Synthesis of Benzobicyclo[2.2.1]heptylimidazoles as Conformationally Constrained Adrenergic Receptor Antagonists

Heterocycles ◽  
2005 ◽  
Vol 65 (11) ◽  
pp. 2783 ◽  
Author(s):  
Jari Yli-Kauhaluoma ◽  
Aki Laine ◽  
Jari Ratilainen ◽  
Arto Karjalainen
Keyword(s):  
Adrenergic Receptor ◽  
Receptor Antagonists ◽  
Conformationally Constrained

Ligand and Structure Based Models for the Identification of Beta 2 Adrenergic Receptor Antagonists

2015 ◽  
Vol 11 (3) ◽  
pp. 222-236 ◽  
Author(s):  
Jayadev Joshi ◽  
Manali Dimri ◽  
Subhajit Ghosh ◽  
Nitisha Shrivastava ◽  
Rina Chakraborti ◽  
...  
Keyword(s):  
Adrenergic Receptor ◽  
Receptor Antagonists ◽  
Beta 2

scholarly journals Role of α1-adrenergic receptor subtypes in contractility of the rabbit abdominal aorta in vitro

2013 ◽  
Vol 82 (3) ◽  
pp. 331-336 ◽  
Author(s):  
Jan Gnus ◽  
Albert Czerski ◽  
Stanisław Ferenc ◽  
Wojciech Zawadzki ◽  
Wojciech Witkiewicz ◽  
...  
Keyword(s):  
Smooth Muscle ◽  
Receptor Antagonist ◽  
Abdominal Aorta ◽  
Adrenergic Receptor ◽  
Receptor Subtypes ◽  
Organ Bath ◽  
Dependent Manner ◽  
Receptor Antagonists ◽  
Selective Antagonists

Investigation of the effect of α1-adrenergic receptor subtypes on the contraction of the abdominal aorta will allow for more effective treatment of hypertension by use of selective antagonists. The aim of the study was to evaluate the participation of α1-adrenergic receptor subtypes in the contractility of the aortic smooth muscle cells in rabbits. The in vitro experiments were performed in isolated tissue preparations from 30 adult female New Zealand rabbits. The abdominal aortic sections were placed in organ bath chambers and contracted with increasing doses of non-selective α1-adrenergic receptor agonist phenylephrine without pre-incubation or after incubation in α1-adrenergic receptor subtype-selective or non-selective antagonists. Separate sections were incubated with increasing concentrations of antagonists. Phenylephrine caused maximal rise in arterial smooth muscle tone to 4.75 ± 0.47 mN. The most potent in blocking phenylephrine induced contraction was 5-metylurapidil (α1A-adrenergic receptor antagonist) followed by phentolamine and prazosin (non-selective α1-adrenergic receptor antagonists); BMY 7378 (α1D-adrenergic receptor antagonist), cyclazosin and L-765.314 (α1B-adrenergic receptor antagonists) were less effective. All antagonists, except BMY 7378 elicited relaxation of non-precontracted aorta in dose dependent manner. Our results indicate that postsynaptic α1A receptors are the most potent in producing rabbit abdominal aorta contraction, while α1B and α1D subtypes are less effective.

“Methylene Bridge” to 5-HT3 Receptor Antagonists: Conformationally Constrained Phenylguanidines

2018 ◽  
Vol 10 (3) ◽  
pp. 1380-1389 ◽  
Author(s):  
Ahmed S. Abdelkhalek ◽  
Genevieve S. Alley ◽  
Osama I. Alwassil ◽  
Shailesh Khatri ◽  
Philip D. Mosier ◽  
...  
Keyword(s):  
Receptor Antagonists ◽  
Methylene Bridge ◽  
Conformationally Constrained
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