Search for lead structures to develop new allosteric modulators of muscarinic receptors.

@article{Trnkle1996SearchFL,
  title={Search for lead structures to develop new allosteric modulators of muscarinic receptors.},
  author={Christian Tr{\"a}nkle and Evi Kostenis and Ulrike Burgmer and K. -H. Mohr},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1996},
  volume={279 2},
  pages={926-33}
}
Various compounds are known to allosterically modulate the binding of ligands to muscarinic receptors. Most of these compounds have another predominant pharmacological action. Identification of the potent representatives should be useful for the development of allosteric modulators that are specific and highly active. For various reasons, a direct comparison of allosteric potencies on the basis of literature data is difficult. Therefore, a series of compounds was compared with regard to the… CONTINUE READING

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Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Gallamine showed intermediate potency ( EC50 values of 180 nM and 16,000 nM in Na , K , Pi buffer and Mg , Tris , Cl , Pi buffer , respectively ) .
Gallamine showed intermediate potency ( EC50 values of 180 nM and 16,000 nM in Na , K , Pi buffer and Mg , Tris , Cl , Pi buffer , respectively ) .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
MagnesiumNo subtypeSodium
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
SodiumNo subtypeMagnesium
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
Therefore , a series of compounds was compared with regard to the allosteric delay of the dissociation of N-[3H]methylscopolamine from porcine heart M2 receptors under the following assay conditions : " Na , K , Pi buffer " , 4 mM Na2HPO4 , 1 mM KH2PO4 , pH 7.4 , 23 degrees C ; " Mg , Tris , Cl , Pi buffer ' , 50 mM Tris - HCl , 3 mM MgHPO4,pH 7.3 , 37 degrees C. Generally , the allosteric potency of the compounds was higher in the Na , K , Pi buffer , compared with the Mg , Tris , Cl , Pi buffer .
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