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Items: 1 to 50 of 164

1.

Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators.

Jakubík J, Randáková A, El-Fakahany EE, Doležal V.

PLoS One. 2019 Mar 27;14(3):e0214255. doi: 10.1371/journal.pone.0214255. eCollection 2019.

2.

Applications and limitations of fitting of the operational model to determine relative efficacies of agonists.

Jakubík J, Randáková A, Rudajev V, Zimčík P, El-Fakahany EE, Doležal V.

Sci Rep. 2019 Mar 15;9(1):4637. doi: 10.1038/s41598-019-40993-w.

3.

Role of membrane cholesterol in differential sensitivity of muscarinic receptor subtypes to persistently bound xanomeline.

Randáková A, Dolejší E, Rudajev V, Zimčík P, Doležal V, El-Fakahany EE, Jakubík J.

Neuropharmacology. 2018 May 1;133:129-144. doi: 10.1016/j.neuropharm.2018.01.027.

4.

Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors.

Jakubík J, Randáková A, Zimčík P, El-Fakahany EE, Doležal V.

Sci Rep. 2017 Jan 16;7:40381. doi: 10.1038/srep40381.

5.

Lipid-Based Diets Improve Muscarinic Neurotransmission in the Hippocampus of Transgenic APPswe/PS1dE9 Mice.

Janickova H, Rudajev V, Dolejsi E, Koivisto H, Jakubik J, Tanila H, El-Fakahany EE, Dolezal V.

Curr Alzheimer Res. 2015;12(10):923-31.

PMID:
26502816
6.

Towards predictive docking at aminergic G-protein coupled receptors.

Jakubík J, El-Fakahany EE, Doležal V.

J Mol Model. 2015 Nov;21(11):284. doi: 10.1007/s00894-015-2824-9. Epub 2015 Oct 9.

PMID:
26453085
7.

Classical and atypical agonists activate M1 muscarinic acetylcholine receptors through common mechanisms.

Randáková A, Dolejší E, Rudajev V, Zimčík P, Doležal V, El-Fakahany EE, Jakubík J.

Pharmacol Res. 2015 Jul;97:27-39. doi: 10.1016/j.phrs.2015.04.002. Epub 2015 Apr 13.

8.

Molecular mechanisms of methoctramine binding and selectivity at muscarinic acetylcholine receptors.

Jakubík J, Zimčík P, Randáková A, Fuksová K, El-Fakahany EE, Doležal V.

Mol Pharmacol. 2014 Aug;86(2):180-92. doi: 10.1124/mol.114.093310. Epub 2014 May 28.

PMID:
24870405
9.

Changes in Membrane Cholesterol Differentially Influence Preferential and Non-preferential Signaling of the M1 and M3 Muscarinic Acetylcholine Receptors.

Michal P, El-Fakahany EE, Doležal V.

Neurochem Res. 2015 Oct;40(10):2068-77. doi: 10.1007/s11064-014-1325-z. Epub 2014 May 13.

10.

Outline of therapeutic interventions with muscarinic receptor-mediated transmission.

Jakubík J, Šantrůčková E, Randáková A, Janíčková H, Zimčík P, Rudajev V, Michal P, El-Fakahany EE, Doležal V.

Physiol Res. 2014;63 Suppl 1:S177-89. Review.

11.

Long-term activation upon brief exposure to xanomleline is unique to M1 and M4 subtypes of muscarinic acetylcholine receptors.

Šantrůčková E, Doležal V, El-Fakahany EE, Jakubík J.

PLoS One. 2014 Feb 18;9(2):e88910. doi: 10.1371/journal.pone.0088910. eCollection 2014.

12.

Uncoupling of M1 muscarinic receptor/G-protein interaction by amyloid β(1-42).

Janíčková H, Rudajev V, Zimčík P, Jakubík J, Tanila H, El-Fakahany EE, Doležal V.

Neuropharmacology. 2013 Apr;67:272-83. doi: 10.1016/j.neuropharm.2012.11.014. Epub 2012 Nov 30.

13.

Subtype differences in pre-coupling of muscarinic acetylcholine receptors.

Jakubík J, Janíčková H, Randáková A, El-Fakahany EE, Doležal V.

PLoS One. 2011;6(11):e27732. doi: 10.1371/journal.pone.0027732. Epub 2011 Nov 16.

14.

Pharmacological evaluation of the long-term effects of xanomeline on the M(1) muscarinic acetylcholine receptor.

Grant MK, Noetzel MJ, De Lorme KC, Jakubík J, Doležal V, El-Fakahany EE.

PLoS One. 2010 Dec 23;5(12):e15722. doi: 10.1371/journal.pone.0015722.

15.

Negative cooperativity in binding of muscarinic receptor agonists and GDP as a measure of agonist efficacy.

Jakubík J, Janíčková H, El-Fakahany EE, Doležal V.

Br J Pharmacol. 2011 Mar;162(5):1029-44. doi: 10.1111/j.1476-5381.2010.01081.x.

16.

Allosteric Modulation of Muscarinic Acetylcholine Receptors.

Jakubík J, El-Fakahany EE.

Pharmaceuticals (Basel). 2010 Aug 30;3(9):2838-2860. Review.

17.

Divergence of allosteric effects of rapacuronium on binding and function of muscarinic receptors.

Jakubík J, Randáková A, El-Fakahany EE, Dolezal V.

BMC Pharmacol. 2009 Dec 28;9:15. doi: 10.1186/1471-2210-9-15.

18.

M2, M3, and M4 muscarinic receptors are expressed in the guinea pig gallbladder.

Cabadak H, Cuadra AE, El-Fakahany EE, Kan B.

J Recept Signal Transduct Res. 2009;29(1):63-6. doi: 10.1080/10799890802687416.

PMID:
19519171
19.

Mechanisms of M3 muscarinic receptor regulation by wash-resistant xanomeline binding.

Noetzel MJ, Grant MK, El-Fakahany EE.

Pharmacology. 2009;83(5):301-17. doi: 10.1159/000214843. Epub 2009 Apr 28.

20.

Membrane cholesterol content influences binding properties of muscarinic M2 receptors and differentially impacts activation of second messenger pathways.

Michal P, Rudajev V, El-Fakahany EE, Dolezal V.

Eur J Pharmacol. 2009 Mar 15;606(1-3):50-60. doi: 10.1016/j.ejphar.2009.01.028. Epub 2009 Jan 29.

21.

Immediate and delayed consequences of xanomeline wash-resistant binding at the M3 muscarinic receptor.

Noetzel MJ, Grant MK, El-Fakahany EE.

Neurochem Res. 2009 Jun;34(6):1138-49. doi: 10.1007/s11064-008-9886-3. Epub 2008 Dec 12.

22.

Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.

Kane BE, Grant MK, El-Fakahany EE, Ferguson DM.

Bioorg Med Chem. 2008 Feb 1;16(3):1376-92. Epub 2007 Oct 22.

PMID:
17977730
23.

Long-term changes in the muscarinic M1 receptor induced by instantaneous formation of wash-resistant xanomeline-receptor complex.

De Lorme KC, Grant MK, Noetzel MJ, Polson SB, El-Fakahany EE.

J Pharmacol Exp Ther. 2007 Dec;323(3):868-76. Epub 2007 Sep 12.

PMID:
17855477
24.

Wash-resistantly bound xanomeline inhibits acetylcholine release by persistent activation of presynaptic M(2) and M(4) muscarinic receptors in rat brain.

Machová E, Jakubík J, El-Fakahany EE, Dolezal V.

J Pharmacol Exp Ther. 2007 Jul;322(1):316-23. Epub 2007 Apr 19.

PMID:
17446301
25.

Muscarinic M2 receptors directly activate Gq/11 and Gs G-proteins.

Michal P, El-Fakahany EE, Dolezal V.

J Pharmacol Exp Ther. 2007 Feb;320(2):607-14. Epub 2006 Oct 25.

PMID:
17065363
26.

Long-term wash-resistant effects of brief interaction of xanomeline at the M1 muscarinic receptor.

De Lorme KC, Sikorski KL, Grant MK, El-Fakahany EE.

Neurosci Lett. 2006 Dec 13;410(1):11-4. Epub 2006 Oct 18.

27.

Differences in kinetics of xanomeline binding and selectivity of activation of G proteins at M(1) and M(2) muscarinic acetylcholine receptors.

Jakubík J, El-Fakahany EE, Dolezal V.

Mol Pharmacol. 2006 Aug;70(2):656-66. Epub 2006 May 4.

PMID:
16675658
28.

Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor.

Grant MK, El-Fakahany EE.

J Pharmacol Exp Ther. 2005 Oct;315(1):313-9. Epub 2005 Jul 7.

PMID:
16002459
29.

Mechanisms of M(1) muscarinic receptor-mediated up-regulation of neuronal nitric oxide synthase in N1E-115 neuroblastoma cells.

Cuadra AE, El-Fakahany EE.

Brain Res Mol Brain Res. 2005 Apr 4;134(2):198-204. Epub 2005 Jan 12.

PMID:
15836917
30.
31.

Role of receptor protein and membrane lipids in xanomeline wash-resistant binding to muscarinic M1 receptors.

Jakubík J, Tucek S, El-Fakahany EE.

J Pharmacol Exp Ther. 2004 Jan;308(1):105-10. Epub 2003 Oct 20.

PMID:
14569060
33.

Endogenous expression of nNOS protein in several neuronal cell lines.

Grant MK, Cuadra AE, El-Fakahany EE.

Life Sci. 2002 Jul 5;71(7):813-7.

PMID:
12074940
34.
35.

Microglial derived nitric oxide decreases serotonin content in rat basophilic leukemia (RBL-2H3) cells.

Linden DR, El-Fakahany EE.

Eur J Pharmacol. 2002 Feb 1;436(1-2):53-6.

PMID:
11834246
36.

Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.

Christopoulos A, Grant MK, Ayoubzadeh N, Kim ON, Sauerberg P, Jeppesen L, El-Fakahany EE.

J Pharmacol Exp Ther. 2001 Sep;298(3):1260-8.

PMID:
11504829
37.

The role of nitric oxide in development of topographic precision in the retinotectal projection of chick.

Wu HH, Selski DJ, El-Fakahany EE, McLoon SC.

J Neurosci. 2001 Jun 15;21(12):4318-25.

38.

Transducer abstraction: a novel approach to the detection of partial agonist efficacy in radioligand binding studies.

Christopoulos A, Grant MK, El-Fakahany EE.

J Pharmacol Toxicol Methods. 2000 Jan-Feb;43(1):55-67.

PMID:
11091130
39.

M(2) and M(4) muscarinic receptor subtypes couple to activation of endothelial nitric oxide synthase.

Waid DK, Chell M, El-Fakahany EE.

Pharmacology. 2000 Jul;61(1):37-42.

PMID:
10895079
40.

Prenatal viral infection causes alterations in nNOS expression in developing mouse brains.

Fatemi SH, Cuadra AE, El-Fakahany EE, Sidwell RW, Thuras P.

Neuroreport. 2000 May 15;11(7):1493-6.

PMID:
10841364
41.

Neurokinin(3) receptors couple to the activation of neuronal nitric-oxide synthase in stably transfected Chinese hamster ovary cells.

Linden DR, Chell MJ, El-Fakahany EE, Seybold VS.

J Pharmacol Exp Ther. 2000 May;293(2):559-68.

PMID:
10773029
42.

Evidence for a tandem two-site model of ligand binding to muscarinic acetylcholine receptors.

Jakubik J, El-Fakahany EE, Tucek S.

J Biol Chem. 2000 Jun 23;275(25):18836-44.

43.
44.

Further evidence for the heterogeneity of functional muscarinic receptors in guinea pig gallbladder.

Akici A, Karaalp A, Iskender E, Christopoulos A, El-Fakahany EE, Oktay S.

Eur J Pharmacol. 2000 Jan 24;388(1):115-23.

PMID:
10657554
45.

The assessment of antagonist potency under conditions of transient response kinetics.

Christopoulos A, Parsons AM, Lew MJ, El-Fakahany EE.

Eur J Pharmacol. 1999 Oct 15;382(3):217-27.

PMID:
10556673
46.

Muscarinic M(2) receptors are not primarily involved in the contraction of guinea-pig gallbladder smooth muscle.

Akici A, Karaalp A, Skender E, El-Fakahany EE, Oktay S.

Pharmacol Res. 1999 Nov;40(5):443-9.

PMID:
10527660
47.

Regulation of acetylcholine binding by ATP at the muscarinic M(1) receptor in intact CHO cells.

Grant MK, Christopoulos A, El-Fakahany EE.

Brain Res. 1999 Aug 21;839(1):94-9.

PMID:
10482803
48.

Qualitative and quantitative assessment of relative agonist efficacy.

Christopoulos A, El-Fakahany EE.

Biochem Pharmacol. 1999 Sep 1;58(5):735-48. Review.

PMID:
10449182
49.

Clozapine interaction with the M2 and M4 subtypes of muscarinic receptors.

Michal P, Lysíková M, El-Fakahany EE, Tucek S.

Eur J Pharmacol. 1999 Jul 2;376(1-2):119-25.

PMID:
10440097
50.

Pharmacological analysis of the novel mode of interaction between xanomeline and the M1 muscarinic acetylcholine receptor.

Christopoulos A, Parsons AM, El-Fakahany EE.

J Pharmacol Exp Ther. 1999 Jun;289(3):1220-8.

PMID:
10336509

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