Intestinal gaboxadol absorption via PAT1 (SLC36A1): Modified absorption in vivo following co-administration of L-tryptophan

British Journal of Pharmacology

Volumn 157, Issue 8, 2009, Pages 1380-1389

  Larsen, M ^a   Holm, R ^b   Jensen, K G ^b   Brodin, B ^a   Nielsen, C U ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b H LUNDBECK A S   (Denmark)

Author keywords

Caco 2 cells; Dog; Drug delivery; Gaboxadol; HPAT1 (SLC36A1); Modified intestinal absorption; Pharmacokinetics; Tryptophan

Indexed keywords

AMINO ACID TRANSPORTER; BUFFER; GABOXADOL; PARACETAMOL; PROLINE; TRYPTOPHAN;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFECT; DRUG POTENTIATION; DRUG TRANSPORT; IN VITRO STUDY; IN VIVO STUDY; INTESTINE ABSORPTION; MALE; NONHUMAN; PRIORITY JOURNAL;

ADMINISTRATION, ORAL; AMINO ACID TRANSPORT SYSTEMS; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CACO-2 CELLS; DOGS; DRUG INTERACTIONS; HUMANS; HYDROGEN-ION CONCENTRATION; INJECTIONS, INTRAVENOUS; INTESTINAL ABSORPTION; ISOXAZOLES; MALE; SYMPORTERS; TISSUE DISTRIBUTION; TRYPTOPHAN;

EID: 70350337094     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2009.00253.x     Document Type: Article

References (37)

1. Abbot EL, Grenade DS, Kennedy DJ, Gatfield KM, Thwaites DT (2006). Vigabatrin transport across the human intestinal epithelial (Caco-2) brush-border membrane is via the H+-coupled amino-acid transporter hPAT1. Br J Pharmacol 147: 298-306.
2. Anderson CM, Grenade DS, Boll M, Foltz M, Wake KA, Kennedy DJ et al. (2004). H+/Amino acid transporter 1 (PAT1) is the imino acid carrier: an intestinal nutrient/drug transporter in human and rat. Gastroenterology 127: 1410-1422.
3. Boll M, Foltz M, Rubio-Aliaga I, Kottra G, Daniel H (2002). Functional characterization of two novel mammalian electrogenic proton-dependent amino acid cotransporters. J Biol Chem 277: 22966-22973.
4. Broer A, Klingel K, Kowalczuk S, Rasko JE, Cavanaugh J, Broer S (2004). Molecular cloning of mouse amino acid transport system B0, a neutral amino acid transporter related to Hartnup disorder. J Biol Chem 279: 24467-24476.
5. Calbet JA, MacLean DA (1997). Role of caloric content on gastric emptying in humans. J Physiol 498: 553-559.
6. Chen Z, Fei YJ, Anderson CM, Wake KA, Miyauchi S, Huang W et al. (2003). Structure, function and immunolocalization of a proton-coupled amino acid transporter (hPAT1) in the human intestinal cell line Caco-2. J Physiol 546: 349-361.
7. Cheng Y, Prusoff WH (1973). Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22: 3099-3108.
8. Corey JL, Guastella J, Davidson N, Lester HA (1994). GABA uptake and release by a mammalian cell line stably expressing a cloned rat brain GABA transporter. Mol Membr Biol 11: 23-30.
9. Dave MH, Schulz N, Zecevic M, Wagner CA, Verrey F (2004). Expression of heteromeric amino acid transporters along the murine intestine. J Physiol 558: 597-610. (Pubitemid 39117604)
10. Ebert B, Wafford KA (2006). Benzodiazepine receptor agonist and insomnia: is subtype selsctivity lost in translation? Drug Discov Today 3: 547-554.
11. Ebert B, Wafford KA, Deacon S (2006). Treating insomnia: current and investigational pharmacological approaches. Pharmacol Ther 112: 612-629.
12. Hatanaka T, Huang W, Nakanishi T, Bridges CC, Smith SB, Prasad PD et al. (2002). Transport of D-serine via the amino acid transporter ATB0,+ expressed in the colon. Biochem Biophys Res Commun 291: 291-295.
13. Kall MA, Fu I, Dige T, Vallano P, Woolf E, Jorgensen M (2007). Development and validation of a selective and sensitive bioanalytical procedure for the quantitative determination of gaboxadol in human plasma employing mixed mode solid phase extraction and hydrophilic interaction liquid chromatography with tandem mass spectroscopic detection. J Chromatogr B Analyt Technol Biomed Life Sci 858: 168-176.
14. Kjaer M, Nielsen H (1983). The analgesic effect of the GABA-agonist THIP in patients with chronic pain of malignant origin. A phase-1-2 study. Br J Clin Pharmacol 16: 477-485.
15. Krogsgaard-Larsen P, Frolund B, Jorgensen FS, Schousboe A (1994). GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects. J Med Chem 37: 2489-2505.
16. Lancel M, Faulhaber J (1996). The GABAA agonist THIP (gaboxadol) increases non-REM sleep and enhances delta activity in the rat. Neuroreport 7: 2241-2245.
17. Langenbucher F (1982). Numerical convolution/deconvolution as a tool for correlating in vitro with in vivo drug availability. Pharm Ind 44: 1166-1172.
18. Larsen M, Larsen BB, Frolund B, Nielsen CU (2008). Transport of amino acids and GABA analogues via the human proton-coupled amino acid transporter, hPAT1: characterization of conditions for affinity and transport experiments in Caco-2 cells. Eur J Pharm Sci 35: 86-95.
19. Lund J, Helboe T, Mengel H (2006). Absorption, metabolism and excretion profile of gaboxadol in humans. Sleep 29: A41.
20. Lundahl J, Staner L, Staner C, Loft H, Deacon S (2007). Short-term treatment with gaboxadol improves sleep maintenance and enhances slow wave sleep in adult patients with primary insomnia. Psychopharmacology (Berl) 195: 139-146. (Pubitemid 47568617)
21. Metzner L, Kottra G, Neubert K, Daniel H, Brandsch M (2005). Serotonin, L-tryptophan, and tryptamine are effective inhibitors of the amino acid transport system PAT1. FASEB J 19: 1468-1473.
22. Mizuta H, Kawazoe Y, Haga K, Ogawa K (1990). Effects of meals on gastric emptying and small intestinal transit times of a suspension in the beagle dog assessed using acetaminophen and salicylazosul-fapyridine as markers. Chem Pharm Bull (Tokyo) 38: 2224-2227.
23. Nguyen TV, Smith DE, Fleisher D (2007). PEPT1 enhances the uptake of gabapentin via trans-stimulation of b0,+ exchange. Pharm Res 24: 353-360.
24. Nutt DJ (2005). Making sense of GABA(A) receptor subtypes: is a new nomenclature needed? J Psychopharmacol 19: 219-220.
25. Palacin M (1994). A new family of proteins (rBAT and 4F2hc) involved in cationic and zwitterionic amino acid transport: a tale of two proteins in search of a transport function. J Exp Biol 196: 123-137.
26. Rowland M, Tozer TN (1995). Clinical Pharmacokinetics Concepts and Applications, 3rd edn. Lippincott, Williams & Wilkins: Philadelphia, PA.
27. Sagné C, Agulhon C, Ravassard P, Darmon M, Hamon M, El Mes-tikawy S et al. (2001). Identification and characterization of a lyso-somal transporter for small neutral amino acids. Proc Natl Acad Sci USA 98: 7206-7211.
28. Schultz B, Aaes-Jorgensen T, Bogeso KP, Jorgensen A (1981). Preliminary studies on the absorption, distribution, metabolism, and excretion of THIP in animal and man using 14C-labelled compound. Acta Pharmacol Toxicol (Copenh) 49: 116-124.
29. Shadle C, Rainakrishnan R, Gargano C, Fu I, Luo R, Alexander R et al. (2006). Assessment of dose proportionality, absolute bioavailability, and tolerability of gaboxadol in healthy young adults. Sleep 29: A40-A41.
30. Su TZ, Logsdon CD, Oxender DL (1992). Chinese hamster ovary mRNA-dependent, Na+-independent L-leucine trasport in Xenopus laevis oocytes. Mol Cell Biol 12: 5281-5287.
31. Sunesen VH, Vedelsdal R, Kristensen HG, Christrup L, Mullertz A (2005). Effect of liquid volume and food intake on the absolute bioavailability of danazol, a poorly soluble drug. Eur J Pharm Sci 24: 297-303.
32. Tate SS, Yan N, Udenfriend S (1992). Expression cloning of a Na+-independent neutral amino acid transporter from rat kidney. Proc Natl Acad Sci USA 89: 1-5.
33. Thwaites DT, McEwan GT, Cook MJ, Hirst BH, Simmons NL (1993). H+-coupled (Na+-independent) proline transport in human intestinal (Caco-2) epithelial cell monolayers. FEBS Lett 333: 78-82.
34. Thwaites DT, Armstrong G, Hirst BH, Simmons NL (1995a). D-cycloserine transport in human intestinal epithelial (Caco-2) cells: mediation by a H+-coupled amino acid transporter. Br J Pharmacol 115: 761-766.
35. Thwaites DT, McEwan GT, Simmons NL (1995b). The role of the proton electrochemical gradient in the transepithelial absorption of amino acids by human intestinal Caco-2 cell monolayers. J Membr Biol 145: 245-256.
36. Uchiyama T, Matsuda Y, Wada M, Takahashi S, Fujita T (2005). Functional regulation of Na+-dependent neutral amino acid transporter ASCT2 by S-nitrosothiols and nitric oxide in Caco-2 cells. FEBS Lett 579: 2499-2506.
37. Wenzel U, Meissner B, Doring F, Daniel H (2001). PEPT1-mediated uptake of dipeptides enhances the intestinal absorption of amino acids via transport system b0,+. J Cell Physiol 186: 251-259.