메뉴 건너뛰기




Volumn 165, Issue 6, 2012, Pages 1757-1772

Different in vitro and in vivo profiles of substituted 3- aminopropylphosphinate and 3-aminopropyl(methyl)phosphinate GABA B receptor agonists as inhibitors of transient lower oesophageal sphincter relaxation

Author keywords

GABA transporter; GABA B receptor; gastro oesophageal reflux disease; hypothermia; transient lower oesophageal sphincter relaxation

Indexed keywords

3 AMINOPROPYL(METHYL)PHOSPHINIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B1 RECEPTOR; 4 AMINOBUTYRIC ACID B2 RECEPTOR; LESOGABERAN; UNCLASSIFIED DRUG;

EID: 84857463153     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2011.01682.x     Document Type: Article
Times cited : (2)

References (38)
  • 1
    • 81355156238 scopus 로고    scopus 로고
    • Guide to Receptors and Channels (GRAC), 5th Edition
    • Alexander SPH, Mathie A, Peters JA, (2011). Guide to Receptors and Channels (GRAC), 5th Edition. Br J Pharmacol 164 (Suppl. 1): S1-S324.
    • (2011) Br J Pharmacol , vol.164 , Issue.SUPPL. 1
    • Alexander, S.P.H.1    Mathie, A.2    Peters, J.A.3
  • 3
    • 0032720273 scopus 로고    scopus 로고
    • Inhibition of transient LOS relaxations and reflux in ferrets by GABA receptor agonists
    • Blackshaw LA, Staunton E, Lehmann A, Dent J, (1999). Inhibition of transient LOS relaxations and reflux in ferrets by GABA receptor agonists. Am J Physiol 277: G867-G874.
    • (1999) Am J Physiol , vol.277
    • Blackshaw, L.A.1    Staunton, E.2    Lehmann, A.3    Dent, J.4
  • 4
    • 77955502520 scopus 로고    scopus 로고
    • Effects of lesogaberan on reflux and lower esophageal sphincter function in patients with gastroesophageal reflux disease
    • Boeckxstaens GE, Beaumont H, Mertens V, Denison H, Ruth M, Adler J, et al,. (2010a). Effects of lesogaberan on reflux and lower esophageal sphincter function in patients with gastroesophageal reflux disease. Gastroenterology 139: 409-417.
    • (2010) Gastroenterology , vol.139 , pp. 409-417
    • Boeckxstaens, G.E.1    Beaumont, H.2    Mertens, V.3    Denison, H.4    Ruth, M.5    Adler, J.6
  • 6
    • 80051551701 scopus 로고    scopus 로고
    • A novel reflux inhibitor lesogaberan (AZD3355) as add-on treatment in patients with GORD with persistent reflux symptoms despite proton pump inhibitor therapy: A randomised placebo-controlled trial
    • Boeckxstaens GE, Beaumont H, Hatlebakk JG, Silberg DG, Björck K, Karlsson M, et al,. (2011). A novel reflux inhibitor lesogaberan (AZD3355) as add-on treatment in patients with GORD with persistent reflux symptoms despite proton pump inhibitor therapy: a randomised placebo-controlled trial. Gut 60: 1182-1188.
    • (2011) Gut , vol.60 , pp. 1182-1188
    • Boeckxstaens, G.E.1    Beaumont, H.2    Hatlebakk, J.G.3    Silberg, D.G.4    Björck, K.5    Karlsson, M.6
  • 8
    • 0028072376 scopus 로고
    • Peripheral and central sites of action of GABA-B agonists to inhibit the cough reflex in the cat and guinea pig
    • Bolser DC, DeGennaro FC, O'Reilly S, Chapman RW, Kreutner W, Egan RW, et al,. (1994). Peripheral and central sites of action of GABA-B agonists to inhibit the cough reflex in the cat and guinea pig. Br J Pharmacol 113: 1344-1348.
    • (1994) Br J Pharmacol , vol.113 , pp. 1344-1348
    • Bolser, D.C.1    Degennaro, F.C.2    O'Reilly, S.3    Chapman, R.W.4    Kreutner, W.5    Egan, R.W.6
  • 9
    • 77951205836 scopus 로고    scopus 로고
    • B receptor agonist lesogaberan (AZD3355) inhibits acid reflux and reduces esophageal acid exposure as measured with 24-h pHmetry in dogs
    • B receptor agonist lesogaberan (AZD3355) inhibits acid reflux and reduces esophageal acid exposure as measured with 24-h pHmetry in dogs. Eur J Pharmacol 634: 138-141.
    • (2010) Eur J Pharmacol , vol.634 , pp. 138-141
    • Brändén, L.1    Fredriksson, A.2    Harring, E.3    Jensen, J.4    Lehmann, A.5
  • 11
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50)
    • Cheng Y-C, Prusoff WH, (1973). Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 percent inhibition (I50). Biochem Pharmacol 22: 3099-3108.
    • (1973) Biochem Pharmacol , vol.22 , pp. 3099-3108
    • Cheng, Y.-C.1    Prusoff, W.H.2
  • 12
    • 0001703033 scopus 로고
    • Diethoxymethylphosphonites and phosphinates. Intermediates for the synthesis of α,β- and X aminoalkylphosphonous acids
    • Dingwall JG, Ehrenfreund J, Hall RG, (1989). Diethoxymethylphosphonites and phosphinates. Intermediates for the synthesis of α,β- and X aminoalkylphosphonous acids. Tetrahedron 45: 3787-3808.
    • (1989) Tetrahedron , vol.45 , pp. 3787-3808
    • Dingwall, J.G.1    Ehrenfreund, J.2    Hall, R.G.3
  • 15
    • 0034464103 scopus 로고    scopus 로고
    • Excess gastroesophageal reflux in patients with hiatus hernia is caused by mechanisms other than transient LOS relaxations
    • van Herwaarden MA, Samsom M, Smout AJ, (2000). Excess gastroesophageal reflux in patients with hiatus hernia is caused by mechanisms other than transient LOS relaxations. Gastroenterology. 119: 1439-1446.
    • (2000) Gastroenterology. , vol.119 , pp. 1439-1446
    • Van Herwaarden, M.A.1    Samsom, M.2    Smout, A.J.3
  • 17
    • 0033594164 scopus 로고    scopus 로고
    • Piperidinyl-3-phosphinic acids as novel uptake inhibitors of the neurotransmitter Î-aminobutyric acid (GABA)
    • Kehler J, Stensbol TB, Krogsgaard-Larsen P, (1999). Piperidinyl-3- phosphinic acids as novel uptake inhibitors of the neurotransmitter Î-aminobutyric acid (GABA). Bioorg Med Chem Lett 9: 811-814.
    • (1999) Bioorg Med Chem Lett , vol.9 , pp. 811-814
    • Kehler, J.1    Stensbol, T.B.2    Krogsgaard-Larsen, P.3
  • 19
    • 77956393744 scopus 로고    scopus 로고
    • Beyond acid suppression: New pharmacologic approaches for treatment of GORD
    • Kuo P, Holloway RH, (2010). Beyond acid suppression: new pharmacologic approaches for treatment of GORD. Curr Gastroenterol Rep 12: 175-180.
    • (2010) Curr Gastroenterol Rep , vol.12 , pp. 175-180
    • Kuo, P.1    Holloway, R.H.2
  • 21
    • 30644478087 scopus 로고    scopus 로고
    • Effects of (2R)-(3-amino-2-fluoropropyl)sulphinic acid (AFPSiA) on transient lower oesophageal sphincter relaxation in dogs and mechanism of hypothermic effects in mice
    • Lehmann A, Holmberg AA, Bhatt U, Bremner-Danielsen M, Brändén L, Elg S, et al,. (2005). Effects of (2R)-(3-amino-2-fluoropropyl)sulphinic acid (AFPSiA) on transient lower oesophageal sphincter relaxation in dogs and mechanism of hypothermic effects in mice. Br J Pharmacol 146: 89-97.
    • (2005) Br J Pharmacol , vol.146 , pp. 89-97
    • Lehmann, A.1    Holmberg, A.A.2    Bhatt, U.3    Bremner-Danielsen, M.4    Brändén, L.5    Elg, S.6
  • 23
    • 77955081953 scopus 로고    scopus 로고
    • B receptor agonism as a novel therapeutic modality in the treatment of gastroesophageal reflux disease
    • B receptor agonism as a novel therapeutic modality in the treatment of gastroesophageal reflux disease. Adv Pharmacol 58: 287-313.
    • (2010) Adv Pharmacol , vol.58 , pp. 287-313
    • Lehmann, A.1    Jensen, J.M.2    Boeckxstaens, G.E.3
  • 25
    • 0036889719 scopus 로고    scopus 로고
    • Baclofen blocks LOS relaxation and crural diaphragm inhibition by esophageal and gastric distension in cats
    • Liu J, Pehlivanov N, Mittal RK, (2002). Baclofen blocks LOS relaxation and crural diaphragm inhibition by esophageal and gastric distension in cats. Am J Physiol 283: G1276-G1281.
    • (2002) Am J Physiol , vol.283
    • Liu, J.1    Pehlivanov, N.2    Mittal, R.K.3
  • 27
    • 33748977207 scopus 로고    scopus 로고
    • Effect of baclofen on esophagogastric motility and gastroesophageal reflux in children with gastroesophageal reflux disease: A randomized controlled trial
    • Omari TI, Benninga MA, Sansom L Butler RN, Dent J, Davidson GP, (2006). Effect of baclofen on esophagogastric motility and gastroesophageal reflux in children with gastroesophageal reflux disease: a randomized controlled trial. J Pediatr 149: 468-474.
    • (2006) J Pediatr , vol.149 , pp. 468-474
    • Omari, T.I.1    Benninga, M.A.2    Sansom Butler L, R.N.3    Dent, J.4    Davidson, G.P.5
  • 28
    • 0035015204 scopus 로고    scopus 로고
    • GABAB receptors on vagal afferent pathways: Peripheral and central inhibition
    • Partosoedarso ER, Young RL, Blackshaw LA, (2001). GABAB receptors on vagal afferent pathways: peripheral and central inhibition. Am J Physiol 280: G658-G668.
    • (2001) Am J Physiol , vol.280
    • Partosoedarso, E.R.1    Young, R.L.2    Blackshaw, L.A.3
  • 30
    • 84857495805 scopus 로고    scopus 로고
    • Alternative splicing generates a novel isoform of the rat metabotropic GABA(B)R1 receptor
    • Pfaff T, Malitschek B, Kaupmann K, Prezeau L, Pin JP, Bettler B, et al,. (1999). Alternative splicing generates a novel isoform of the rat metabotropic GABA(B)R1 receptor. Eur J Neurosci 112: 874-882.
    • (1999) Eur J Neurosci , vol.112 , pp. 874-882
    • Pfaff, T.1    Malitschek, B.2    Kaupmann, K.3    Prezeau, L.4    Pin, J.P.5    Bettler, B.6
  • 32
    • 0025295851 scopus 로고
    • Ion and temperature effects on the binding of gamma-aminobutyrate to its receptors and the high-affinity transport system
    • Shank RP, Baldy WJ, Mattucci LC, Villani FJ, (1990). Ion and temperature effects on the binding of gamma-aminobutyrate to its receptors and the high-affinity transport system. J Neurochem 54: 2007-2015.
    • (1990) J Neurochem , vol.54 , pp. 2007-2015
    • Shank, R.P.1    Baldy, W.J.2    Mattucci, L.C.3    Villani, F.J.4
  • 33
    • 0035661904 scopus 로고    scopus 로고
    • GABA(B)R expressed on vagal afferent neurones inhibit gastric mechanosensitivity in ferret proximal stomach
    • Smid S, Young R, Cooper N, Blackshaw LA, (2001). GABA(B)R expressed on vagal afferent neurones inhibit gastric mechanosensitivity in ferret proximal stomach. Am J Physiol 281: G1494-G1501.
    • (2001) Am J Physiol , vol.281
    • Smid, S.1    Young, R.2    Cooper, N.3    Blackshaw, L.A.4
  • 34
    • 0033002144 scopus 로고    scopus 로고
    • Influence of different intragastric stimuli on triggering of transient lower oesophageal sphincter relaxation in the dog
    • Stakeberg J, Lehmann A, (1999). Influence of different intragastric stimuli on triggering of transient lower oesophageal sphincter relaxation in the dog. Neurogastroenterol Motil 11: 125-132.
    • (1999) Neurogastroenterol Motil , vol.11 , pp. 125-132
    • Stakeberg, J.1    Lehmann, A.2
  • 35
    • 77950627333 scopus 로고    scopus 로고
    • Small volumes of feed can trigger transient lower esophageal sphincter relaxation and gastroesophageal reflux in the right lateral position in infants
    • van Wijk MP, Benninga MA, Davidson GP, Haslam R, Omari TI, (2010). Small volumes of feed can trigger transient lower esophageal sphincter relaxation and gastroesophageal reflux in the right lateral position in infants. J Pediatr 156: 744-748.
    • (2010) J Pediatr , vol.156 , pp. 744-748
    • Van Wijk, M.P.1    Benninga, M.A.2    Davidson, G.P.3    Haslam, R.4    Omari, T.I.5
  • 36
    • 33947322204 scopus 로고    scopus 로고
    • Obesity is associated with increased transient lower esophageal sphincter relaxation
    • Wu JC-Y, Mui LM, Cheung CM-Y, Chan Y, Sung JJ-Y, (2007). Obesity is associated with increased transient lower esophageal sphincter relaxation. Gastroenterology 132: 883-889.
    • (2007) Gastroenterology , vol.132 , pp. 883-889
    • Wu, J.-Y.1    Mui, L.M.2    Cheung, C.-Y.3    Chan, Y.4    Sung, J.-Y.5
  • 37
    • 33748369873 scopus 로고    scopus 로고
    • Esophageal pH-impedance monitoring and symptom analysis in GORD: A study in patients off and on therapy
    • Zerbib F, Roman S, Ropert A, Bruley des Varannes S, Pouderoux P, Chaput U, et al,. (2006). Esophageal pH-impedance monitoring and symptom analysis in GORD: a study in patients off and on therapy. Am J Gastroenterol 101: 1956-1963.
    • (2006) Am J Gastroenterol , vol.101 , pp. 1956-1963
    • Zerbib, F.1    Roman, S.2    Ropert, A.3    Bruley Des Varannes, S.4    Pouderoux, P.5    Chaput, U.6
  • 38
    • 0036136088 scopus 로고    scopus 로고
    • Control of transient lower oesophageal sphincter relaxations and reflux by the GABAB agonist baclofen in patients with gastro-oesophageal reflux disease
    • Zhang Q, Lehmann A, Rigda R, Dent J, Holloway RH, (2002). Control of transient lower oesophageal sphincter relaxations and reflux by the GABAB agonist baclofen in patients with gastro-oesophageal reflux disease. Gut 50: 19-24.
    • (2002) Gut , vol.50 , pp. 19-24
    • Zhang, Q.1    Lehmann, A.2    Rigda, R.3    Dent, J.4    Holloway, R.H.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.