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G protein-coupled receptor allosterism and complexing.
Christopoulos A, Kenakin T. Christopoulos A, et al. Pharmacol Rev. 2002 Jun;54(2):323-74. doi: 10.1124/pr.54.2.323. Pharmacol Rev. 2002. PMID: 12037145 Review.
Allosteric sites on GPCRs represent novel drug targets because allosteric modulators possess a number of theoretical advantages over classic orthosteric ligands, such as a ceiling level to the allosteric effect and a potential for greater GPCR subtype-selecti …
Allosteric sites on GPCRs represent novel drug targets because allosteric modulators possess a number of theoretical advantages over …
[3H]N-methylscopolamine dissociation from muscarine receptors affected by low concentrations of allosteric modulators.
Christopoulos A, Mitchelson F. Christopoulos A, et al. Eur J Pharmacol. 1995 Aug 15;290(3):259-62. doi: 10.1016/0922-4106(95)90002-0. Eur J Pharmacol. 1995. PMID: 7589221
Gallamine, at a concentration approximating its KD value, slowed the dissociation of [3H]N-methylscopolamine in the presence of ca. 30 x KD of both unlabelled NMS or atropine. ...
Gallamine, at a concentration approximating its KD value, slowed the dissociation of [3H]N-methylscopolamine in the presence of ca. 3 …
Assessment of the allosteric interactions of the bisquaternary heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at M1 and M2 muscarine receptors.
Christopoulos A, Mitchelson F. Christopoulos A, et al. Mol Pharmacol. 1994 Jul;46(1):105-14. Mol Pharmacol. 1994. PMID: 8058045
Cooperativity factors for the interaction of C7/3-phth with other antagonists were obtained by fitting the data to a theoretical model for interaction between an agonist, a competitive antagonist, and an allosteric antagonist. The values obtained indicate that C7/3- …
Cooperativity factors for the interaction of C7/3-phth with other antagonists were obtained by fitting the data to a theoretical mode …
Binding of the muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at cholinoceptor sites.
Christopoulos A, Loiacono R, Mitchelson F. Christopoulos A, et al. Eur J Pharmacol. 1993 Jun 15;246(1):1-8. doi: 10.1016/0922-4106(93)90002-q. Eur J Pharmacol. 1993. PMID: 8354340
The binding of the bisquaternary muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)-ammonium bromide (C7/3-phth) was investigated at a number of cholinergic binding sites using (-)-[3H]nicotine, [3H]pirenzepine and (-)-[3H]quinuclidinyl benzilate …
The binding of the bisquaternary muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)-ammonium bromide (C7/3-phth) w …
Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure.
Christopoulos A, Lanzafame A, Ziegler A, Mitchelson F. Christopoulos A, et al. Biochem Pharmacol. 1997 Mar 21;53(6):795-800. doi: 10.1016/s0006-2952(96)00814-3. Biochem Pharmacol. 1997. PMID: 9113100
The dissociation rate for [3H]NMS, initiated by diluting the incubation mixture in a 100-fold volume of buffer, was 0.61 +/- 0.10 min-1. ...In contrast, gallamine and the bisquaternary, heptane-1,7-bis-(dimethyl-3'-phthalimidopropyl-ammonium bromide) (C7/3'-phth), produced …
The dissociation rate for [3H]NMS, initiated by diluting the incubation mixture in a 100-fold volume of buffer, was 0.61 +/- 0.10 min …
Three allosteric modulators act at a common site, distinct from that of competitive antagonists, at muscarinic acetylcholine M2 receptors.
Lanzafame A, Christopoulos A, Mitchelson F. Lanzafame A, et al. J Pharmacol Exp Ther. 1997 Jul;282(1):278-85. J Pharmacol Exp Ther. 1997. PMID: 9223565
Functional studies were conducted on guinea pig atrial muscarinic acetylcholine M2 receptors with the allosteric modulators heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide (C7/3'-phth), gallamine and alcuronium to determine whether these ligands are able to recogni …
Functional studies were conducted on guinea pig atrial muscarinic acetylcholine M2 receptors with the allosteric modulators heptane-1,7-bis( …
Application of an allosteric ternary complex model to the technique of pharmacological resultant analysis.
Christopoulos A, Mitchelson F. Christopoulos A, et al. J Pharm Pharmacol. 1997 Aug;49(8):781-6. doi: 10.1111/j.2042-7158.1997.tb06112.x. J Pharm Pharmacol. 1997. PMID: 9379356
A simple ternary complex model of drug-receptor interaction has been used to extend the procedure of pharmacological resultant analysis, enabling the quantitation of interactions between allosteric modulators and orthosteric antagonists. ...
A simple ternary complex model of drug-receptor interaction has been used to extend the procedure of pharmacological resultant analys
Pharmacological analysis of the mode of interaction of McN-A-343 at atrial muscarinic M2 receptors.
Christopoulos A, Mitchelson F. Christopoulos A, et al. Eur J Pharmacol. 1997 Nov 27;339(2-3):153-6. doi: 10.1016/s0014-2999(97)01379-4. Eur J Pharmacol. 1997. PMID: 9473129
Following partial receptor inactivation with propylbenzylcholine mustard, the properties of McN-A-343 as an inhibitor of the carbachol-mediated responses were assessed. ...The log KB of McN-A-343 as an antagonist was - 4.65+/-0.06, and was not significantly differen …
Following partial receptor inactivation with propylbenzylcholine mustard, the properties of McN-A-343 as an inhibitor of the carbacho …
Allosteric interactions at muscarinic cholinoceptors.
Christopoulos A, Lanzafame A, Mitchelson F. Christopoulos A, et al. Clin Exp Pharmacol Physiol. 1998 Mar-Apr;25(3-4):185-94. doi: 10.1111/j.1440-1681.1998.t01-4-.x. Clin Exp Pharmacol Physiol. 1998. PMID: 9590567 Review.
An allosteric interaction occurs when the binding of a ligand to its site on a receptor is able to modify the binding of another ligand to a topographically distinct site on the same receptor and vice versa. ...Evidence has accumulated pointing to the existen …
An allosteric interaction occurs when the binding of a ligand to its site on a receptor is able to modify the binding of anoth …
Use of a spreadsheet to quantitate the equilibrium binding of an allosteric modulator.
Christopoulos A, Mitchelson F. Christopoulos A, et al. Eur J Pharmacol. 1998 Aug 14;355(1):103-11. doi: 10.1016/s0014-2999(98)00476-2. Eur J Pharmacol. 1998. PMID: 9754944
Using the program Microsoft EXCEL, a spreadsheet was developed for constrained, simultaneous analysis of multiple datasets obtained from equilibrium binding experiments, according to an allosteric model of interaction. ...
Using the program Microsoft EXCEL, a spreadsheet was developed for constrained, simultaneous analysis of multiple datasets obtained f …
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