[1]
Chua, H.C.; Chebib, M. GABAA receptors and the diversity in their structure and pharmacology. Adv. Pharmacol., 2017, 79, 1-34. [http://dx.doi.org/10.1016/bs.apha.2017.03.003]. [PMID: 28528665].
[2]
Franks, N.P. Molecular targets underlying general anaesthesia. Br. J. Pharmacol., 2006, 147(Suppl. 1), S72-S81. [http://dx.doi.org/10. 1038/sj.bjp.0706441]. [PMID: 16402123].
[3]
Akk, G.; Covey, D.F.; Evers, A.S.; Steinbach, J.H.; Zorumski, C.F.; Mennerick, S. Mechanisms of neurosteroid interactions with GABA(A) receptors. Pharmacol. Ther., 2007, 116(1), 35-57. [http:// dx.doi.org/10.1016/j.pharmthera.2007.03.004]. [PMID: 17524487].
[4]
Monod, J.; Wyman, J.; Changeux, J.P. On the nature of allosteric transitions: a plausible model. J. Mol. Biol., 1965, 12, 88-118. [http:// dx.doi.org/10.1016/S0022-2836(65)80285-6]. [PMID: 14343300].
[5]
Karlin, A. On the application of “a plausible model” of allosteric proteins to the receptor for acetylcholine. J. Theor. Biol., 1967, 16(2), 306-320. [http://dx.doi.org/10.1016/0022-5193(67)90011-2]. [PMID: 6048545].
[6]
Auerbach, A. Thinking in cycles: MWC is a good model for acetylcholine receptor-channels. J. Physiol., 2012, 590(1), 93-98. [http:// dx.doi.org/10.1113/jphysiol.2011.214684]. [PMID: 21807612].
[7]
Chang, Y.; Weiss, D.S. Allosteric activation mechanism of the α 1 β 2 γ 2 γ-aminobutyric acid type A receptor revealed by mutation of the conserved M2 leucine. Biophys. J., 1999, 77(5), 2542-2551. [http://dx.doi.org/10.1016/S0006-3495(99)77089-X]. [PMID: 10545355].
[8]
Stewart, D.; Desai, R.; Cheng, Q.; Liu, A.; Forman, S.A. Tryptophan mutations at azi-etomidate photo-incorporation sites on α1 or β2 subunits enhance GABAA receptor gating and reduce etomidate modulation. Mol. Pharmacol., 2008, 74(6), 1687-1695. [http://dx. doi.org/10.1124/mol.108.050500]. [PMID: 18805938].
[9]
Akk, G.; Shin, D.J.; Germann, A.L.; Steinbach, J.H. GABA type A receptor activation in the allosteric coagonist model framework: relationship between EC50 and basal activity. Mol. Pharmacol., 2018, 93(2), 90-100. [http://dx.doi.org/10.1124/mol.117.110569]. [PMID: 29150461].
[10]
Rüsch, D.; Forman, S.A. Classic benzodiazepines modulate the open-close equilibrium in α1β2γ2L γ-aminobutyric acid type A receptors. Anesthesiology, 2005, 102(4), 783-792. [http://dx.doi.org/ 10.1097/00000542-200504000-00014]. [PMID: 15791108].
[11]
Rüsch, D.; Zhong, H.; Forman, S.A. Gating allosterism at a single class of etomidate sites on α1β2γ2L GABA A receptors accounts for both direct activation and agonist modulation. J. Biol. Chem., 2004, 279(20), 20982-20992. [http://dx.doi.org/10.1074/jbc. M400472200]. [PMID: 15016806].
[12]
Ruesch, D.; Neumann, E.; Wulf, H.; Forman, S.A. An allosteric coagonist model for propofol effects on α1β2γ2L γ-aminobutyric acid type A receptors. Anesthesiology, 2012, 116(1), 47-55. [http:// dx.doi.org/10.1097/ALN.0b013e31823d0c36]. [PMID: 22104494].
[13]
Campo-Soria, C.; Chang, Y.; Weiss, D.S. Mechanism of action of benzodiazepines on GABAA receptors. Br. J. Pharmacol., 2006, 148(7), 984-990. [http://dx.doi.org/10.1038/sj.bjp.0706796]. [PMID: 16783415].
[14]
Eaton, M.M.; Germann, A.L.; Arora, R.; Cao, L.Q.; Gao, X.; Shin, D.J.; Wu, A.; Chiara, D.C.; Cohen, J.B.; Steinbach, J.H.; Evers, A.S.; Akk, G. Multiple non-equivalent interfaces mediate direct activation of GABAA receptors by propofol. Curr. Neuropharmacol., 2016, 14(7), 772-780. [http://dx.doi.org/10.2174/1570159X146661 60202121319]. [PMID: 26830963].
[15]
Forman, S.A.; Stewart, D. Mutations in the GABAA receptor that mimic the allosteric ligand etomidate. Methods Mol. Biol., 2012, 796, 317-333. [http://dx.doi.org/10.1007/978-1-61779-334-9_17]. [PMID: 22052498].
[16]
Lape, R.; Colquhoun, D.; Sivilotti, L.G. On the nature of partial agonism in the nicotinic receptor superfamily. Nature, 2008, 454(7205), 722-727. [http://dx.doi.org/10.1038/nature07139]. [PMID: 18633353].
[17]
Gielen, M.C.; Lumb, M.J.; Smart, T.G. Benzodiazepines modulate GABAA receptors by regulating the preactivation step after GABA binding. J. Neurosci., 2012, 32(17), 5707-5715. [http://dx.doi.org/ 10.1523/JNEUROSCI.5663-11.2012]. [PMID: 22539833].
[18]
Forman, S.A. Monod-Wyman-Changeux allosteric mechanisms of action and the pharmacology of etomidate. Curr. Opin. Anaesthesiol., 2012, 25(4), 411-418. [http://dx.doi.org/10.1097/ACO.0b013 e328354feea]. [PMID: 22614249].
[19]
Steinbach, J.H.; Akk, G. Applying the Monod-Wyman-Changeux allosteric activation model to pseudo-steady-state responses from GABAA receptors. Mol. Pharmacol., 2019, 95(1), 106-119. [http://dx.doi.org/10.1124/mol.118.113787]. [PMID: 30333132].
[20]
Ehlert, F.J. Analysis of Allosteric Interactions at Ligand-Gated Ion Channels In: Affinity and Efficacy; World Scientific Publishing Co.
Pte. Ltd, 2014; pp. Singapore179-249
[21]
Cao, L.Q.; Montana, M.C.; Germann, A.L.; Shin, D.J.; Chakrabarti, S.; Mennerick, S.; Yuede, C.M.; Wozniak, D.F.; Evers, A.S.; Akk, G. Enhanced GABAergic actions resulting from the coapplication of the steroid 3α-hydroxy-5α-pregnane-11,20-dione (alfaxalone) with propofol or diazepam. Sci. Rep., 2018, 8(1), 10341. [http:// dx.doi.org/10.1038/s41598-018-28754-7]. [PMID: 29985445].
[22]
Li, P.; Eaton, M.M.; Steinbach, J.H.; Akk, G. The benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists. Anesthesiology, 2013, 118(6), 1417-1425. [http://dx. doi.org/10.1097/ALN.0b013e318289bcd3]. [PMID: 23407108].
[23]
Amin, J.; Weiss, D.S. GABAA receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature, 1993, 366(6455), 565-569. [http://dx.doi.org/ 10.1038/366565a0]. [PMID: 7504783].
[24]
Chang, Y.; Wang, R.; Barot, S.; Weiss, D.S. Stoichiometry of a recombinant GABAA receptor. J. Neurosci., 1996, 16(17), 5415-5424. [http://dx.doi.org/10.1523/JNEUROSCI.16-17-05415.1996]. [PMID: 8757254].
[25]
Shin, D.J.; Germann, A.L.; Johnson, A.D.; Forman, S.A.; Steinbach, J.H.; Akk, G. Propofol is an allosteric agonist with multiple binding sites on concatemeric ternary GABAA receptors. Mol. Pharmacol., 2018, 93(2), 178-189. [http://dx.doi.org/10.1124/mol. 117.110403]. [PMID: 29192122].
[26]
Shin, D.J.; Germann, A.L.; Steinbach, J.H.; Akk, G. The actions of drug combinations on the GABAA receptor manifest as curvilinear isoboles of additivity. Mol. Pharmacol., 2017, 92(5), 556-563. [http://dx.doi.org/10.1124/mol.117.109595]. [PMID: 28790148].
[27]
Tran, P.N.; Laha, K.T.; Wagner, D.A. A tight coupling between β2Y97 and β2F200 of the GABA(A) receptor mediates GABA binding. J. Neurochem., 2011, 119(2), 283-293. [http://dx.doi.org/ 10.1111/j.1471-4159.2011.07409.x]. [PMID: 21806616].
[28]
Boileau, A.J.; Newell, J.G.; Czajkowski, C. GABA(A) receptor β 2 Tyr97 and Leu99 line the GABA-binding site. Insights into mechanisms of agonist and antagonist actions. J. Biol. Chem., 2002, 277(4), 2931-2937. [http://dx.doi.org/10.1074/jbc.M109334200]. [PMID: 11711541].
[29]
Shin, D.J.; Germann, A.L.; Covey, D.F.; Steinbach, J.H.; Akk, G. Analysis of GABAA receptor activation by combinations of agonists acting at the same or distinct binding sites. Mol. Pharmacol., 2019, 95(1), 70-81. [http://dx.doi.org/10.1124/mol.118.113464]. [PMID: 30337372].
[30]
Chiara, D.C.; Jayakar, S.S.; Zhou, X.; Zhang, X.; Savechenkov, P.Y.; Bruzik, K.S.; Miller, K.W.; Cohen, J.B. Specificity of intersubunit general anesthetic-binding sites in the transmembrane domain of the human α1β3γ2 γ-aminobutyric acid type A (GABAA) receptor. J. Biol. Chem., 2013, 288(27), 19343-19357. [http://dx.doi.org/10.1074/jbc.M113.479725]. [PMID: 23677991].
[31]
Jayakar, S.S.; Zhou, X.; Chiara, D.C.; Dostalova, Z.; Savechenkov, P.Y.; Bruzik, K.S.; Dailey, W.P.; Miller, K.W.; Eckenhoff, R.G.; Cohen, J.B. Multiple propofol-binding sites in a γ-aminobutyric acid type A receptor (GABAAR) identified using a photoreactive propofol analog. J. Biol. Chem., 2014, 289(40), 27456-27468. [http://dx.doi.org/10.1074/jbc.M114.581728]. [PMID: 25086038].
[32]
Germann, A.L.; Shin, D.J.; Kuhrau, C.R.; Johnson, A.D.; Evers, A.S.; Akk, G. High constitutive activity accounts for the combination of enhanced direct activation and reduced potentiation in mutated GABAA receptors. Mol. Pharmacol., 2018, 93(5), 468-476. [http://dx.doi.org/10.1124/mol.117.111435]. [PMID: 29439087].
[33]
Li, P.; Akk, G. Synaptic-type α1β2γ2L GABAA receptors produce large persistent currents in the presence of ambient GABA and anesthetic drugs. Mol. Pharmacol., 2015, 87(5), 776-781. [http://dx. doi.org/10.1124/mol.114.096453]. [PMID: 25667223].
[34]
Nourmahnad, A.; Stern, A.T.; Hotta, M.; Stewart, D.S.; Ziemba, A.M.; Szabo, A.; Forman, S.A. Tryptophan and cysteine mutations in M1 helices of α1β3γ2L γ-aminobutyric acid type A receptors indicate distinct intersubunit sites for four intravenous anesthetics and one orphan site. Anesthesiology, 2016, 125(6), 1144-1158. [http:// dx.doi.org/10.1097/ALN.0000000000001390]. [PMID: 27753644].
[35]
Bracamontes, J.R.; Steinbach, J.H. Steroid interaction with a single potentiating site is sufficient to modulate GABA-A receptor function. Mol. Pharmacol., 2009, 75(4), 973-981. [http://dx.doi.org/ 10.1124/mol.108.053629]. [PMID: 19176850].
[36]
Bracamontes, J.; McCollum, M.; Esch, C.; Li, P.; Ann, J.; Steinbach, J.H.; Akk, G. Occupation of either site for the neurosteroid allopregnanolone potentiates the opening of the GABAA receptor induced from either transmitter binding site. Mol. Pharmacol., 2011, 80(1), 79-86. [http://dx.doi.org/10.1124/mol.111.071662]. [PMID: 21498656].
