emerging evidence suggests that autophagy, an important intracellular catabolic process, is involved in Aβ clearance. Here, we investigated whether temsirolimus, a newly developed compound approved by Food ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2014.02.008
更新日期：2014-03-01 00:00:00
abstract：:Protein kinase C (PKC) is a family of kinases that are critical in many cellular events. These enzymes are activated by lipid-derived second messengers, are dependent on binding to negatively charged phospholipids and some members also require calcium to attain full activation. The interaction with lipids and calcium ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2007.04.014
更新日期：2007-06-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2008.07.008
更新日期：2008-08-01 00:00:00
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journal_title：Pharmacological research
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doi：10.1006/phrs.2001.0902
更新日期：2001-12-01 00:00:00
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journal_title：Pharmacological research
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doi：10.1016/j.phrs.2010.01.008
更新日期：2010-06-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章
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更新日期：2020-09-01 00:00:00
abstract：:The isolated heart is deservedly one of the most popular experimental models in cardiovascular research, both in terms of cost and the quality and quantity of data it provides. However, it is a deceptively simple model, capable of throwing many problems in the path of the inexperienced or unwary perfuser. The followin...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
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更新日期：2000-06-01 00:00:00
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更新日期：2003-05-01 00:00:00
abstract：:Diabetic erectile dysfunction (DED) hugely affected the patients' sexual life quality. However, there are no satisfactory therapeutic methods and intervention targets for this subtype of erectile dysfunction (ED). Inspired by the clinical practice of traditional Chinese medicine (TCM), we found that hirudin, the main ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105244
更新日期：2021-01-01 00:00:00
abstract：:Atropine (5 mg/kg, s.c., twice daily) had no significant effect on 24-h water consumption on day 1 of treatment; on subsequent days the rats showed a significant increase. Procyclidine (5 mg/kg, s.c., twice daily) had a similar effect, except that the increase in daily water consumption began on the third day of treat...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(90)90745-y
更新日期：1990-01-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2013.01.005
更新日期：2013-04-01 00:00:00
abstract：:A bovine dopamine transporter (bDAT) cDNA was transfected into CV-1 cells, a cell line that lacks vesicular storage and release mechanisms. Using this cell line, the effects of neuroleptic drugs on DAT-mediated uptake and release of dopamine (DA) were examined. All of the neuroleptic drugs tested, inhibited DA uptakes...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：
更新日期：1997-05-01 00:00:00
abstract：:Bleomycin (BLM) is a drug used to treat different types of neoplasms. BLM's most severe adverse effect is lung toxicity, which induces remodeling of lung architecture and loss of pulmonary function, rapidly leading to death. While its clinical role as an anticancer agent is limited, its use in experimental settings is...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2015.04.012
更新日期：2015-07-01 00:00:00
abstract：:Curcumin, a bioactive polyphenol, is a yellow pigment of the Curcuma longa (turmeric) plant. Curcumin has many pharmacologic effects including antioxidant, anti-carcinogenic, anti-obesity, anti-angiogenic and anti-inflammatory properties. Recently, it has been found that curcumin affects lipid metabolism, and subseque...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.008
更新日期：2017-05-01 00:00:00
