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Bronchospasmolytic and Adenosine Binding Activity of 8- (Proline / Pyrazole)- Substituted Xanthine Derivatives.

Curr Drug Discov Technol

January 2022

Department of Pharmacy, Banasthali Vidyapith, Banasthali-304022, Rajasthan, India.

Background: 8-Phenyltheophylline derivatives exhibit prophylactic effects at a specific dose but do not produce the cardiovascular or emetic side effects associated with xanthines, thereby exhibiting unique characteristics of potential therapeutic importance.

Methods: Novel series of 8-(proline/pyrazole)-substituted xanthine analogs have been synthesized. The affinity and selectivity of compounds to adenosine receptors have been assessed by radioligand binding studies.

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The β-adrenergic receptor (βAR) is relevant for surfactant formation in alveolar type 2 cells and reduction of intracellular calcium concentration in bronchial muscle cells and thus for secretolytic and bronchospasmolytic effects. Herbal medicinal products that affect the βAR system are used to treat common cold and bronchitis accompanied with mucus covered and narrowed airways. The present work compares the influence of an ivy preparation and an ivy/thyme combination on the β-adrenergic signal transduction.

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The aldehyde derivatives of 1,3-dipropyl xanthines as described in this paper, constitutes a new series of selective adenosine ligands displaying bronchospasmolytic activity. The effect of substitution at third- and fourth-position of 8-phenyl xanthine has also been taken into consideration. The synthesized compounds showed varying binding affinities at different adenosine receptor subtypes (A , A , A , and A ) and also good in vivo bronchospasmolytic activity against histamine aerosol-induced asthma in guinea pigs.

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EA 575 is an ivy leaves dry extract (DER 5-7.5:1, 30% ethanol) used against diseases of the lower respiratory tract associated with productive cough. EA 575 improves symptoms associated with chronic inflammatory bronchial conditions.

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Is Myrtol® Standardized a New Alternative toward Antibiotics?

Pharmacogn Rev

January 2016

Department of Pulmonary Diseases, Klinikum Kassel, University Hospital of Southampton, Mönchebergstrasse 41-43, D-35125 Kassel, Germany.

GeloMyrtol and GeloMyrtol forte, also known as Myrtol standardized, is an herbal medical product (phytomedicine) obtained by a multistep distillation procedure from essential oils. The major biological marker of and activity of Myrtol standardized is the monoterpenes, d-limonene, 1,8-cineole, and alpha-pinene. Myrtol standardized is estimated to have antioxidative, anti-inflammatory, and antibacterial potential while many studies confirmed its secretolytic and bronchospasmolytic effects.

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