Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 83


Multiple functional neurosteroid binding sites on GABAA receptors.

Chen ZW, Bracamontes JR, Budelier MM, Germann AL, Shin DJ, Kathiresan K, Qian MX, Manion B, Cheng WWL, Reichert DE, Akk G, Covey DF, Evers AS.

PLoS Biol. 2019 Mar 7;17(3):e3000157. doi: 10.1371/journal.pbio.3000157. eCollection 2019 Mar.


Application of the Co-Agonist Concerted Transition Model to Analysis of GABAA Receptor Properties.

Germann AL, Steinbach JH, Akk G.

Curr Neuropharmacol. 2018 Dec 5. doi: 10.2174/1570159X17666181206092418. [Epub ahead of print]


Analysis of GABAA Receptor Activation by Combinations of Agonists Acting at the Same or Distinct Binding Sites.

Shin DJ, Germann AL, Covey DF, Steinbach JH, Akk G.

Mol Pharmacol. 2019 Jan;95(1):70-81. doi: 10.1124/mol.118.113464. Epub 2018 Oct 18.


Applying the Monod-Wyman-Changeux Allosteric Activation Model to Pseudo-Steady-State Responses from GABAA Receptors.

Steinbach JH, Akk G.

Mol Pharmacol. 2019 Jan;95(1):106-119. doi: 10.1124/mol.118.113787. Epub 2018 Oct 17.


Chemogenetic Isolation Reveals Synaptic Contribution of δ GABAA Receptors in Mouse Dentate Granule Neurons.

Sun MY, Shu HJ, Benz A, Bracamontes J, Akk G, Zorumski CF, Steinbach JH, Mennerick SJ.

J Neurosci. 2018 Sep 19;38(38):8128-8145. doi: 10.1523/JNEUROSCI.0799-18.2018. Epub 2018 Aug 3.


Enhanced GABAergic actions resulting from the coapplication of the steroid 3α-hydroxy-5α-pregnane-11,20-dione (alfaxalone) with propofol or diazepam.

Cao LQ, Montana MC, Germann AL, Shin DJ, Chakrabarti S, Mennerick S, Yuede CM, Wozniak DF, Evers AS, Akk G.

Sci Rep. 2018 Jul 9;8(1):10341. doi: 10.1038/s41598-018-28754-7.


High Constitutive Activity Accounts for the Combination of Enhanced Direct Activation and Reduced Potentiation in Mutated GABAA Receptors.

Germann AL, Shin DJ, Kuhrau CR, Johnson AD, Evers AS, Akk G.

Mol Pharmacol. 2018 May;93(5):468-476. doi: 10.1124/mol.117.111435. Epub 2018 Feb 8.


Mapping two neurosteroid-modulatory sites in the prototypic pentameric ligand-gated ion channel GLIC.

Cheng WWL, Chen ZW, Bracamontes JR, Budelier MM, Krishnan K, Shin DJ, Wang C, Jiang X, Covey DF, Akk G, Evers AS.

J Biol Chem. 2018 Feb 23;293(8):3013-3027. doi: 10.1074/jbc.RA117.000359. Epub 2018 Jan 4.


Propofol Is an Allosteric Agonist with Multiple Binding Sites on Concatemeric Ternary GABAA Receptors.

Shin DJ, Germann AL, Johnson AD, Forman SA, Steinbach JH, Akk G.

Mol Pharmacol. 2018 Feb;93(2):178-189. doi: 10.1124/mol.117.110403. Epub 2017 Nov 30.


GABA Type A Receptor Activation in the Allosteric Coagonist Model Framework: Relationship between EC50 and Basal Activity.

Akk G, Shin DJ, Germann AL, Steinbach JH.

Mol Pharmacol. 2018 Feb;93(2):90-100. doi: 10.1124/mol.117.110569. Epub 2017 Nov 17.


The Actions of Drug Combinations on the GABAA Receptor Manifest as Curvilinear Isoboles of Additivity.

Shin DJ, Germann AL, Steinbach JH, Akk G.

Mol Pharmacol. 2017 Nov;92(5):556-563. doi: 10.1124/mol.117.109595. Epub 2017 Aug 8.


Determination of the Residues in the Extracellular Domain of the Nicotinic α Subunit Required for the Actions of Physostigmine on Neuronal Nicotinic Receptors.

Jin X, Germann AL, Shin DJ, Akk G, Steinbach JH.

Mol Pharmacol. 2017 Sep;92(3):318-326. doi: 10.1124/mol.117.108894. Epub 2017 Jun 19.


Nicotine dependence is associated with functional variation in FMO3, an enzyme that metabolizes nicotine in the brain.

Teitelbaum AM, Murphy SE, Akk G, Baker TB, Germann A, von Weymarn LB, Bierut LJ, Goate A, Kharasch ED, Bloom AJ.

Pharmacogenomics J. 2018 Jan;18(1):136-143. doi: 10.1038/tpj.2016.92. Epub 2017 Mar 14.


The E Loop of the Transmitter Binding Site Is a Key Determinant of the Modulatory Effects of Physostigmine on Neuronal Nicotinic α4β2 Receptors.

Jin X, McCollum MM, Germann AL, Akk G, Steinbach JH.

Mol Pharmacol. 2017 Feb;91(2):100-109. doi: 10.1124/mol.116.106484. Epub 2016 Nov 28.


Activation and modulation of recombinant glycine and GABAA receptors by 4-halogenated analogues of propofol.

Germann AL, Shin DJ, Manion BD, Edge CJ, Smith EH, Franks NP, Evers AS, Akk G.

Br J Pharmacol. 2016 Nov;173(21):3110-3120. doi: 10.1111/bph.13566. Epub 2016 Sep 6.


Introduced Amino Terminal Epitopes Can Reduce Surface Expression of Neuronal Nicotinic Receptors.

Bracamontes JR, Akk G, Steinbach JH.

PLoS One. 2016 Mar 10;11(3):e0151071. doi: 10.1371/journal.pone.0151071. eCollection 2016.


Multiple Non-Equivalent Interfaces Mediate Direct Activation of GABAA Receptors by Propofol.

Eaton MM, Germann AL, Arora R, Cao LQ, Gao X, Shin DJ, Wu A, Chiara DC, Cohen JB, Steinbach JH, Evers AS, Akk G.

Curr Neuropharmacol. 2016;14(7):772-80. Review.


Comparison of Steroid Modulation of Spontaneous Inhibitory Postsynaptic Currents in Cultured Hippocampal Neurons and Steady-State Single-Channel Currents from Heterologously Expressed α1β2γ2L GABA(A) Receptors.

Chakrabarti S, Qian M, Krishnan K, Covey DF, Mennerick S, Akk G.

Mol Pharmacol. 2016 Apr;89(4):399-406. doi: 10.1124/mol.115.102202. Epub 2016 Jan 14.


Mutational Analysis of the Putative High-Affinity Propofol Binding Site in Human β3 Homomeric GABAA Receptors.

Eaton MM, Cao LQ, Chen Z, Franks NP, Evers AS, Akk G.

Mol Pharmacol. 2015 Oct;88(4):736-45. doi: 10.1124/mol.115.100347. Epub 2015 Jul 23.


Synaptic-type α1β2γ2L GABAA receptors produce large persistent currents in the presence of ambient GABA and anesthetic drugs.

Li P, Akk G.

Mol Pharmacol. 2015 May;87(5):776-81. doi: 10.1124/mol.114.096453. Epub 2015 Feb 9.


γ-aminobutyric acid type A α4, β2, and δ subunits assemble to produce more than one functionally distinct receptor type.

Eaton MM, Bracamontes J, Shu HJ, Li P, Mennerick S, Steinbach JH, Akk G.

Mol Pharmacol. 2014 Dec;86(6):647-56. doi: 10.1124/mol.114.094813. Epub 2014 Sep 19.


The neurosteroid 5β-pregnan-3α-ol-20-one enhances actions of etomidate as a positive allosteric modulator of α1β2γ2L GABAA receptors.

Li P, Bracamontes JR, Manion BD, Mennerick S, Steinbach JH, Evers AS, Akk G.

Br J Pharmacol. 2014 Dec;171(23):5446-57. doi: 10.1111/bph.12861.


11-trifluoromethyl-phenyldiazirinyl neurosteroid analogues: potent general anesthetics and photolabeling reagents for GABAA receptors.

Chen ZW, Wang C, Krishnan K, Manion BD, Hastings R, Bracamontes J, Taylor A, Eaton MM, Zorumski CF, Steinbach JH, Akk G, Mennerick S, Covey DF, Evers AS.

Psychopharmacology (Berl). 2014 Sep;231(17):3479-91. doi: 10.1007/s00213-014-3568-4. Epub 2014 Apr 23.


Mutations in the main cytoplasmic loop of the GABA(A) receptor α4 and δ subunits have opposite effects on surface expression.

Bracamontes JR, Li P, Akk G, Steinbach JH.

Mol Pharmacol. 2014 Jul;86(1):20-7. doi: 10.1124/mol.114.092791. Epub 2014 Apr 10.


Neurosteroid analogues. 18. Structure-activity studies of ent-steroid potentiators of γ-aminobutyric acid type A receptors and comparison of their activities with those of alphaxalone and allopregnanolone.

Qian M, Krishnan K, Kudova E, Li P, Manion BD, Taylor A, Elias G, Akk G, Evers AS, Zorumski CF, Mennerick S, Covey DF.

J Med Chem. 2014 Jan 9;57(1):171-90. doi: 10.1021/jm401577c. Epub 2013 Dec 24.


Modulation of the human ρ1 GABAA receptor by inhibitory steroids.

Eaton MM, Lim YB, Covey DF, Akk G.

Psychopharmacology (Berl). 2014 Sep;231(17):3467-78. doi: 10.1007/s00213-013-3379-z. Epub 2013 Dec 7.


Energetic contributions to channel gating of residues in the muscle nicotinic receptor β1 subunit.

Akk G, Eaton M, Li P, Zheng S, Lo J, Steinbach JH.

PLoS One. 2013 Oct 23;8(10):e78539. doi: 10.1371/journal.pone.0078539. eCollection 2013.


A neurosteroid potentiation site can be moved among GABAA receptor subunits.

Bracamontes JR, Li P, Akk G, Steinbach JH.

J Physiol. 2012 Nov 15;590(22):5739-47. doi: 10.1113/jphysiol.2012.237255. Epub 2012 Sep 17.


Impact of human D398N single nucleotide polymorphism on intracellular calcium response mediated by α3β4α5 nicotinic acetylcholine receptors.

Tammimäki A, Herder P, Li P, Esch C, Laughlin JR, Akk G, Stitzel JA.

Neuropharmacology. 2012 Nov;63(6):1002-11. doi: 10.1016/j.neuropharm.2012.07.022. Epub 2012 Jul 20.


Agonist-specific conformational changes in the α1-γ2 subunit interface of the GABA A receptor.

Eaton MM, Lim YB, Bracamontes J, Steinbach JH, Akk G.

Mol Pharmacol. 2012 Aug;82(2):255-63. doi: 10.1124/mol.112.077875. Epub 2012 May 9.


Rare missense variants in CHRNB4 are associated with reduced risk of nicotine dependence.

Haller G, Druley T, Vallania FL, Mitra RD, Li P, Akk G, Steinbach JH, Breslau N, Johnson E, Hatsukami D, Stitzel J, Bierut LJ, Goate AM.

Hum Mol Genet. 2012 Feb 1;21(3):647-55. doi: 10.1093/hmg/ddr498. Epub 2011 Oct 31.


Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes.

Shu HJ, Bracamontes J, Taylor A, Wu K, Eaton MM, Akk G, Manion B, Evers AS, Krishnan K, Covey DF, Zorumski CF, Steinbach JH, Mennerick S.

Br J Pharmacol. 2012 Apr;165(7):2228-43. doi: 10.1111/j.1476-5381.2011.01690.x.


Use of concatemers of ligand-gated ion channel subunits to study mechanisms of steroid potentiation.

Steinbach JH, Akk G.

Anesthesiology. 2011 Dec;115(6):1328-37. doi: 10.1097/ALN.0b013e318233046a. Review.


Structural studies of the actions of anesthetic drugs on the γ-aminobutyric acid type A receptor.

Akk G, Steinbach JH.

Anesthesiology. 2011 Dec;115(6):1338-48. doi: 10.1097/ALN.0b013e3182315d93. Review.


Functional characterization of the α5(Asn398) variant associated with risk for nicotine dependence in the α3β4α5 nicotinic receptor.

Li P, McCollum M, Bracamontes J, Steinbach JH, Akk G.

Mol Pharmacol. 2011 Nov;80(5):818-27. doi: 10.1124/mol.111.073841. Epub 2011 Aug 19.


Activation and modulation of human α4β2 nicotinic acetylcholine receptors by the neonicotinoids clothianidin and imidacloprid.

Li P, Ann J, Akk G.

J Neurosci Res. 2011 Aug;89(8):1295-301. doi: 10.1002/jnr.22644. Epub 2011 Apr 28.


Occupation of either site for the neurosteroid allopregnanolone potentiates the opening of the GABAA receptor induced from either transmitter binding site.

Bracamontes J, McCollum M, Esch C, Li P, Ann J, Steinbach JH, Akk G.

Mol Pharmacol. 2011 Jul;80(1):79-86. doi: 10.1124/mol.111.071662. Epub 2011 Apr 15.


Pharmacology of structural changes at the GABA(A) receptor transmitter binding site.

Akk G, Li P, Bracamontes J, Wang M, Steinbach JH.

Br J Pharmacol. 2011 Feb;162(4):840-50. doi: 10.1111/j.1476-5381.2010.01083.x.


Kinetic and structural determinants for GABA-A receptor potentiation by neuroactive steroids.

Akk G, Covey DF, Evers AS, Mennerick S, Zorumski CF, Steinbach JH.

Curr Neuropharmacol. 2010 Mar;8(1):18-25. doi: 10.2174/157015910790909458.


Molecular pharmacology of the GABA(A) receptor.

Akk G.

Curr Neuropharmacol. 2010 Mar;8(1):1. doi: 10.2174/157015910790909539. No abstract available.


Site-specific fluorescence reveals distinct structural changes induced in the human rho 1 GABA receptor by inhibitory neurosteroids.

Li P, Khatri A, Bracamontes J, Weiss DS, Steinbach JH, Akk G.

Mol Pharmacol. 2010 Apr;77(4):539-46. doi: 10.1124/mol.109.062885. Epub 2010 Jan 8.


Hydrogen bonding between the 17beta-substituent of a neurosteroid and the GABA(A) receptor is not obligatory for channel potentiation.

Li P, Bandyopadhyaya AK, Covey DF, Steinbach JH, Akk G.

Br J Pharmacol. 2009 Nov;158(5):1322-9. doi: 10.1111/j.1476-5381.2009.00390.x. Epub 2009 Aug 20.


The influence of the membrane on neurosteroid actions at GABA(A) receptors.

Akk G, Covey DF, Evers AS, Steinbach JH, Zorumski CF, Mennerick S.

Psychoneuroendocrinology. 2009 Dec;34 Suppl 1:S59-66. doi: 10.1016/j.psyneuen.2009.05.020. Review.


Activation and modulation of concatemeric GABA-A receptors expressed in human embryonic kidney cells.

Akk G, Li P, Bracamontes J, Steinbach JH.

Mol Pharmacol. 2009 Jun;75(6):1400-11. doi: 10.1124/mol.108.054510. Epub 2009 Mar 16.


The insecticide fipronil and its metabolite fipronil sulphone inhibit the rat alpha1beta2gamma2L GABA(A) receptor.

Li P, Akk G.

Br J Pharmacol. 2008 Nov;155(5):783-94. doi: 10.1038/bjp.2008.309. Epub 2008 Jul 28.


Mutations of the GABA-A receptor alpha1 subunit M1 domain reveal unexpected complexity for modulation by neuroactive steroids.

Akk G, Li P, Bracamontes J, Reichert DE, Covey DF, Steinbach JH.

Mol Pharmacol. 2008 Sep;74(3):614-27. doi: 10.1124/mol.108.048520. Epub 2008 Jun 10.


Activation and block of the adult muscle-type nicotinic receptor by physostigmine: single-channel studies.

Militante J, Ma BW, Akk G, Steinbach JH.

Mol Pharmacol. 2008 Sep;74(3):764-76. doi: 10.1124/mol.108.047134. Epub 2008 Jun 3.


Neurosteroid analogues. 14. Alternative ring system scaffolds: GABA modulatory and anesthetic actions of cyclopenta[b]phenanthrenes and cyclopenta[b]anthracenes.

Scaglione JB, Jastrzebska I, Krishnan K, Li P, Akk G, Manion BD, Benz A, Taylor A, Rath NP, Evers AS, Zorumski CF, Mennerick S, Covey DF.

J Med Chem. 2008 Mar 13;51(5):1309-18. doi: 10.1021/jm701128r. Epub 2008 Feb 15.


Actions of anesthetics on excitatory transmitter-gated channels.

Akk G, Mennerick S, Steinbach JH.

Handb Exp Pharmacol. 2008;(182):53-84. doi: 10.1007/978-3-540-74806-9_3. Review.


Supplemental Content

Support Center