Pharmacological evidence that 5-HT1A/1B/1D, α2-adrenoceptors and D2-like receptors mediate ergotamine-induced inhibition of the vasopressor sympathetic outflow in pithed rats

Villamil-Hernández, Ma. Trinidad; Alcántara-Vázquez, Oscar; Sánchez-López, Araceli; Gutiérrez-Lara, Erika J.; Centurión, David

doi:10.1016/j.ejphar.2014.06.036

Cited by 5 publications

(3 citation statements)

References 39 publications

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“…2A, 3A, 4A). The vasopressor responses to electrical stimulation of the sympathetic outflow were accompanied with negligible increases in heart rate (not shown), as previously demonstrated (Villamil-Hernández et al, 2014).…”

Section: Initial Effects Induced By Electrical Stimulation Exogenoussupporting

confidence: 78%

Pharmacological evidence that NaHS inhibits the vasopressor responses induced by stimulation of the preganglionic sympathetic outflow in pithed rats

Centurión

Cruz

Gutiérrez-Lara

et al. 2016

European Journal of Pharmacology

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Section: Initial Effects Induced By Electrical Stimulation Exogenoussupporting

confidence: 78%

Pharmacological evidence that NaHS inhibits the vasopressor responses induced by stimulation of the preganglionic sympathetic outflow in pithed rats

Centurión

Cruz

Gutiérrez-Lara

et al. 2016

European Journal of Pharmacology

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“…Dihydroergotamine, Dihydroergotoxine and Ergotamine are the synthetic drugs developed in the 20th century for treating migraine (Metra et al, 1995;Villamil-Hernandez et al, 2014; Connelly et al, 2020) (Figure 4). Our docking results show that one hydrogen bonds involving LYS-26 and van der Waals energy maintained upon the binding of DHE with the interface of ACE2 and Spike glycoprotein complex.…”

Section: Docking Results Of Eight Drugs Against Ace2(cats)-sars-cov-2mentioning

confidence: 99%

Predicting the Animal Susceptibility and Therapeutic Drugs to SARS-CoV-2 Based on Spike Glycoprotein Combined With ACE2

Shen

Liu

et al. 2020

Front. Genet.

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Recently, a few animals have been frequently reported to have been diagnosed with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Whether they are SARS-CoV-2 intermediate hosts is worthy of great attention. The interaction of SARS-CoV-2 spike protein and its acceptor protein ACE2 is an important issue in determining viral host range and cross-species infection, while the binding capacity of Spike protein to ACE2 of different species is unknown. Here, we used the atomic structure model of SARS-CoV-2 and human ACE2 to assess the receptor utilization capacity of ACE2s from 10 kinds of animals. Results show that chimpanzees, domestic cats and cattles are more susceptible to infection by SARS-CoV-2. Cats in particular, such as pet cats and stray cats, interact very closely with humans, implying the necessity to carefully evaluate the risk of cats during the current COVID-19 pandemic. Furthermore, based on ACE2(cats)-SARS-CoV-2-RBD model, through high-throughput screening methods using a pool of 30,000 small molecules, eight compounds were selected for binding free energy calculations. All the eight compounds can effectively interfere with the binding of ACE2 and Spike protein, especially Nelfinavir, providing drug candidates for the treatment and prevention of SARS-CoV-2, suggesting further assessment of the anti-SARS-CoV-2 activity of these compounds in cell culture. Although we only reported the results of the simulation, and more laboratory and epidemiological investigation are required. Like cats are a risk factor, we can further detect SARS-CoV-2 according to the susceptibility of different animals, find the potential host of infection, and completely cut off the living space of the virus. Especially, cats could be a choice of animal model for screening antiviral drugs or vaccine candidates against SARS-CoV-2.

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“…5-HT 1 receptors are widely expressed in perivascular and cardiac sympathetic nerve endings; their activation is linked to cardiovascular sympathetic inhibition [48][49][50][51]. Specifically, selective stimulation of 5-HT 1A , 5-HT 1B , and 5-HT 1D receptors produced inhibition of the sympathetic vasopressor outflow in pithed rats [38,52]. This is a useful experimental model to pharmacologically study the prejunctional modulation of sympathetic nerve endings, since the CNS in not functional and, consequently, central compensatory cardiovascular reflexes are excluded [3].…”

Section: The 5-ht Receptors Inhibiting the Autonomic Outflowmentioning

confidence: 99%

Serotonergic Modulation of Neurovascular Transmission: A Focus on Prejunctional 5-HT Receptors/Mechanisms

et al. 2023

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5-Hydroxytryptamine (5-HT), or serotonin, plays a crucial role as a neuromodulator and/or neurotransmitter of several nervous system functions. Its actions are complex, and depend on multiple factors, including the type of effector or receptor activated. Briefly, 5-HT can activate: (i) metabotropic (G-protein-coupled) receptors to promote inhibition (5-HT1, 5-HT5) or activation (5-HT4, 5-HT6, 5-HT7) of adenylate cyclase, as well as activation (5-HT2) of phospholipase C; and (ii) ionotropic receptor (5-HT3), a ligand-gated Na+/K+ channel. Regarding blood pressure regulation (and beyond the intricacy of central 5-HT effects), this monoamine also exerts direct postjunctional (on vascular smooth muscle and endothelium) or indirect prejunctional (on autonomic and sensory perivascular nerves) effects. At the prejunctional level, 5-HT can facilitate or preclude the release of autonomic (e.g., noradrenaline and acetylcholine) or sensory (e.g., calcitonin gene-related peptide) neurotransmitters facilitating hypertensive or hypotensive effects. Hence, we cannot formulate a specific impact of 5-HT on blood pressure level, since an increase or decrease in neurotransmitter release would be favoured, depending on the type of prejunctional receptor involved. This review summarizes and discusses the current knowledge on the prejunctional mechanisms involved in blood pressure regulation by 5-HT and its impact on some vascular-related diseases.

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Pharmacological evidence that 5-HT1A/1B/1D, α2-adrenoceptors and D2-like receptors mediate ergotamine-induced inhibition of the vasopressor sympathetic outflow in pithed rats

Cited by 5 publications

References 39 publications

Pharmacological evidence that NaHS inhibits the vasopressor responses induced by stimulation of the preganglionic sympathetic outflow in pithed rats

Pharmacological evidence that NaHS inhibits the vasopressor responses induced by stimulation of the preganglionic sympathetic outflow in pithed rats

Predicting the Animal Susceptibility and Therapeutic Drugs to SARS-CoV-2 Based on Spike Glycoprotein Combined With ACE2

Serotonergic Modulation of Neurovascular Transmission: A Focus on Prejunctional 5-HT Receptors/Mechanisms

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