Nonpeptide antagonists herald new era in tachykinin research

Article Abstract:

Nonpeptide tachykinin antagonists are being tested for their biologic activity on three receptor types. These may be useful in research involving physiologic responses to tachykinin because these provide a selective, stable and bioavailable antagonist. Upon testing, nonpeptide antagonists prevent interaction between substance P and specific NK receptors. The antagonist readily decreases neuronal response to noxious stimuli and mediates pain and inflammatory mechanisms. These effects may have future therapeutic use although further research is recommended.

Drugs, Testing, Tachykinins, Nociceptors

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Receptor classification using antagonists without determining pA2 values

Article Abstract:

A rapid technique of identifying receptor subtypes has been developed. The technique circumvents the problems normally encountered in determining antagonist affinity values against various agonists (pA2 values). Individual receptor binding affinities are used in conjunction with individual inhibition values to form an affinity-inhibition curve which reflects the behavior of a concentration-inhibition curve. Similar receptor subtypes feature binding affinities with a common affinity-inhibition curve relative to a particular functional inhibition.

Research, Muscarinic receptors, Muscarinic antagonists, Drug receptors, Chemical affinity

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Nonpeptide angiotensin II receptor antagonists

Article Abstract:

DuP753 is a specific nonpeptide angiotensin II receptor antagonist that has proven effective in regulating the renin-angiotensin system. This compound, which features a tetrazol-5-yl aromatic carboxylic acid, competitively blocks the activity of angiotensin II. The presence of the carboxylic acid unit ensures the potency of the compound even during oral administration. Moreover, the physiological effect of angiotensin II and the diversity of angiotensin II receptors have been identified using the nonpeptide angiotensin II inhibitors.

ACE inhibitors, Angiotensin converting enzyme inhibitors, Angiotensin, Angiotensin receptors, Renin-angiotensin system

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