Usefulness of 5-Ht2a Receptor Antagonists for The Treatment of Cardiovascular Complications in Diabetes

Goyal, Ramesh K.; Umrani, Dhananjay N.; Bodiwala, Dipali N.; Dhalla, Naranjan S.

doi:10.1007/978-1-4419-9232-1_25

Cited by 3 publications

(5 citation statements)

References 59 publications

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“…Lumb (1993) reported the involvement of 5-HT 3 receptors in the anti-emetic action of Z. officinale. Earlier studies from our laboratory have reported that 5-HT-induced hyperglycaemia was inhibited by the 5-HT 2A antagonist sarpogrelate and the 5-HT 3 antagonist ondansetron (Goyal et al 2003). The inhibition of 5-HT-induced hyperglycaemia by Z. officinale suggests the presence of a 5-HT 2A or 5-HT 3 receptor antagonist in Z. officinale.…”

Section: Blood Pressurementioning

confidence: 66%

“…The inhibition of 5-HT-induced hyperglycaemia by Z. officinale suggests the presence of a 5-HT 2A or 5-HT 3 receptor antagonist in Z. officinale. Chronic treatment with sarpogrelate and ondansetron is reported to decrease blood glucose and to have beneficial effects on lipid profile in STZ-diabetic rats (Goyal et al 2003). If Z. officinale contains a 5-HT receptor antagonist, it is expected to produce beneficial effects in STZ-diabetic rats.…”

Section: Blood Pressurementioning

confidence: 99%

“…Various studies have shown that 5-HT levels are high in streptozotocin (STZ) diabetic rats (Martin et al 1985). 5-HT produces hyperglycaemia in normoglycaemic rats involving specific 5-HT 2A and 5-HT 3 receptors (Goyal et al 2003). It has further been shown that chronic treatment with the 5-HT 2 antagonist sarpogrelate and 5-HT 3 antagonist ondansetron produces a number of beneficial effects in diabetic rats with respect to glucose and other biochemical alterations (Goyal et al 2003).…”

Section: Introductionmentioning

confidence: 99%

“…5-HT produces hyperglycaemia in normoglycaemic rats involving specific 5-HT 2A and 5-HT 3 receptors (Goyal et al 2003). It has further been shown that chronic treatment with the 5-HT 2 antagonist sarpogrelate and 5-HT 3 antagonist ondansetron produces a number of beneficial effects in diabetic rats with respect to glucose and other biochemical alterations (Goyal et al 2003). Much of the activity of Z. officinale is because of its 5-HT antagonism.…”

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Anti-diabetic activity of Zingiber officinale in streptozotocin-induced type I diabetic rats

Akhani

Vishwakarma

Goyal

2004

Journal of Pharmacy and Pharmacology

205

132

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The fresh and dried rhizome of Zingiber officinale Roscoe (commonly known as ginger) is widely used in traditional medicine. We have studied the effect of the juice of Z. officinale (4 mL kg(-1), p.o. daily) for 6 weeks on streptozotocin (STZ)-induced type I diabetic rats with particular reference to the involvement of serotonin (5-hydroxytryptamine; 5-HT) receptors in glycaemic control. In normoglycaemic rats, 5-HT (1mg kg(-1), i.p.) produced hyperglycaemia and hypoinsulinaemia, which was significantly prevented by the juice of Z. officinale. STZ-diabetes produced a significant increase in fasting glucose levels that was associated with a significant decrease in serum insulin levels. Treatment with Z. officinale produced a significant increase in insulin levels and a decrease in fasting glucose levels in diabetic rats. In an oral glucose tolerance test, treatment with Z. officinale was found to decrease significantly the area under the curve of glucose and to increase the area under the curve of insulin in STZ-diabetic rats. Treatment with Z. officinale also caused a decrease in serum cholesterol, serum triglyceride and blood pressure in diabetic rats. Our data suggest a potential antidiabetic activity of the juice of Z. officinale in type I diabetic rats, possibly involving 5-HT receptors.

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Section: Blood Pressurementioning

confidence: 66%

Section: Blood Pressurementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Anti-diabetic activity of Zingiber officinale in streptozotocin-induced type I diabetic rats

Akhani

Vishwakarma

Goyal

2004

Journal of Pharmacy and Pharmacology

205

132

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“…[ 25 ] Moreover, it has been shown that these effects can be inhibited by 5-HT 2A R blockers such as ketanserin, which suppresses 5-HT release and protects the heart against ischemia. [ 26 27 28 ] Since elevations of platelet 5-HT 2A R have been found in depressed patients, these studies suggest that 5-HT 2A R may constitute the pathophysiological cause of co-occurring MI and depression.…”

Section: Discussionmentioning

confidence: 91%

5-Hydroxytryptamine Changes under Different Pretreatments on Rat Models of Myocardial Infarction and/or Depression

Zhang

Zhou

Wei

2017

Chinese Medical Journal

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Background:Psychocardiological researches have suggested a central role of 5-hydroxytryptamine (5-HT) on psychocardiological mechanism. This study aimed to further explore the central role of 5-HT and pretreatment effects of XinLingWan on rats with myocardial infarction (MI) and/or depression.Methods:Ninety Sprague-Dawley rats were randomly divided into three groups: MI group, depression group, and MI + depression group (n = 30 in each group). Each group was then divided into three subgroups (n = 10 in each subgroup): a negative control subgroup (NCS), a Western medicine subgroup (WMS), and a traditional Chinese medicine subgroup (TCMS), which were received pretreatment once a day for 4 weeks by saline, 20 mg/kg sertraline mixed with 2 ml saline, and 40 mg/kg XingLingWan mixed with 2 ml saline, respectively. Different rat models were established after different pretreatments. Rats were then sacrificed for detection of serum 5-HT, platelet 5-HT, 5-HT2A receptors (5-HT2AR), and serotonin transporter (SERT). Data were analyzed by one-way analysis of variance (ANOVA) and least-significant difference (LSD) testing.Results:MI group: compared with NCS, there was a significant increase in WMS and TCMS of serum 5-HT (176.15 ± 11.32 pg/ml vs. 334.50 ± 29.09 pg/ml and 474.04 ± 10.86 pg/ml, respectively, both P = 0.000), platelet 5-HT (129.74 ± 27.17 pg/ml vs. 322.24 ± 11.60 pg/ml and 340.4 5 ± 17.99 pg/ml, respectively, both P = 0.000); depression group: compared with NCS, there was a significant increase in WMS and TCMS of serum 5-HT (194.69 ± 5.09 pg/ml vs. 326.21 ± 39.98 pg/ml and 456.33 ± 23.12 pg/ml, respectively, both P = 0.000), platelet 5-HT (175.15 ± 4.07 pg/ml vs. 204.56 ± 18.59 pg/ml and 252.03 ± 22.26 pg/ml, respectively, P = 0.004 and P = 0.000, respectively); MI + depression group: compared with NCS, there was a significant increase in both WMS and TCMS of serum 5-HT (182.50 ± 10.23 pg/ml vs. 372.55 ± 52.23 pg/ml and 441.76 ± 23.38 pg/ml, respectively, both P = 0.000) and platelet 5-HT (180.83 ± 11.08 pg/ml vs. 221.12 ± 22.23 pg/ml and 265.37 ± 29.49 pg/ml, respectively, P = 0.011 and P = 0.000, respectively).Conclusions:By elevating the amount of 5-HT and modulating 5-HT2AR and SERT levels in serum and platelets, XinLingWan and sertraline were found to exert pretreatment effect on rat models of MI and/or depression.

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Mechanisms of subcellular remodeling in heart failure due to diabetes

et al. 2013

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Diabetic cardiomyopathy is not only associated with heart failure but there also occurs a loss of the positive inotropic effect of different agents. It is now becoming clear that cardiac dysfunction in chronic diabetes is intimately involved with Ca(2+)-handling abnormalities, metabolic defects and impaired sensitivity of myofibrils to Ca(2+) in cardiomyocytes. On the other hand, loss of the inotropic effect in diabetic myocardium is elicited by changes in signal transduction mechanisms involving hormone receptors and depressions in phosphorylation of various membrane proteins. Ca(2+)-handling abnormalities in the diabetic heart occur mainly due to defects in sarcolemmal Na(+)-K(+) ATPase, Na(+)-Ca(2+) exchange, Na(+)-H(+) exchange, Ca(2+)-channels and Ca(2+)-pump activities as well as changes in sarcoplasmic reticular Ca(2+)-uptake and Ca(2+)-release processes; these alterations may lead to the occurrence of intracellular Ca(2+) overload. Metabolic defects due to insulin deficiency or ineffectiveness as well as hormone imbalance in diabetes are primarily associated with a shift in substrate utilization and changes in the oxidation of fatty acids in cardiomyocytes. Mitochondria initially seem to play an adaptive role in serving as a Ca(2+) sink, but the excessive utilization of long-chain fatty acids for a prolonged period results in the generation of oxidative stress and impairment of their function in the diabetic heart. In view of the activation of sympathetic nervous system and renin-angiotensin system as well as platelet aggregation, endothelial dysfunction and generation of oxidative stress in diabetes and blockade of their effects have been shown to attenuate subcellular remodeling, metabolic derangements and signal transduction abnormalities in the diabetic heart. On the basis of these observations, it is suggested that oxidative stress and subcellular remodeling due to hormonal imbalance and metabolic defects play a critical role in the genesis of heart failure during the development of diabetic cardiomyopathy.

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Usefulness of 5-Ht2a Receptor Antagonists for The Treatment of Cardiovascular Complications in Diabetes

Cited by 3 publications

References 59 publications

Anti-diabetic activity of Zingiber officinale in streptozotocin-induced type I diabetic rats

Anti-diabetic activity of Zingiber officinale in streptozotocin-induced type I diabetic rats

5-Hydroxytryptamine Changes under Different Pretreatments on Rat Models of Myocardial Infarction and/or Depression

Mechanisms of subcellular remodeling in heart failure due to diabetes

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