The Benzodiazepine Diazepam Potentiates Responses of α1β2γ 2L γ-Aminobutyric Acid Type A Receptors Activated by either γ-Aminobutyric Acid or Allosteric Agonists

Anesthesiology

Volumn 118, Issue 6, 2013, Pages 1417-1425

  Li, Ping ^a   Eaton, Megan M ^a   Steinbach, Joe Henry ^a   Akk, Gustav ^a  

^a Department of Anesthesiology ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; ALFAXALONE; ALPHA1BETA2GAMMA2L GAMMA AMINOBUTYRIC ACID A RECEPTOR; DIAZEPAM; ETOMIDATE; PENTOBARBITAL; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; DRUG BINDING SITE; DRUG POTENTIATION; HUMAN; HUMAN CELL; KIDNEY CELL; PATCH CLAMP; PRIORITY JOURNAL;

ANESTHETICS; ANIMALS; BINDING SITES; DIAZEPAM; DRUG SYNERGISM; ETOMIDATE; GABA MODULATORS; GAMMA-AMINOBUTYRIC ACID; HUMANS; PATCH-CLAMP TECHNIQUES; PENTOBARBITAL; PREGNANEDIONES; RATS; RECEPTORS, GABA-A;

EID: 84878652938     PISSN: 00033022     EISSN: 15281175     Source Type: Journal    
DOI: 10.1097/ALN.0b013e318289bcd3     Document Type: Article

References (35)

1. Franks NP: General anaesthesia: From molecular targets to neuronal pathways of sleep and arousal. Nat Rev Neurosci 2008; 9:370-86
2. Rudolph U, Knoflach F: Beyond classical benzodiazepines: Novel therapeutic potential of GABAA receptor subtypes. Nat Rev Drug Discov 2011; 10:685-97
3. Berezhnoy D, Nyfeler Y, Gonthier A, Schwob H, Goeldner M, Sigel E: On the benzodiazepine binding pocket in GABAA receptors. J Biol Chem 2004; 279:3160-8
4. Walters RJ, Hadley SH, Morris KD, Amin J: Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms. Nat Neurosci 2000; 3:1274-81
5. Rogers CJ, Twyman RE, Macdonald RL: Benzodiazepine and beta-carboline regulation of single GABAA receptor channels of mouse spinal neurones in culture. J Physiol (Lond) 1994; 475:69-82
6. O'Shea SM, Wong LC, Harrison NL: Propofol increases agonist efficacy at the GABA(A) receptor. Brain Res 2000; 852:344-8
7. Krampfl K, Lepier A, Jahn K, Franke C, Bufler J: Molecular modulation of recombinant rat α1β2γ2 GABA(A) receptor channels by diazepam. Neurosci Lett 1998; 256:143-6
8. Campo-Soria C, Chang Y, Weiss DS: Mechanism of action of benzodiazepines on GABAA receptors. Br J Pharmacol 2006; 148:984-90
9. Rüsch D, Forman SA: Classic benzodiazepines modulate the open-close equilibrium in α1β2γ2L gamma-Aminobutyric acid type A receptors. Anesthesiology 2005; 102:783-92
10. Downing SS, Lee YT, Farb DH, Gibbs TT: Benzodiazepine modulation of partial agonist efficacy and spontaneously active GABA(A) receptors supports an allosteric model of modulation. Br J Pharmacol 2005; 145:894-906
11. Hosie AM, Wilkins ME, da Silva HM, Smart TG: Endogenous neurosteroids regulate GABAA receptors through two discrete transmembrane sites. Nature 2006; 444:486-9
12. Li GD, Chiara DC, Sawyer GW, Husain SS, Olsen RW, Cohen JB: Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog. J Neurosci 2006; 26:11599-605
13. Akk G, Li P, Bracamontes J, Reichert DE, Covey DF, Steinbach JH: Mutations of the GABA-A receptor α1 subunit M1 domain reveal unexpected complexity for modulation by neuroactive steroids. Mol Pharmacol 2008; 74:614-27
14. Stewart D, Desai R, Cheng Q, Liu A, Forman SA: Tryptophan mutations at azi-etomidate photo-incorporation sites on α1 or β2 subunits enhance GABAA receptor gating and reduce etomidate modulation. Mol Pharmacol 2008; 74:1687-95
15. Akk G: Contributions of the non-Alpha subunit residues (loop D) to agonist binding and channel gating in the muscle nicotinic acetylcholine receptor. J Physiol (Lond) 2002; 544:695-705
16. Ueno S, Zorumski C, Bracamontes J, Steinbach JH: Endogenous subunits can cause ambiguities in the pharmacology of exogenous gamma-Aminobutyric acidA receptors expressed in human embryonic kidney 293 cells. Mol Pharmacol 1996; 50:931-8
17. Li P, Covey DF, Steinbach JH, Akk G: Dual potentiating and inhibitory actions of a benz[e]indene neurosteroid analog on recombinant α1β2γ2 GABAA receptors. Mol Pharmacol 2006; 69:2015-26
18. Akk G, Bracamontes J, Steinbach JH: Pregnenolone sulfate block of GABA(A) receptors: Mechanism and involvement of a residue in the M2 region of the alpha subunit. J Physiol (Lond) 2001; 532:673-84
19. Akk G, Bracamontes JR, Covey DF, Evers A, Dao T, Steinbach JH: Neuroactive steroids have multiple actions to potentiate GABAA receptors. J Physiol (Lond) 2004; 558:59-74
20. Sakmann B, Patlak J, Neher E: Single acetylcholine-Activated channels show burst-kinetics in presence of desensitizing concentrations of agonist. Nature 1980; 286:71-3
21. Morlock EV, Czajkowski C: Different residues in the GABAA receptor benzodiazepine binding pocket mediate benzodiazepine efficacy and binding. Mol Pharmacol 2011; 80:14-22
22. Hanson SM, Czajkowski C: Structural mechanisms underlying benzodiazepine modulation of the GABA(A) receptor. J Neurosci 2008; 28:3490-9
23. Wieland HA, Lüddens H, Seeburg PH: A single histidine in GABAA receptors is essential for benzodiazepine agonist binding. J Biol Chem 1992; 267:1426-9
24. Steinbach JH, Akk G: Modulation of GABA(A) receptor channel gating by pentobarbital. J Physiol (Lond) 2001; 537:715-33
25. Akk G, Covey DF, Evers AS, Mennerick S, Zorumski CF, Steinbach JH: Kinetic and structural determinants for GABA-A receptor potentiation by neuroactive steroids. Curr Neuropharmacol 2010; 8:18-25
26. Padgett CL, Lummis SC: The F-loop of the GABA A receptor gamma2 subunit contributes to benzodiazepine modulation. J Biol Chem 2008; 283:2702-8
27. Akk G, Shu HJ, Wang C, Steinbach JH, Zorumski CF, Covey DF, Mennerick S: Neurosteroid access to the GABAA receptor. J Neurosci 2005; 25:11605-13
28. Gielen MC, Lumb MJ, Smart TG: Benzodiazepines modulate GABAA receptors by regulating the preactivation step after GABA binding. J Neurosci 2012; 32:5707-15
29. Sharkey LM, Czajkowski C: Individually monitoring ligandinduced changes in the structure of the GABAA receptor at benzodiazepine binding site and non-binding-site interfaces. Mol Pharmacol 2008; 74:203-12
30. Eaton MM, Lim YB, Bracamontes J, Steinbach JH, Akk G: Agonist-specific conformational changes in the α1-γ2 subunit interface of the GABA A receptor. Mol Pharmacol 2012; 82:255-63
31. Muroi Y, Theusch CM, Czajkowski C, Jackson MB: Distinct structural changes in the GABAA receptor elicited by pentobarbital and GABA. Biophys J 2009; 96:499-509
32. Mercado J, Czajkowski C: Gamma-Aminobutyric acid (GABA) and pentobarbital induce different conformational rearrangements in the GABA A receptor α1 and β2 pre-M1 regions. J Biol Chem 2008; 283:15250-7
33. Short TG, Chui PT: Propofol and midazolam act synergistically in combination. Br J Anaesth 1991; 67:539-45
34. Paspatis GA, Charoniti I, Manolaraki M, Vardas E, Papanikolaou N, Anastasiadou A, Gritzali A: Synergistic sedation with oral midazolam as a premedication and intravenous propofol versus intravenous propofol alone in upper gastrointestinal endoscopies in children: A prospective, randomized study. J Pediatr Gastroenterol Nutr 2006; 43:195-9
35. Wilder-Smith OH, Ravussin PA, Decosterd LA, Despland PA, Bissonnette B: Midazolam premedication reduces propofol dose requirements for multiple anesthetic endpoints. Can J Anaesth 2001; 48:439-45