- A literature perspective on the pharmacological applications of yohimbine. [Review]
- Introduction: Phytochemicals have garnered much attention because they are useful in managing several human diseases. Yohimbine is one such phytochemical with significant pharmacological potential and could be exploited for research by medicinal chemists. It is an indole alkaloid obtained from various natural/synthetic sources.Aims and Results: The research on yohimbine started early, and its use…
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- Alpha2-adrenergic receptor activation reinstates motor deficits in rats recovering from cortical injury. [Journal Article]
- Norepinephrine plays an important role in motor functional recovery after a brain injury caused by ferrous chloride. Inhibition of norepinephrine release by clonidine is correlated with motor deficits after motor cortex injury. The aim of this study was to analyze the role of α2-adrenergic receptors in the restoration of motor deficits in recovering rats after brain damage. The rats were randomly…
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- The Antiarrhythmic and Hypotensive Effects of S-61 and S-73, the Pyrrolidin-2-one Derivatives with α1-Adrenolytic Properties. [Journal Article]
- Heart rhythm abnormalities are a cause of many deaths worldwide. Unfortunately, the available antiarrhythmic drugs show limited efficacy and proarrhythmic potential. Thus, efforts should be made to search for new, more effective, and safer pharmacotherapies. Several studies suggested that blocking the α1-adrenoceptors could restore normal heart rhythm in arrhythmia. In this study, we aimed to ass…
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- 6-nitrodopamine is a major endogenous modulator of human vas deferens contractility. [Journal Article]
- CONCLUSIONS: 6-ND should be considered a major endogenous modulator of human vas deferens contractility and possibly plays a pivotal role in the emission process of ejaculation. It offers a novel and shared mechanism of action for tricyclic antidepressants and α1 -adrenergic receptor antagonists.
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- Cannabigerol (CBG) attenuates mechanical hypersensitivity elicited by chemotherapy-induced peripheral neuropathy. [Journal Article]
- CONCLUSIONS: Our findings support the role of CBG in alleviating mechanical hypersensitivity evoked by cisplatin-induced peripheral neuropathy, but highlight that these effects may be limited to specific types of pain.
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- Adrenergic Control of Primo Tissue Size in Rats. [Journal Article]J Acupunct Meridian Stud. 2022 Feb 28; 15(1):25-36.JA
- CONCLUSIONS: Adrenergic signaling controls hyperplastic changes in the organ surface PVS in rats. These findings may explain the morphological dynamics of the PVS tissues proposed by Bong Han Kim and further clarify the pathophysiological roles of the PVS.
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- Sympathetic modulation of tumor necrosis factor alpha-induced nociception in the presence of oral squamous cell carcinoma. [Journal Article]
- Head and neck squamous cell carcinoma (HNSCC) causes more severe pain and psychological stress than other types of cancer. Despite clinical evidence linking pain, stress, and cancer progression, the underlying relationship between pain and sympathetic neurotransmission in oral cancer is unknown. We found that human HNSCC tumors and mouse tumor tissue are innervated by peripheral sympathetic and s…
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- Deleterious effects of levamisole, a cocaine adulterant, in rabbit aorta. [Journal Article]Vascul Pharmacol. 2022 06; 144:106992.VP
- Levamisole, a veterinary anthelmintic drug, is one of the most widely used and dangerous cocaine adulterants. Like cocaine, levamisole acutely blocks noradrenaline reuptake but with much less potency, although its vascular effects are not well known. In this study, we evaluated the vascular effects of levamisole and cocaine in rabbit aortic rings used for isometric recording of tension in organ b…
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- Mitigation of dexamethasone-induced nephrotoxicity by modulating the activity of adrenergic receptors: Implication of Wnt/β-arrestin2/β-catenin pathway. [Journal Article]
- The present study aimed to investigate the role of α and β-adrenergic receptors (βARs) in mediation or modulation of the dexamethasone-induced nephrotoxicity by using different pharmacological interventions. Nephrotoxicity was induced by subcutaneous injection of dexamethasone (10 mg/kg) for 7 days in Wistar albino rats. Eight groups were used: control; dexamethasone; carvedilol; phenylephrine; c…
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- Increased β-adrenergic stimulation augments vascular smooth muscle cell calcification via PKA/CREB signalling. [Journal Article]
- In chronic kidney disease (CKD), hyperphosphatemia promotes medial vascular calcification, a process augmented by osteogenic transdifferentiation of vascular smooth muscle cells (VSMCs). VSMC function is regulated by sympathetic innervation, and these cells express α- and β-adrenergic receptors. The present study explored the effects of β2-adrenergic stimulation by isoproterenol on VSMC calcifica…
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- A clinical comparative study of dexmedetomidine as an adjuvant to 2% plain lignocaine and 2% lignocaine with 1:200,000 adrenaline as local anesthetic agents for surgical removal of impacted mandibular third molars. [Journal Article]
- CONCLUSIONS: The study concluded that the combination of dexmedetomidine with lignocaine enhances the local anesthetic potency of lignocaine when injected for nerve blocks.
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- Involvement of dopamine D2 and glutamate NMDA receptors in the antidepressant-like effect of amantadine in mice. [Journal Article]
- The present study investigated the pharmacological mechanisms of the antidepressant-like effects of amantadine in mice and their influence on hippocampal neurogenesis. To improve the translational validity of preclinical results, reproducibility across laboratories and replication in other animal models and species are crucial. Single amantadine administration at doses of 50 and 75 mg/kg resulted…
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- Dexmedetomidine exerts a protective effect on ischemic brain injury by inhibiting the P2X7R/NLRP3/Caspase-1 signaling pathway. [Journal Article]
- Dexmedetomidine (Dex) has been suggested to exert a protective function in ischemic brain injury. In this study, we aimed to elucidate the intrinsic mechanisms of Dex in regulating microglia pyroptosis in ischemic brain injury via the purinergic 2X7 receptor (P2X7R)/NLRP3/Caspase-1 signaling pathway. First, permanent middle cerebral artery occlusion (p-MCAO) rat model was established, followed by…
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- Carvedilol, an Adrenergic Blocker, Suppresses Melanin Synthesis by Inhibiting the cAMP/CREB Signaling Pathway in Human Melanocytes and Ex Vivo Human Skin Culture. [Journal Article]
- Catecholamines function via G protein-coupled receptors, triggering an increase in intracellular levels of 3',5'-cyclic adenosine monophosphate (cAMP) in various cells. Catecholamine biosynthesis and the β-adrenergic receptor exist in melanocytes; thus, catecholamines may play critical roles in skin pigmentation. However, their action and mechanisms mediating melanogenesis in human skin have not …
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- Impairment of Hypoxia-Induced CA IX by Beta-Blocker Propranolol-Impact on Progression and Metastatic Potential of Colorectal Cancer Cells. [Journal Article]
- The coexistence of cancer and other concomitant diseases is very frequent and has substantial implications for treatment decisions and outcomes. Beta-blockers, agents that block the beta-adrenergic receptors, have been related also to cancers. In the model of multicellular spheroids formed by colorectal cancer cells we described a crosstalk between beta-blockade by propranolol and tumour microenv…
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- A Review of Antipsychotics and Priapism. [Review]
- CONCLUSIONS: Clinicians should educate patients treated with antipsychotics about the potential for priapism and its sequelae including permanent erectile dysfunction. Appropriate patient education will raise awareness, encourage early reporting, and help reduce the long-term consequences associated with priapism through early intervention. Hwang T, Shah T,Sadeghi-NejadH. A Review of Antipsychotics and Priapism. Sex Med Rev 2021;9:464-471.
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- Pharmacological Screening of Mangifera indica Seeds for Antidepressant-like Action Along with a Mechanistic Study. [Journal Article]
- Depression is emerging as a major global issue. There are several antidepressants available in the market, but their efficacy is usually unpredictable. Therefore, there is a need to find an alternative therapeutic agent with better therapeutic efficacy and availability. In the current investigation, the antidepressant-like action of the aqueous methanolic extract of Mangifera indica seeds (25, 50…
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- Fine tuning by protein kinases of CaV1.2 channel current in rat tail artery myocytes. [Journal Article]
- Seventeen compounds, rather selective, direct or indirect inhibitors and activators of PKA, PKG, and PKC, were analysed for effects on vascular CaV1.2 channel current (ICa1.2) by using the patch-clamp technique in single rat tail artery myocytes. The aim was to investigate how PKs regulate ICa1.2 and disclose any unexpected modulation of CaV1.2 channel function by these agents. The cAMP analogues…
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- Carvedilol induces biased β1 adrenergic receptor-nitric oxide synthase 3-cyclic guanylyl monophosphate signalling to promote cardiac contractility. [Journal Article]
- CONCLUSIONS: These observations present a novel β1AR-NOS3 signalling pathway to promote cardiac inotropy in the heart, indicating that this signalling paradigm may be targeted in therapy of heart diseases with reduced ejection fraction.
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- Imipramine improves visceral sensation and gut barrier in rat models of irritable bowel syndrome. [Journal Article]
- An impaired gut barrier, possibly leading to visceral hypersensitivity has been recently recognized to be one of the pivotal pathophysiology of irritable bowel syndrome (IBS). We previously showed that lipopolysaccharide (LPS), corticotropin-releasing factor (CRF), and repeated water avoidance stress (WAS) induce visceral hypersensitivity and colonic hyperpermeability via pro-inflammatory cytokin…
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- Effects of blocking mGluR5 on primate dorsolateral prefrontal cortical neuronal firing and working memory performance. [Journal Article]
- CONCLUSIONS: The mixed effects of MTEP on cognitive performance may arise from opposing actions at pre- vs. post-synaptic mGluR5 in dlPFC. These data from monkeys suggest that future clinical trials should include low doses, and identification of potential subgroup responders.
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- Loss of diffuse noxious inhibitory control after traumatic brain injury in rats: A chronic issue. [Journal Article]
- Chronic pain is one of the most challenging and debilitating symptoms to manage after traumatic brain injury (TBI), yet the underlying mechanisms remain elusive. The disruption of normal endogenous pain control mechanisms has been linked to several forms of chronic pain and may play a role in pain after TBI. We hypothesized therefore that dysfunctional descending noradrenergic and serotonergic pa…
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- Endothelial Nitric Oxide Suppresses Action-Potential-Like Transient Spikes and Vasospasm in Small Resistance Arteries. [Journal Article]
- Endothelial dysfunction in small arteries is a ubiquitous, early feature of cardiovascular disease, including hypertension. Dysfunction reflects reduced bioavailability of endothelium-derived nitric oxide (NO) and depressed endothelium-dependent hyperpolarization that enhances vasoreactivity. We measured smooth muscle membrane potential and tension, smooth muscle calcium, and used real-time quant…
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- Mirtazapine, an α2 Antagonist-Type Antidepressant, Reverses Pain and Lack of Morphine Analgesia in Fibromyalgia-Like Mouse Models. [Journal Article]
- Treatment of fibromyalgia is an unmet medical need; however, its pathogenesis is still poorly understood. In a series of studies, we have demonstrated that some pharmacological treatments reverse generalized chronic pain but do not affect the lack of morphine analgesia in the intermittent cold stress (ICS)-induced fibromyalgia-like pain model in mice. Here we report that repeated intraperitoneal …
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- The affinity and selectivity of α-adrenoceptor antagonists, antidepressants, and antipsychotics for the human α1A, α1B, and α1D-adrenoceptors. [Journal Article]
- α1-adrenoceptor antagonists are widely used for hypertension (eg, doxazosin) and benign prostatic hypertrophy (BPH, eg, tamsulosin). Some antidepressants and antipsychotics have been reported to have α1 affinity. This study examined 101 clinical drugs and laboratory compounds to build a comprehensive understanding of α1-adrenoceptor subtype affinity and selectivity. [3H]prazosin whole-cell bindin…
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- Fentanyl but not Morphine Interacts with Nonopioid Recombinant Human Neurotransmitter Receptors and Transporters. [Journal Article]
- Synthetic opioids, including fentanyl and its analogs, have therapeutic efficacy in analgesia and anesthesia. However, their illicit use in the United States has increased and contributed to the number one cause of death for adults 18-50 years old. Fentanyl and the heroin metabolite morphine induce respiratory depression that can be treated with the μ opioid receptor (MOR) antagonist naloxone. Wi…
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- Acute Fulminant Hepatic Failure and Renal Failure Induced by Oral Amiodarone: A Case Report and Literature Review. [Case Reports]
- Amiodarone is a class III antiarrhythmic agent that inhibits adrenergic stimulation by blocking alpha and beta receptors. It prolongs action potential and refractory period in myocardial tissue. Its remarkably long half-life is associated with a myriad of adverse events. Here, we present an 85-year-old male patient who was started on amiodarone for atrial flutter. After three oral doses, he devel…
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- Successful Outcome Following Intravenous Lipid Emulsion Rescue Therapy in a Patient with Cardiac Arrest Due to Amitriptyline Overdose. [Case Reports]
- BACKGROUND The management of patients with tricyclic antidepressant drug overdose can be a challenge for the emergency department physician. Tricyclic antidepressants block alpha-adrenergic receptors and the anticholinergic effects may lead to cardiotoxicity, resulting in arrhythmias and hypotension that can lead to patient mortality. This report is of a case of a 28-year-old woman who presented …
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- Synthesis, in vitro and in vivo evaluation of 11C-O-methylated arylpiperazines as potential serotonin 1A (5-HT1A) receptor antagonist radiotracers. [Journal Article]
- CONCLUSIONS: Despite efficient radiolabeling, results from PET imaging experiments limit the application of [11C]3 for in vivo quantification of 5-HT1A receptors. Nevertheless, derivatives of compound 3 may provide a scaffold for alternative PET radiotracers with improved selectivity for 5-HT 1A receptors or α1-adrenergic receptors.
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