β2-adrenoceptor agonist

PURPOSE: This study analyzes the influence of various factors on the hypotensive effect of selective laser trabeculoplasty (SLT) in patients with primary open-angle glaucoma (POAG). MATERIAL AND METHODS: A retrospective study of the SLT effect was performed in 582 patients (756 eyes; mean age - 71.9±9.5 years) with POAG stages I-III. The level of intraocular pressure (IOP) decrease was assessed at 1 day, 1, 3, 6, and 12 months after SLT. The relationship between the hypotensive effect and age, gender, glaucoma stage, initial IOP level, number and type of instilled drugs, presence of intraocular lenses, and the surgeon performing the intervention were analyzed...

INTRODUCTION: Studies have shown that dexmedetomidine (DEX, an a2-adrenoceptors agonist) provides a neuroprotective effect and influences blood glucose levels. Here, we evaluated the effect of prolonged treatment with low doses of DEX on the survival rate of dopaminergic (DAergic) neurons in the substantia nigra and also serum glucose levels in 6-hydroxydopamine (6-OHDA) - induced Parkinson's disease (PD) in the rat. MATERIAL AND METHODS: The neurotoxin of 6-OHDA was injected into the medial forebrain bundle by stereotaxic surgery...

BACKGROUND: Acute kidney injury (AKI) was reported to be one of the initiators of chronic kidney disease (CKD) development. Necroinflammation may contribute to the progression from AKI to CKD. Dexmedetomidine (Dex), a highly selective α2 -adrenoreceptor (AR) agonist, has cytoprotective and "anti-" inflammation effects. This study was designed to investigate the anti-fibrotic properties of Dex in sepsis models. METHODS: C57BL/6 mice were randomly treated with an i...

Alpha-2-adrenoceptor agonist detomidine is a commonly used sedative agent in horses. In addition to the sedative effect, detomidine has been reported to elicit changes in energy metabolism such as hypoinsulinaemia and hyperglycaemia. This study aimed to investigate the effects of detomidine with and without peripherally acting alpha-2-adrenoceptor antagonist vatinoxan on insulin and blood glucose (BG) concentrations in horses after a standard dose of oral carbohydrates. Sixteen horses were assigned to four intravenous treatments in a randomized cross-over design: saline (SAL), detomidine (0...

β2-Adrenoceptors (β2-ARs) are the most abundant subtype of adrenergic receptors in skeletal muscles. Their activation via a stabilization of postsynaptic architecture has beneficial effects in certain models of neuromuscular disorders. However, the ability of β2-ARs to regulate neuromuscular transmission at the presynaptic level is poorly understood. Using electrophysiological recordings and fluorescent FM dyes, we found that β2-AR activation with fenoterol enhanced an involvement of synaptic vesicles in exocytosis and neurotransmitter release during intense activity at the neuromuscular junctions of mouse diaphragm...

Dexmedetomidine (DEX) is a highly selective and potent α2-adrenoceptor (α2-AR) agonist that is widely used as a clinical anesthetic to induce anxiolytic, sedative, and analgesic effects. In recent years, a growing body of evidence has demonstrated that DEX protects against acute kidney injury (AKI) caused by sepsis, drugs, surgery, and ischemia-reperfusion (I/R) in organs or tissues, indicating its potential role in the prevention and treatment of AKI. In this review, we summarized the evidence of the renoprotective effects of DEX on different models of AKI and explored the mechanism...

INTRODUCTION: Many athletes use short-acting inhaled β2 -agonists multiple times weekly during training sessions to prevent exercise-induced bronchoconstriction, but it is unclear if treatment impairs training outcomes. Herein, we investigated performance adaptations in well-trained females and males training with prior inhalation of salbutamol. METHODS: 19 females and 21 males with maximal oxygen uptake ( V 'O2max ) of 50.5±3.3 and 57.9±4.9 mL·min-1 ·kg-1 , respectively, participated in this double-blinded, placebo-controlled, parallel-group study...

The determination of affinity by using functional assays is important in drug discovery because it provides a more relevant estimate of the strength of interaction of a ligand to its cognate receptor than radioligand binding. However, empirical evidence for, so-called, "functional affinity" is limited. Herein, we determined whether the affinity of carvedilol, a β-adrenoceptor antagonist used to treat heart failure that also promotes ERK1/2 phosphorylation, differed between these two pharmacological activities...

INTRODUCTION: Dihydroergotamine mesylate (DHE) is an established effective acute therapy for migraine and is often characterized by its broad receptor pharmacology. Knowledge of DHE pharmacology largely comes from studies employing older methodologies. OBJECTIVE: To assess DHE receptor activity using high-throughput methods to screen for functional ß-arrestin activity at G protein-coupled receptors (GPCRs). METHODS: Functional receptor activities of DHE and sumatriptan succinate (both 10 μM) were screened against 168 GPCRs using the gpcrMAX assay...

Diabetes accelerates muscle atrophy, leading to the deterioration of skeletal muscles. This study aimed to assess the potential of the β2-adrenoceptor agonist, salbutamol (SLB), to alleviate muscle atrophy in streptozotocin (STZ)-induced diabetic rats. Male Sprague Dawley rats were randomized into four groups (n=6): control, SLB, STZ (55 mg/kg, single i.p.), and STZ + SLB (6 mg/kg, orally for 4 weeks). After the final SLB dose, animals underwent tests to evaluate muscle strength and coordination, including forelimb grip strength, wire-hanging, actophotometer, rotarod, and footprint assessments...

INTRODUCTION: Therapeutic advances in drug therapy of chronic obstructive pulmonary disease (COPD) really effective in suppressing the pathological processes underlying the disease deterioration are still needed. Artificial Intelligence (AI) via Machine Learning (ML) may represent an effective tool to predict clinical development of investigational agents. AREAL COVERED: Experimental drugs in Phase I and II development for COPD from early 2014 to late 2022 were identified in the ClinicalTrials...

The pharmacological profile of cannabigerol (CBG), which acid form constitutes the main precursor of the most abundant cannabinoids, has been scarcely studied. It has been reported to target α2- adrenoceptor and 5-HT1A receptor. The locus coeruleus (LC) and the dorsal raphe nucleus (DRN) are the main serotonergic (5-HT) and noradrenergic (NA) areas in the rat brain, respectively. We aimed to study the effect of CBG on the firing rate of LC NA cells and DRN 5-HT cells and on α2 -adrenergic and 5-HT1A autoreceptors by electrophysiological techniques in male Sprague-Dawley rat brain slices...

AIMS: Vascular dysfunction and elevated circulating dipeptidyl peptidase 4 (DPP4) activity are both reported to be involved in the progression of heart failure (HF). While the cardiac benefits of DPP4 inhibitors (DPP4i) have been extensively studied, little is known about the effects of DPP4i on vascular dysfunction in nondiabetic HF. This study tested the hypothesis that vildagliptin (DPP4i) mitigates aortic hyperreactivity in male HF rats. MATERIALS AND METHODS: Male Wistar rats were subjected to left ventricle (LV) radiofrequency ablation to HF induction or sham operation (SO)...

We reported previously that α1 -adrenoceptor (α1 -AR) ligands inhibit chemokine receptor (CR) heteromerization partners of α1B/D -AR. The underlying mechanisms are unknown and in vivo evidence for such effects is missing. Utilizing CCR2 and α1B -AR as prototypical partners, we observed in recombinant systems and THP-1 cells that α1B -AR enhanced whereas its absence inhibited Gαi signaling of CCR2. Phenylephrine and phentolamine reduced the CCR2:α1B -AR heteromerization propensity and inhibited Gαi signaling of CCR2...

OBJECTIVE: Approximately 70% of cancer patients require radiotherapy. However, despite its effectiveness in the treatment of cancer, radiotherapy can also affect and damage surrounding healthy tissues in addition to tumorous tissues. Since testicular tissues are highly radiosensitive, radiotherapy can cause impairments in spermatogenesis leading to infertility. The purpose of this study was to examine the potential radio-protective effect of dexmedetomidine (Dex), an α2-adrenoceptor agonist, on oxidative stress and apoptosis in testicular tissues caused by x-irradiation in rats...

AIMS: Animal models are essential to investigate cardiovascular pathophysiology and pharmacology, but phylogenetic diversity makes it necessary to identify the model with vasculature most similar to that of humans. METHODS AND RESULTS: In this study, we compared the mesenteric arteries of humans, pigs, rabbits and rats in terms of the i) evolutionary changes in the amino acid sequences of α1 and β2 adrenoceptors; M1 , M2 , and M3 muscarinic receptors; and bradykinin (BKR) and thromboxane-prostanoid (TP) receptors, through bioinformatics tools; ii) expression of α1 , β2 , M1, M3 and TP receptors in each tunica, as assessed by immunofluorescence; and iii) reactivity to receptor-dependent and independent contractile agonists and relaxants, by performing organ bath assays...

BACKGROUND: Local and regional anesthetic procedures are valuable tools in veterinary practice. Caudal epidural administration of local anesthetic agents is widely reported for surgical interventions of the tail, anus, rectum, vulva, vagina, urethra, and bladder in the standing horse. Epidural analgesia is also obtained using various drugs such as alpha-2 adrenoceptor agonists, dissociative anesthetics, and opioids. The present study evaluates the anti-nociceptive and sedative effects of epidural administration of romifidine, a romifidine-lidocaine combination, and lidocaine alone in donkeys...

Spinal α2 -adrenoceptor induces analgesia by neuronal inhibition of primary afferent fibers. This family receptor coupled to G i/o proteins can be subdivided into three functional subtypes: α2A , α2B, and α2C -adrenoceptors, and current evidence on spinal analgesia supports the relevance of α2A and seems to exclude the role of α2B , but the functional contribution of α2C -adrenoceptors remains elusive. The present study was designed to pharmacologically dissect the contribution of spinal α2 -adrenoceptor subtypes modulating tonic or acute peripheral nociception...

Abnormalities in the cardiac sympathetic innervation and tone, as well as in the noradrenergic system are associated, among other peripheral complications, with diabetes mellitus. Furthermore, B-HT 933, an agonist at α2 -adrenoceptors, induces a greater cardiac sympathetic inhibition in diabetic rats than in normoglycaemic rats. Accordingly, this pharmacological study analysed the specific involvement of the α2A/2B/2C adrenoceptor subtypes mediating inhibition of the cardioaccelerator sympathetic tone (i...

α2 adrenergic agonists are widely used in clinical anesthesia and ICU sedation owing to their effective sedative and analgesic effects. Lumbago and leg pain is the most common clinical pain disease. Studies have reported that lumbago and leg pain is associated with dysregulation of paravertebral muscles, especially psoas major muscles. In the present study, a unilateral lower extremity chronic inflammation and pain model was established by subcutaneous administration of low-dose complete Fredrin's adjuvant (CFA) into the posterior paw of rats...