Biopolym. Cell. 1999; 15(1):23-27.
http://dx.doi.org/10.7124/bc.000501
Structure and Function of Biopolymers
Search for the most common properties of extracellular receptors agonists and antagonists in the in vitro transcription as the model
1Prokopenko V. V., 1Kholodovych V. V., 1Luik A. I.
  1. Institute of Bioorganic Chemistry and Petrochemistry, NAS of Ukraine
    1, Murmans'ka Str., Kyiv, Ukraine, 02094

Abstract

To search the most common properties of exiraeellular receptors agonists and antagonists the study of their action on the bade riophage T7 RNA-polymerase in vitro transcription was undertaken. Propranolol (β-adrenoceptors antagonist), prazusin (α 1adrenoceptors antagonist), yohimbine, (α2-adrenoceptors antagonist), airopine (muscarinic antagonist), isoproterenol (β-adreno-ceptors agonist), phenylephrine (aradrenoceptors agonist), clonidine (α2-adrenoceptors agonist), carbochol (muscarinic agonist) and synthetical tripeptide fMLP (polymorphonuclear leucocytes chemotaxrs receptors agonist) were studied. It was shown that agonists at the concentration of 10–5 –10–4 M either do not affect transcription or elevate its activity as much as 8–21 %. Antagonists at the same concentrations inhibit the polymerase reaction making it 15–45 % less active. The structural differences of the agonists and antagonists are discussed.
Full text: (PDF, in Russian)

References

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