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.
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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.
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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.
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