Clarke and Bond reply
Article Abstract:
The use of efficacy rank order matching in drug-screening procedures has been proposed by Dr. Gerald Zernig. The proposal has been based on the studies that the efficacy order of agonists for eliciting each of the multiple signal transduction responses from the activation of a single receptor subtype is unique. However, the capacity of ligand to elicit a response is dependent on both the intrinsic efficacy of the ligand and on the characteristics of the system under the study. Thus efficacy rank order matching can not be used in the identification of neurochemical or electrophysiological mechanisms for certain behavioral of physiological response determined in vitro.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1999
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Keeping an eye on the I site: imidazoline-preferring receptors
Article Abstract:
A nomenclature system has been assigned to facilitate the functional and biochemical study of imidazoline receptor sites. Clonidine analogs that exhibit nanomolar binding properties are classified as I1 sites while those that show micromolar binding properties and are labelled by (3H)idazoxan are classified as I2 sites. Moreover, developments in purification, selective antisera and photoaffinity probes may result in better identification of I2 sites. In addition, researches on the actions of rilmenidine and moxonidine drugs may benefit the study of the physiological functions of imidazoline receptors.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1992
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