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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.


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.


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.


Functional PDF Signaling in the Drosophila Circadian Neural Circuit Is Gated by Ral A-Dependent Modulation.

Klose M, Duvall L, Li W, Liang X, Ren C, Steinbach JH, Taghert PH.

Neuron. 2016 May 18;90(4):781-794. doi: 10.1016/j.neuron.2016.04.002. Epub 2016 May 5.


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.


Potentiation of Neuronal Nicotinic Receptors by 17β-Estradiol: Roles of the Carboxy-Terminal and the Amino-Terminal Extracellular Domains.

Jin X, Steinbach JH.

PLoS One. 2015 Dec 18;10(12):e0144631. doi: 10.1371/journal.pone.0144631. eCollection 2015.


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.


Functional characterization improves associations between rare non-synonymous variants in CHRNB4 and smoking behavior.

Haller G, Li P, Esch C, Hsu S, Goate AM, Steinbach JH.

PLoS One. 2014 May 7;9(5):e96753. doi: 10.1371/journal.pone.0096753. eCollection 2014. Erratum in: PLoS One. 2014;9(6):e99748.


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.


Cis-regulatory variants affect CHRNA5 mRNA expression in populations of African and European ancestry.

Wang JC, Spiegel N, Bertelsen S, Le N, McKenna N, Budde JP, Harari O, Kapoor M, Brooks A, Hancock D, Tischfield J, Foroud T, Bierut LJ, Steinbach JH, Edenberg HJ, Traynor BJ, Goate AM.

PLoS One. 2013 Nov 26;8(11):e80204. doi: 10.1371/journal.pone.0080204. eCollection 2013.


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.


The nicotinic α5 subunit can replace either an acetylcholine-binding or nonbinding subunit in the α4β2* neuronal nicotinic receptor.

Jin X, Bermudez I, Steinbach JH.

Mol Pharmacol. 2014 Jan;85(1):11-7. doi: 10.1124/mol.113.089979. Epub 2013 Nov 1.


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.


Neurosteroid analog photolabeling of a site in the third transmembrane domain of the β3 subunit of the GABA(A) receptor.

Chen ZW, Manion B, Townsend RR, Reichert DE, Covey DF, Steinbach JH, Sieghart W, Fuchs K, Evers AS.

Mol Pharmacol. 2012 Sep;82(3):408-19. doi: 10.1124/mol.112.078410. Epub 2012 May 30.


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.


Neurosteroid analogues. 17. Inverted binding orientations of androsterone enantiomers at the steroid potentiation site on γ-aminobutyric acid type A receptors.

Krishnan K, Manion BD, Taylor A, Bracamontes J, Steinbach JH, Reichert DE, Evers AS, Zorumski CF, Mennerick S, Covey DF.

J Med Chem. 2012 Feb 9;55(3):1334-45. doi: 10.1021/jm2014925. Epub 2012 Jan 18.


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.


Common polymorphisms in FMO1 are associated with nicotine dependence.

Hinrichs AL, Murphy SE, Wang JC, Saccone S, Saccone N, Steinbach JH, Goate A, Stevens VL, Bierut LJ.

Pharmacogenet Genomics. 2011 Jul;21(7):397-402. doi: 10.1097/FPC.0b013e328346886f.


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.


A portable site: a binding element for 17β-estradiol can be placed on any subunit of a nicotinic α4β2 receptor.

Jin X, Steinbach JH.

J Neurosci. 2011 Mar 30;31(13):5045-54. doi: 10.1523/JNEUROSCI.4802-10.2011.


Flapping loops: roles for hinges in a ligand-binding domain of the nicotinic receptor.

Steinbach JH.

Mol Pharmacol. 2011 Mar;79(3):337-9. doi: 10.1124/mol.110.070102. Epub 2010 Dec 20.


Uncovering hidden variance: pair-wise SNP analysis accounts for additional variance in nicotine dependence.

Culverhouse RC, Saccone NL, Stitzel JA, Wang JC, Steinbach JH, Goate AM, Schwantes-An TH, Grucza RA, Stevens VL, Bierut LJ.

Hum Genet. 2011 Feb;129(2):177-88. doi: 10.1007/s00439-010-0911-7. Epub 2010 Nov 16.


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.


The neuronal nicotinic alpha4beta2 receptor has a high maximal probability of being open.

Li P, Steinbach JH.

Br J Pharmacol. 2010 Aug;160(8):1906-15. doi: 10.1111/j.1476-5381.2010.00761.x.


Structurally diverse amphiphiles exhibit biphasic modulation of GABAA receptors: similarities and differences with neurosteroid actions.

Chisari M, Shu HJ, Taylor A, Steinbach JH, Zorumski CF, Mennerick S.

Br J Pharmacol. 2010 May;160(1):130-41. doi: 10.1111/j.1476-5381.2010.00679.x.


A synthetic 18-norsteroid distinguishes between two neuroactive steroid binding sites on GABAA receptors.

Evers AS, Chen ZW, Manion BD, Han M, Jiang X, Darbandi-Tonkabon R, Kable T, Bracamontes J, Zorumski CF, Mennerick S, Steinbach JH, Covey DF.

J Pharmacol Exp Ther. 2010 May;333(2):404-13. doi: 10.1124/jpet.109.164079. Epub 2010 Feb 2.


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.


Inhibition of muscle acetylcholine receptors by nondepolarizing drugs: humans are not unique.

Dilger JP, Steinbach JH.

Anesthesiology. 2010 Jan;112(1):247-9; author reply 249-50. doi: 10.1097/ALN.0b013e3181c5dbbc. No abstract available.


The CHRNA5-CHRNA3-CHRNB4 nicotinic receptor subunit gene cluster affects risk for nicotine dependence in African-Americans and in European-Americans.

Saccone NL, Wang JC, Breslau N, Johnson EO, Hatsukami D, Saccone SF, Grucza RA, Sun L, Duan W, Budde J, Culverhouse RC, Fox L, Hinrichs AL, Steinbach JH, Wu M, Rice JP, Goate AM, Bierut LJ.

Cancer Res. 2009 Sep 1;69(17):6848-56. doi: 10.1158/0008-5472.CAN-09-0786. Epub 2009 Aug 25.


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.


Photoaffinity labeling the agonist binding domain of alpha4beta4 and alpha4beta2 neuronal nicotinic acetylcholine receptors with [(125)I]epibatidine and 5[(125)I]A-85380.

Hamouda AK, Jin X, Sanghvi M, Srivastava S, Pandhare A, Duddempudi PK, Steinbach JH, Blanton MP.

Biochim Biophys Acta. 2009 Sep;1788(9):1987-95. doi: 10.1016/j.bbamem.2009.06.012. Epub 2009 Jun 21.


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.


Risk for nicotine dependence and lung cancer is conferred by mRNA expression levels and amino acid change in CHRNA5.

Wang JC, Cruchaga C, Saccone NL, Bertelsen S, Liu P, Budde JP, Duan W, Fox L, Grucza RA, Kern J, Mayo K, Reyes O, Rice J, Saccone SF, Spiegel N, Steinbach JH, Stitzel JA, Anderson MW, You M, Stevens VL, Bierut LJ, Goate AM; COGEND collaborators and GELCC collaborators.

Hum Mol Genet. 2009 Aug 15;18(16):3125-35. doi: 10.1093/hmg/ddp231. Epub 2009 May 14.


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.


Steroid interaction with a single potentiating site is sufficient to modulate GABA-A receptor function.

Bracamontes JR, Steinbach JH.

Mol Pharmacol. 2009 Apr;75(4):973-81. doi: 10.1124/mol.108.053629. Epub 2009 Jan 28.

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