Beta-Adrenergic Blockers

Frishman, William H.; Cheng-Lai, Angela; Chen, Julie

doi:10.1007/978-1-4615-6767-7_8

Cited by 5 publications

(8 citation statements)

References 37 publications

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“…Beta-blockers that normalize catecholamine production ( 88 ) and reduce proinflammatory cytokine levels ( 89 ) have been shown to alleviate pain in patients with CPPCs. Previously, we found that delivery of the β3AR antagonist SR59230A prevents the development of COMT inhibitor-induced pain at plantar sites ( 90 ).…”

Section: Discussionmentioning

confidence: 99%

A Novel Mouse Model of Chronic Primary Pain Conditions that Integrates Clinically Relevant Genetic and Environmental Factors

Wang

Kim

Klein

et al. 2022

Preprint

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Chronic primary pain conditions (CPPCs) affect over 100 million people, predominantly women. Yet, they remain ineffectively treated due, in large part, to lack of valid animal models with translational relevance. Here, we characterized a novel mouse model of CPPCs that integrated clinically-relevant genetic (catechol-o-methyltransferase; COMT knockdown) and environmental (stress and minor injury) factors. Compared to wildtype mice, COMT+/- mice undergoing the repeated swim stress and molar extraction surgery intervention exhibited pronounced multi-site body pain and depressive-like behavior lasting more than 3 months. The COMT+/- mice undergoing the intervention also exhibited enhanced activity of primary afferent DRG nociceptors innervating hindpaw and back sites and increased plasma levels of norepinephrine and the pro-inflammatory cytokines IL-6 and IL-17A. Notably, the pain and depressive-like behavior was of greater magnitude and longer duration (lasting at least 12 months) in females compared to males. Further, increases in anxiety-like behavior and IL-6 levels were female-specific. Intervention-induced body pain and nociception in COMT+/- mice was blocked by a beta-3 adrenergic antagonist, demonstrating predictive validity. Finally, the effect of COMT genotype x stress interactions on pain and IL-6 and IL-17A levels was observed in our clinical CPPC case-control cohort, demonstrating construct validity. Thus, our novel mouse model reliably recapitulates clinically- and biologically-relevant features of CPPCs and can be further implemented to test underlying mechanisms and discover new therapeutics.

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Section: Discussionmentioning

confidence: 99%

A Novel Mouse Model of Chronic Primary Pain Conditions that Integrates Clinically Relevant Genetic and Environmental Factors

Wang

Kim

Klein

et al. 2022

Preprint

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“…Much effort has been dedicated to developing new vasodilating β ‐blockers in order to minimize the adverse effects of traditional nonvasodilatory β ‐blockers such as propranolol, metoprolol and atenolol (Toda, ). Carvedilol and labetalol are two representative vasodilating β ‐blockers against both α ‐ and β ‐adrenergic receptors (Frishman, ; Frishman & Saunders, ). Recently, our group synthesized another novel vasodilatory β ‐blocker possessing both α ‐ and β ‐adrenoceptor blocking activities.…”

Section: Introductionmentioning

confidence: 99%

Accurate determination of a novel vasodilatory β‐blocker TJ0711 using LC‐MS/MS: Resolution of an isobaric metabolite interference in dog plasma

Zhu

Guan

et al. 2018

Biomedical Chromatography

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A rapid, robust and sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for bioanalysis of TJ0711, a novel vasodilatory β-blocker in dog plasma. This assay is able to chromatographically separate TJ0711 from its isobaric metabolite as well as glucuronide conjugates. Chromatographic separation was achieved on a Welch Ultimate-XB C column (2.1 × 100 mm, 3 μm). The analyte and internal standard (propranolol) were extracted from plasma by liquid-liquid extraction using ethyl acetate. The mass spectrometric detection was carried out in positive ion multiple reaction monitoring mode. Good linearity was obtained over the concentration range of 0.5-500 ng/mL (r > 0.99) for TJ0711. Moreover, the method had good accuracy (RE ranging from -2.70 to -0.32%) and precision (RSD < 7.55%). TJ0711 was stable in dog plasma for at least 6 h at ambient temperature, for at least 30 days at -20°C and after three freeze-thaw cycles. This method was successfully applied to a preclinical pharmacokinetic study and the results demonstrated linear pharmacokinetics of TJ0711 over a dose range from 0.03 to 0.3 mg/kg. No significant gender differences were observed in TJ0711 plasma pharmacokinetic parameters.

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“…When beta blockers are administered, they inhibit the catecholamines to bind the beta adrenergic receptors and lower the blood pressure and heart muscle contraction. [1][2][3] There are mainly three types of beta adrenergic receptors. Beta 1 receptors are mainly found in heart and kidney whereas beta 2 receptors are found in lung, GIT and liver.…”

Section: Introductionmentioning

confidence: 99%

Coating Efficiency in Preventing Photolytic Degradation of Two Randomly Selected Brands of Metoprolol Tartrate

Rahman

Karim

Nandi

et al. 2016

Int. J. Pharm. Sci. Drug Res.

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This research work was carried out to determine whether the film coating is effective to prevent the photolytic degradation of Metoprolol tartrate which is known to have photosensitivity. For this purpose, two randomly selected brands of two different pharmaceutical companies were chosen i.e. Brand A and Brand B. These two brands were exposed to different lighting conditions (normal light, direct sunlight as well as two incandescent lights i.e. 25 watt bulb, 40 watt bulb). Potency tests were performed using UV spectroscopy which showed gradual decline in potency of the tablets under aforesaid lighting conditions and the potency degradations were found 11.48%, 12.92%, 22.62%, 16.87% for Brand A and 14.74%, 14.24%, 10.88%, 18.10% for Brand B under 25 watt bulb, 40 watt bulb, direct sunlight and normal room light respectively. So this study reveals that the both brands containing metoprolol tartrate showed significant light sensitivity even though they are coated and protective opaque packaging is highly recommended for their protection.

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Beta-Adrenergic Blockers

Cited by 5 publications

References 37 publications

A Novel Mouse Model of Chronic Primary Pain Conditions that Integrates Clinically Relevant Genetic and Environmental Factors

A Novel Mouse Model of Chronic Primary Pain Conditions that Integrates Clinically Relevant Genetic and Environmental Factors

Accurate determination of a novel vasodilatory β‐blocker TJ0711 using LC‐MS/MS: Resolution of an isobaric metabolite interference in dog plasma

Coating Efficiency in Preventing Photolytic Degradation of Two Randomly Selected Brands of Metoprolol Tartrate

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