Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors

Current Drug Targets

Volumn 8, Issue 1, 2007, Pages 169-184

  Bräuner Osborne, Hans ^a   Wellendorph, Petrine ^a   Jensen, Anders A ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

aminobutyric acidB receptor; Calcium sensing receptor; GPRC6A; Metabotropic glutamate receptor

Indexed keywords

1 AMINO 1,3 CYCLOPENTANEDICARBOXYLIC ACID; 2 AMINO 2 (2 CARBOXYCYCLOPROPYL) 3 (XANTHEN 9 YL)PROPIONIC ACID; 2 METHYL 6 (2 PHENYLVINYL)PYRIDINE; 2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; 3 AMINOPROPANEPHOSPHINIC ACID; 3 AMINOPROPYLBUTYLPHOSPHINIC ACID; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR BLOCKING AGENT; BACLOFEN; BAY 36 7620; CGP 64213; CGP 71872; CGP 7930; EGLUMETAD; G PROTEIN COUPLED RECEPTOR; GABAERGIC RECEPTOR AFFECTING AGENT; GABAPENTIN; GS 39783; LY 339764; LY 393675; LY 487379; METABOTROPIC RECEPTOR; METABOTROPIC RECEPTOR AGONIST; METABOTROPIC RECEPTOR ANTAGONIST; PHACLOFEN; RO 64 5229; RO 67 4853; SACLOFEN; SGS 752; TALAGLUMETAD; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ALZHEIMER DISEASE; BINDING SITE; CLINICAL TRIAL; COGNITIVE DEFECT; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG INDICATION; DRUG STRUCTURE; DRUG TRANSPORT; GENERALIZED ANXIETY DISORDER; HUMAN; LIGAND BINDING; MUSCLE RELAXATION; MUSCLE SPASM; NEUROLOGIC DISEASE; NONHUMAN; PANIC; PERMEABILITY BARRIER; PROTEIN DETERMINATION; PROTEIN FAMILY; PROTEIN FUNCTION; PROTEIN STRUCTURE; PROTEIN TARGETING; RECEPTOR AFFINITY; REVIEW; SEDATION; SIDE EFFECT; STRUCTURE ANALYSIS;

ANIMALS; HUMANS; LIGANDS; RECEPTORS, CALCIUM-SENSING; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, GABA-B; RECEPTORS, METABOTROPIC GLUTAMATE;

EID: 33845973375     PISSN: 13894501     EISSN: None     Source Type: Journal    
DOI: 10.2174/138945007779315614     Document Type: Review

References (226)

1. Gether, U. (2000) Endocr. Rev., 21, 90-113.
2. Pierce, K.L.; Premont, R.T. and Lefkowitz, R.J. (2002) Nat. Rev. Mol. Cell Biol., 3, 639-650.
3. Lefkowitz, R.J. and Shenoy, S.K. (2005) Science, 308, 512-517.
4. Lei, Q.; Jones, M.B.; Talley, E.M.; Garrison, J.C. and Bayliss, D.A. (2003) Mol. Cells, 15, 1-9.
5. Strock, J. and Diverse-Pierluissi, M.A. (2004) Mol. Pharmacol., 66, 1071-1076.
6. Kolakowski, L.F., Jr. (1994) Recept. Channels, 2, 1-7.
7. Bettler, B.; Kaupmann, K.; Mosbacher, J. and Gassmann, M. (2004) Physiol. Rev., 84, 835-867.
8. Brown, E.M. (1999) Am. J. Med., 106, 238-253.
9. Bräuner-Osborne, H.; Jensen, A.A.; Sheppard, P.O.; Brodin, B.; Krogsgaard-Larsen, P. and O'Hara, P. (2001) Biochim. Biophys. Acta, 1518, 237-248.
10. Bräuner-Osborne, H. and Krogsgaard-Larsen, P. (2000) Genomics, 65, 121-128.
11. Calver, A.R.; Michalovich, D.; Testa, T.T.; Robbins, M.J.; Jaillard, C.; Hill, J.; Szekeres, P.G.; Charles, K.J.; Jourdain, S.; Holbrook, J.D.; Boyfield, I.; Patel, N.; Medhurst, A.D. and Pangalos, M.N. (2003) Mol. Brain Res., 110, 305-317.
12. Cheng, Y. and Lotan, R. (1998) J. Biol. Chem., 273, 35008-35015.
13. Couve, A.; Moss, S.J. and Pangalos, M.N. (2000) Mol. Cell. Neurosci., 16, 296-312.
14. Jensen, A.A. (2004) in Molecular Neuropharmacology. Strategies and Methods, (A. Schousboe and H. Bräuner-Osborne), Humana Press, pp. 47-82.
15. Kuang, D.; Yao, Y.; Lam, J.; Tsushima, R.G. and Hampson, D.R. (2005) J. Neurochem., 93, 383-391.
16. Nelson, G.; Hoon, M.A.; Chandrashekar, J.; Zhang, Y.; Ryba, N.J. and Zuker, C.S. (2001) Cell, 106, 381-390.
17. Pin, J.-P.; Galvez, T. and Prézeau, L. (2003) Pharmacol. Ther., 98, 325-354.
18. Robbins, M.J.; Milchalovich, D.; Hill, J.; Calver, A.R.; Medhurst, A.D.; Gloger, I.; Sims, M.; Middlemiss, D.N. and Pangalos, M.N. (2000) Genomics, 67, 8-18.
19. Tfelt-Hansen, J. and Brown, E.M. (2005) Crit. Rev. Clin. Lab. Sci., 42, 35-70.
20. Vacher, C.M. and Bettler, B. (2003) Curr. Drug Targets CNS Neurol. Disord., 2, 248-259.
21. Wellendorph, P.; Hansen, K.B.; Balsgaard, A.; Greenwood, J.R.; Egebjerg, J. and Bräuner-Osborne, H. (2005) Mol. Pharmacol., 67, 589-597.
22. Zhao, G.Q.; Zhang, Y.; Hoon, M.A.; Chandrashekar, J.; Erlenbach, I.; Ryba, N.J. and Zuker, C.S. (2003) Cell, 115, 255-266.
23. Drews, J. (2000) Science, 287, 1960-1964.
24. Bräuner-Osborne, H.; Egebjerg, J.; Nielsen, E.Ø.; Madsen, U. and Krogsgaard-Larsen, P. (2000) J. Med. Chem., 43, 2609-2645.
25. Kaupmann, K.; Huggel, K.; Heid, J.; Flor, P.J.; Bischoff, S.; Mickel, S.J.; McMaster, G.; Angst, C.; Bittiger, H.; Fröstl, W. and Bettler, B. (1997) Nature, 386, 239-246.
26. Dingledine, R.; Borges, K.; Bowie, D. and Traynelis, S.F. (1999) Pharmacol. Rev., 51, 7-61.
27. Sieghart, W. and Sperk, G. (2002) Curr. Top. Med. Chem., 2, 795-816.
28. Kunishima, N.; Shimada, Y.; Tsuji, Y.; Sato, T.; Yamamoto, M.; Kumasaka, T.; Nakanishi, S.; Jingami, H. and Morikawa, K. (2000) Nature, 407, 971-977.
29. Tsuchiya, D.; Kunishima, N.; Kamiya, N.; Jingami, H. and Morikawa, K. (2002) Proc. Natl. Acad. Sci. USA, 99, 2660-2665.
30. Jingami, H.; Nakanishi, S. and Morikawa, K. (2003) Curr. Opin. Neurobiol., 13, 271-278.
31. Kubo, Y. and Tateyama, M. (2005) Curr. Opin. Neurobiol., 15, 289-295.
32. Pin, J.P.; Kniazeff, J.; Binet, V.; Liu, J.; Maurel, D.; Galvez, T.; Duthey, B.; Havlickova, M.; Blahos, J.; Prezeau, L. and Rondard, P. (2004) Biochem. Pharmacol., 68, 1565-1572.
33. Bouvier, M. (2001) Nat. Rev. Neurosci., 2, 274-286.
34. Rios, C.D.; Jordan, B.A.; Gomes, I. and Devi, L.A. (2001) Pharm. Ther., 92, 71-87.
35. Bai, M.; Trivedi, S. and Brown, E.M. (1998) J. Biol. Chem., 273, 23605-23610.
36. Pace, A.J.; Gama, L. and Breitwieser, G.E. (1999) J. Biol. Chem., 274, 11629-11634.
37. Ray, K. and Hauschild, B.C. (2000) J. Biol. Chem., 275, 34245-34251.
38. Ray, K.; Hauschild, B.C.; Steinbach, P.J.; Goldsmith, P.K.; Hauache, O. and Spiegel, A.M. (1999) J. Biol. Chem., 274, 27642-27650.
39. Romano, C.; Yang, W.L. and Omalley, K.L. (1996) J. Biol. Chem., 271, 28612-28616.
40. Romano, C.; Miller, J.K.; Hyrc, K.; Dikranian, S.; Mennerick, S.; Takeuchi, Y.; Goldberg, M.P. and O'Malley, K.L. (2001) Mol. Pharmacol., 59, 46-53.
41. Tsuji, Y.; Shimada, Y.; Takeshita, T.; Kajimura, N.; Nomura, S.; Sekiyama, N.; Otomo, J.; Usukura, J.; Nakanishi, S. and Jingami, H. (2000) J. Biol. Chem., 275, 28144-28151.
42. Zhang, Z.; Sun, S.; Quinn, S.J.; Brown, E.M. and Bai, M. (2001) J. Biol. Chem., 276, 5316-5322.
43. Couve, A.; Filippov, A.K.; Connolly, C.N.; Bettler, B.; Brown, D.A. and Moss, S.J. (1998) J. Biol. Chem., 273, 26361-26367.
44. Jones, K.A.; Borowsky, B.; Tamm, J.A.; Craig, D.A.; Durkin, M.M.; Dai, M.; Yao, W.J.; Johnson, M.; Gunwaldsen, C.; Huang, L.Y.; Tang, C.; Shen, Q.; Salon, J.A.; Morse, K.; Laz, T.; Smith, K.E.; Nagarathnam, D.; Noble, S.A.; Branchek, T.A. and Gerald, C. (1998) Nature, 396, 674-679.
45. Kaupmann, K.; Malitschek, B.; Schuler, V.; Heid, J.; Fröstl, W.; Beck, P.; Mosbacher, J.; Bischoff, S.; Kulik, A.; Shigemoto, R.; Karschin, A. and Bettler, B. (1998) Nature, 396, 683-687.
46. Kuner, R.; Köhr, G.; Grünewald, S.; Eisenhardt, G.; Bach, A. and Kornau, H.-C. (1999) Science, 283, 74-77.
47. Margeta-Mitrovic, M.; Jan, Y.N. and Jan, L.Y. (2000) Neuron, 27, 97-106.
48. Pagano, A.; Rovelli, G.; Mosbacher, J.; Lohmann, T.; Duthey, B.; Stauffer, D.; Ristig, D.; Schuler, V.; Meigel, I.; Lampert, C.; Stein, T.; Prezeau, L.; Blahos, J.; Pin, J.P.; Froestl, W.; Kuhn, R.; Heid, J.; Kaupmann, K. and Bettler, B. (2001) J. Neurosci., 21, 1189-1202.
49. White, J.H.; Wise, A.; Main, M.J.; Green, A.; Fraser, N.J.; Disney, G.H.; Barnes, A.A.; Emson, P.; Foord, S.M. and Marshall, F.H. (1998) Nature, 396, 679-682.
50. Duthey, B.; Caudron, S.; Perroy, J.; Bettler, B.; Fagni, L.; Pin, J.P. and Prezeau, L. (2002) J. Biol. Chem., 277, 3236-3241.
51. Havlickova, M.; Prezeau, L.; Duthey, B.; Bettler, B.; Pin, J.P. and Blahos, J. (2002) Mol. Pharmacol., 62, 343-350.
52. Margeta-Mitrovic, M.; Jan, Y.N. and Jan, L.Y. (2001) Proc. Natl. Acad. Sci. USA, 98, 14649-14654.
53. Robbins, M.J.; Calver, A.R.; Filippov, A.K.; Hirst, W.D.; Russell, R.B.; Wood, M.D.; Nasir, S.; Couve, A.; Brown, D.A.; Moss, S.J. and Pangalos, M.N. (2001) J. Neurosci., 21, 8043-8052.
54. Morfis, M.; Christopoulos, A. and Sexton, P.M. (2003) Trends Pharmacol. Sci., 24, 596-601.
55. Bräuner-Osborne, H.; Jensen, A.A.; Sheppard, P.O.; O'Hara, P. and Krogsgaard-Larsen, P. (1999) J. Biol. Chem., 274, 18382-18386.
56. Hammerland, L.G.; Krapcho, K.J.; Garrett, J.E.; Alasti, N.; Hung, B.C.; Simin, R.T.; Levinthal, C.; Nemeth, E.F. and Fuller, F.H. (1999) Mol. Pharmacol., 55, 642-648.
57. Malitschek, B.; Schweizer, C.; Keir, M.; Heid, J.; Fröstl, W.; Mosbacher, J.; Kuhn, R.; Henley, J.; Joly, C.; Pin, J.P.; Kaupmann, K. and Bettler, B. (1999) Mol. Pharmacol., 56, 448-454.
58. O'Hara, P.J.; Sheppard, P.O.; Thøgersen, H.; Venezia, D.; Haldeman, B.A.; McGrane, V.; Houamed, K.M.; Thomsen, C.; Gilbert, T.L. and Mulvihill, E.R. (1993) Neuron, 11, 41-52.
59. Okamoto, T.; Sekiyama, N.; Otsu, M.; Shimada, Y.; Sato, A., Nakanishi, S. and Jingami, H. (1998) J. Biol. Chem., 273, 13089-13096.
60. Takahashi, K.; Tsuchida, K.; Tanabe, Y.; Masu, M. and Nakanishi, S. (1993) J. Biol. Chem., 268, 19341-19345.
61. Quiocho, F.A. and Ledvina, P.S. (1996) Mol. Microbiol., 20, 17-25.
62. Costantino, G. and Pellicciari, R. (1996) J. Med. Chem., 39, 3998-4006.
63. Galvez, T.; Parmentier, M.L.; Joly, C.; Malitschek, B.; Kaupmann, K.; Kuhn, R.; Bittiger, H.; Fröstl, W.; Bettler, B. and Pin, J.P. (1999) J. Biol. Chem., 274, 13362-13369.
64. Hampson, D.R.; Huang, X.-P.; Pekhletski, R.; Peltekova, V.; Hornby, G.; Thomsen, C. and Thøgersen, H. (1999) J. Biol. Chem., 274, 33488-33495.
65. Jensen, A.A.; Greenwood, J.R. and Bräuner-Osborne, H. (2002) Trends Pharmacol. Sci., 23, 491-493.
66. Bhave, G.; Nadin, B.M.; Brasier, D.J.; Glauner, K.S.; Shah, R.D.; Heinemann, S.F.; Karim, F. and Gereau, R.W.t. (2003) J. Biol. Chem., 278, 30294-30301.
67. Chang, W.; Chen, T.H.; Pratt, S. and Shoback, D. (2000) J. Biol. Chem., 275, 19955-19963.
68. Francesconi, A. and Duvoisin, R.M. (1998) J. Biol. Chem., 273, 5615-5624.
69. Gomeza, J.; Joly, C.; Kuhn, R.; Knöpfel, T.; Bockaert, J. and Pin, J.-P. (1996) J. Biol. Chem., 271, 2199-2205.
70. Pin, J.P.; Joly, C.; Heinemann, S.F. and Bockaert, J. (1994) EMBO J., 13, 342-348.
71. Wess, J. (1998) Pharmacol. Ther., 80, 231-264.
72. Palczewski, K.; Kumasaka, T.; Hori, T.; Behnke, C.A.; Motoshima, H.; Fox, B.A.; Le Trong, I.; Teller, D.C.; Okada, T.; Stenkamp, R.E.; Yamamoto, M. and Miyano, M. (2000) Science, 289, 739-745.
73. Malherbe, P.; Kratochwil, N.; Knoflach, F.; Zenner, M.T.; Kew, J.N.; Kratzeisen, C.; Maerki, H.P.; Adam, G. and Mutel, V. (2003) J. Biol. Chem., 278, 8340-8347.
74. Malherbe, P.; Kratochwil, N.; Zenner, M.-T.; Piussi, J.; Diener, C.; Kratzeisen, C.; Fischer, C. and Porter, R.H.P. (2003) Mol. Pharmacol., 64, 823-832.
75. Miedlich, S.U.; Gama, L.; Seuwen, K.; Wolf, R.M. and Breitwieser, G.E. (2004) J. Biol. Chem., 279, 7254-7263.
76. Petrel, C.; Kessler, A.; Dauban, P.; Dodd, R.H.; Rognan, D. and Ruat, M. (2004) J. Biol. Chem., 279, 18990-18997.
77. Petrel, C.; Kessler, A.; Maslah, F.; Dauban, P.; Dodd, R.H.; Rognan, D. and Ruat, M. (2003) J. Biol. Chem., 278, 49487-49494.
78. Fan, G.F.; Ray, K.; Zhao, X.M.; Goldsmith, P.K. and Spiegel, A.M. (1998) FEBS Lett., 436, 353-356.
79. Hu, J.; Hauache, O. and Spiegel, A.M. (2000) J. Biol. Chem., 275, 16382-16389.
80. Hu, J.; Reyes-Cruz, G.; Goldsmith, P.K. and Spiegel, A.M. (2001) J. Biol. Chem., 276, 6901-6904.
81. Yu, L.; Liang, S.; Liu, X.; He, Q.; Studholme, D.J. and Wu, Q. (2004) Trends Biochem. Sci., 29, 458-461.
82. Parmentier, M.L.; Prezeau, L.; Bockaert, J. and Pin, J.P. (2002) Trends Pharmacol. Sci., 23, 268-274.
83. Bessis, A.S.; Rondard, P.; Gaven, F.; Brabet, I.; Triballeau, N.; Prezeau, L.; Acher, F. and Pin, J.P. (2002) Proc. Natl. Acad. Sci. USA, 99, 11097-11102.
84. Jensen, A.A.; Sheppard, P.O.; O'Hara, P.J.; Krogsgaard-Larsen, P. and Bräuner-Osborne, H. (2000) Eur. J. Pharmacol., 397, 247-253.
85. Malherbe, P.; Knoflach, F.; Broger, C.; Ohresser, S.; Kratzeisen, C.; Adam, G.; Stadler, H.; Kemp, J.A. and Mutel, V. (2001) Mol. Pharmacol, 60, 944-954.
86. Sato, T.; Shimada, Y.; Nagasawa, N.; Nakanishi, S. and Jingami, H. (2003) J. Biol. Chem., 278, 4314-4321.
87. Rosemond, E.; Peltekova, V.; Naples, M.; Thøgersen, H. and Hampson, D.R. (2002) J. Biol. Chem., 277, 7333-7340.
88. Yao, Y.; Pattabiraman, N.; Michne, W.F.; Huang, X.P. and Hampson, D.R. (2003) J. Neurochem., 86, 947-957.
89. Hermit, M.B.; Greenwood, J.R. and Bräuner-Osborne, H. (2004) J. Biol. Chem., 279, 34811-34817.
90. Zhang, Z.; Qiu, W.; Quinn, S.J.; Conigrave, A.D.; Brown, E.M. and Bai, M. (2002) J. Biol. Chem., 277, 33727-33735.
91. Bernard, P.; Guedin, D. and Hibert, M. (2001) J. Med. Chem., 44, 27-35.
92. Galvez, T.; Prézeau, L.; Milioti, G.; Franek, M.; Joly, C.; Froestl, W.; Bettler, B.; Bertrand, H.O.; Blahos, J. and Pin, J.P. (2000) J. Biol. Chem., 275, 41166-41174.
93. Kniazeff, J.; Galvez, T.; Labesse, G. and Pin, J.P. (2002) J. Neurosci., 22, 7352-7361.
94. Christopoulos, A. and Kenakin, T. (2002) Pharmacol. Rev., 54, 323-374.
95. Jensen, A.A. and Spalding, T.A. (2004) Eur. J. Pharm. Sci., 21, 407-420.
96. Kew, J.N. (2004) Pharmacol. Ther., 104, 233-244.
97. Bräuner-Osborne, H.; Jensen, A.A. and Krogsgaard-Larsen, P. (1999) Neuroreport, 10, 3923-3925.
98. Carroll, F.Y.; Stolle, A.; Beart, P.M.; Voerste, A.; Brabet, I.; Mauler, F.; Joly, C.; Antonicek, H.; Bockaert, J.; Müller, T.; Pin, J.P. and Prézeau, L. (2001) Mol. Pharmacol., 59, 965-973.
99. Hammerland, L.G.; Garrett, J.E.; Hung, B.C.P.; Levinthal, C. and Nemeth, E.F. (1998) Mol. Pharmacol., 53, 1083-1088.
100. Knoflach, F.; Mutel, V.; Jolidon, S.; Kew, J.N.; Malherbe, P.; Vieira, E.; Wichmann, J. and Kemp, J.A. (2001) Proc. Natl. Acad. Sci. USA, 98, 13402-13407.
101. Lavreysen, H.; Janssen, C.; Bischoff, F.; Langlois, X.; Leysen, J.E. and Lesage, A.S. (2003) Mol. Pharmacol., 63, 1082-1093.
102. Litschig, S.; Gasparini, F.; Rüegg, D.; Stoehr, N.; Flor, P.J.; Vranesic, I.; Prézeau, L.; Pin, J.-P.; Thomsen, C. and Kuhn, R. (1999) Mol. Pharmacol., 55, 453-461.
103. Pagano, A.; Rüegg, D.; Litschig, S.; Stoehr, N.; Stierlin, C.; Heinrich, M.; Floersheim, P.; Prézeau, L.; Carroll, F.; Pin, J.P.; Cambria, A.; Vranesic, I.; Flor, P.J.; Gasparini, F. and Kuhn, R. (2000) J. Biol. Chem., 275, 33750-33758.
104. Schaffhauser, H.; Rowe, B.A.; Morales, S.; Chavez-Noriega, L.E.; Yin, R.; Jachec, C.; Rao, S.P.; Bain, G.; Pinkerton, A.B.; Vernier, J.M.; Bristow, L.J.; Varney, M.A. and Daggett, L.P. (2003) Mol. Pharmacol., 64, 798-810.
105. Goudet, C.; Gaven, F.; Kniazeff, J.; Vol, C.; Liu, J.; Cohen-Gonsaud, M.; Acher, F.; Prezeau, L. and Pin, J.P. (2004) Proc. Natl. Acad. Sci. USA, 101, 378-383.
106. Binet, V.; Brajon, C.; Le Corre, L.; Acher, F.; Pin, J.P. and Prezeau, L. (2004) J. Biol. Chem., 279, 29085-29091.
107. O'Brien, J.A.; Lemaire, W.; Chen, T.B.; Chang, R.S.; Jacobson, M.A.; Ha, S.N.; Lindsley, C.W.; Schaffhauser, H.J.; Sur, C.; Pettibone, D.J.; Conn, P.J. and Williams, D.L., Jr. (2003) Mol. Pharmacol., 64, 731-740.
108. Maj, M.; Bruno, V.; Dragic, Z.; Yamamoto, R.; Battaglia, G.; Inderbitzin, W.; Stoehr, N.; Stein, T.; Gasparini, F.; Vranesic, I., Kuhn, R.; Nicoletti, F. and Flor, P.J. (2003) Neuropharmacology, 45, 895-906.
109. Marino, M.J.; Williams, D.L., Jr.; O'Brien, J.A.; Valenti, O.; McDonald, T.P.; Clements, M.K.; Wang, R.; DiLella, A.G.; Hess, J.F.; Kinney, G.G. and Conn, P.J. (2003) Proc. Natl. Acad. Sci. USA, 100, 13668-13673.
110. Mathiesen, J.M.; Svendsen, N.; Bräuner-Osborne, H.; Thomsen, C. and Ramirez, M.T. (2003) Br. J. Pharmacol., 138, 1026-1030.
111. Kubo, Y.; Miyashita, T. and Murata, Y. (1998) Science, 279, 1722-1725.
112. Galvez, T.; Urwyler, S.; Prézeau, L.; Mosbacher, J.; Joly, C.; Malitschek, B.; Heid, J.; Brabet, L; Fröstl, W.; Bettler, B.; Kaupmann, K. and Pin, J.P. (2000) Mol. Pharmacol., 57, 419-426.
113. Jensen, A.A.; Spalding, T.A.; Burstein, E.S.; Sheppard, P.O.; O'Hara, P.J.; Brann, M.R.; Krogsgaard-Larsen, P. and Bräuner-Osborne, H. (2000) J. Biol. Chem., 275, 29547-29555.
114. Jensen, A.A.; Sheppard, P.O.; Jensen, L.B.; O'Hara, P.J. and Bräuner-Osborne, H. (2001) J. Biol. Chem., 276, 10110-10118.
115. Swanson, C.J.; Bures, M.; Johnson, M.P.; Linden, A.M.; Monn, J.A. and Schoepp, D.D. (2005) Nat. Rev. Drug Discov., 4, 131-144.
116. Kellner, M.; Muhtz, C.; Stark, K.; Yassouridis, A.; Arlt, J. and Wiedemann, K. (2005) Psychopharmacology (Berl). 179, 310-315.
117. Schoepp, D.D.; Jane, D.E. and Monn, J.A. (1999) Neuropharmacology, 38, 1431-1476.
118. Madsen, U.; Bräuner-Osborne, H.; Greenwood, J.R.; Johansen, T.N.; Krogsgaard-Larsen, P.; Liljefors, T.; Nielsen, M. and Frölund, B. (2005) in Drug Discovery Handbook, (S. C. Gad), Wiley, New York, USA, pp. 797-907.
119. Eaton, S.A.; Jane, D.E.; Jones, P.L.; Porter, R.H.; Pock, P.C.; Sunter, D.C.; Udvarhelyi, P.M.; Roberts, P.J.; Salt, T.E. and Watkins, J.C. (1993) Eur. J. Pharmacol., 244, 195-197.
120. Hayashi, Y.; Sekiyama, N.; Nakanishi, S.; Jane, D.E.; Sunter, D.C.; Birse, E.F.; Udvarhelyi, P.M. and Watkins, J.C. (1994) J. Neurosci., 14, 3370-3377.
121. Thomsen, C.; Boel, E. and Suzdak, P.D. (1994) Eur. J. Pharmacol., 267, 77-84.
122. Palmer, E.; Monaghan, D.T. and Cotman, C.W. (1989) Eur. J. Pharmacol., 166, 585-587.
123. Desai, M.A. and Conn, P.J. (1990) Neurosci. Lett., 109, 157-162.
124. Irving, A.J.; Schofield, J.G.; Watkins, J.C.; Sunter, D.C. and Collingridge, G.L. (1990) Eur. J. Pharmacol., 186, 363-365.
125. Aramori, I. and Nakanishi, S. (1992) Neuron, 8, 757-765.
126. Tanabe, Y.; Masu, M.; Ishii, T.; Shigemoto, R. and Nakanishi, S. (1992) Neuron, 8, 169-179.
127. Tanabe, Y.; Nomura, A.; Masu, M.; Shigemoto, R.; Mizuno, N. and Nakanishi, S. (1993) J. Neurosci., 13, 1372-1378.
128. Abe, T.; Sugihara, H.; Nawa, H.; Shigemoto, R.; Mizano, N. and Nakanishi, S. (1992) J. Biol. Chem., 267, 13361-13368.
129. Nakajima, Y.; Iwakabe, H.; Akazawa, C.; Nawa, H.; Shigemoto, R.; Mizuno, N. and Nakanishi, S. (1993) J. Biol. Chem., 268, 11868-11873.
130. Okamoto, N.; Hori, S.; Akazawa, C.; Hayashi, Y.; Shigemoto, R.; Mizuno, N. and Nakanishi, S. (1994) J. Biol. Chem., 269, 1231-1236.
131. Saugstad, J.A.; Kinzie, J.M.; Shinohara, M.M.; Segerson, T.P. and Westbrook, G.L. (1997) Mol. Pharmacol., 51, 119-125.
132. Hayashi, Y.; Tanabe, Y.; Aramori, I.; Masu, M.; Shimamoto, K.; Ohfune, Y. and Nakanishi, S. (1992) Br. J. Pharmacol., 107, 539-543.
133. Brabet, I.; Parmentier, M.L.; De Colle, C.; Bockaert, J.; Acher, F. and Pin, J.P. (1998) Neuropharmacology, 37, 1043-1051.
134. Collado, I.; Pedregal, C.; Mazon, A.; Espinosa, J.F.; Blanco-Urgoiti, J.; Schoepp, D.D.; Wright, R.A.; Johnson, B.G. and Kingston, A.E. (2002) J. Med. Chem., 45, 3619-3629.
135. Kingston, A.E.; Ornstein, P.L.; Wright, R.A.; Johnson, B.G.; Mayne, N.G.; Burnett, J.P.; Belagaje, R.; Wu, S. and Schoepp, D.D. (1998) Neuropharmacology, 37, 1-12.
136. Wright, R.A.; Arnold, M.B.; Wheeler, W.J.; Ornstein, P.L. and Schoepp, D.D. (2000) Naunyn. Schmiedebergs Arch. Pharmacol., 362, 546-554.
137. Helton, D.R.; Tizzano, J.P.; Monn, J.A.; Schoepp, D.D. and Kallman, M.J. (1997) Neuropharmacology, 36, 1511-1516.
138. Monn, J.A.; Valli, M.J.; Massey, S.M.; Hansen, M.M.; Kress, T.J.; Wepsiec, J.P.; Harkness, A.R.; Grutsch, J.L., Jr.; Wright, R.A.; Johnson, B.G.; Andis, S.L.; Kingston, A.; Tomlinson, R.; Lewis, R.; Griffey, K.R.; Tizzano, J.P. and Schoepp, D.D. (1999) J. Med. Chem., 42, 1027-1040.
139. Dominguez, C.; Prieto, L.; Valli, M.J.; Massey, S.M.; Bures, M.; Wright, R.A.; Johnson, B.G.; Andis, S.L.; Kingston, A.; Schoepp, D.D. and Monn, J.A. (2005) J. Med. Chem., 48, 3605-3612.
140. Ahmadian, H.; Nielsen, B.; Bräuner-Osborne, H.; Johansen, T.N.; Stensbøl, T.B.; Sløk, F.A.; Sekiyama, N.; Nakanishi, S.; Krogsgaard-Larsen, P. and Madsen, U. (1997) J. Med. Chem., 40, 3700-3705.
141. Thomas, N.K.; Wright, R.A.; Howson, P.A.; Kingston, A.E.; Schoepp, D.D. and Jane, D.E. (2001) Neuropharmacology, 40, 311-318.
142. Annoura, H.; Fukunaga, A.; Uesugi, M.; Tatsuoka, T. and Horikawa, Y. (1996) Bioorg. Med. Chem. Lett., 6, 763-766.
143. Hermans, E.; Nahorski, S.R. and Challiss, R.A. (1998) Neuropharmacology, 37, 1645-1647.
144. Johnson, M.P.; Nisenbaum, E.S.; Large, T.H.; Ernkey, R.; Baez, M. and Kingston, A.E. (2004) Biochem. Soc. Trans., 32, 881-887.
145. Ritzén, A.; Mathiesen, J.M. and Thomsen, C. (2005) Basic Clin. Pharmacol. Toxicol., 97, 202-213.
146. Varney, M.A.; Cosford, N.D.; Jachec, C.; Rao, S.P.; Sacaan, A.; Lin, F.F.; Bleicher, L.; Santori, E.M.; Flor, P.J.; Allgeier, H.; Gasparini, F.; Kuhn, R.; Hess, S.D.; Veli elebi, G. and Johnson, E.C. (1999) J. Pharmacol. Exp. Ther., 290, 170-181.
147. Gasparini, F.; Lingenhöhl, K.; Stoehr, N.; Flor, P.J.; Heinrich, M.; Vranesic, I.; Biollaz, M.; Allgeier, H.; Heckendorn, R.; Urwyler, S.; Varney, M.A.; Johnson, E.C.; Hess, S.D.; Rao, S.P.; Sacaan, A.I.; Santori, E.M.; Veliçelebi, G. and Kuhn, R. (1999) Neuropharmacology, 38, 1493-1503.
148. Cosford, N.D.; Tehrani, L.; Roppe, J.; Schweiger, E.; Smith, N.D.; Anderson, J.; Bristow, L.; Brodkin, J.; Jiang, X.; McDonald, I.; Rao, S.; Washburn, M. and Varney, M.A. (2003) J. Med. Chem., 46, 204-206.
149. Kolczewski, S.; Adam, G.; Stadler, H.; Mutel, V.; Wichmann, J. and Woltering, T. (1999) Bioorg. Med. Chem. Lett., 9, 2173-2176.
150. Adam, G.; Kolczewski, S.; Ohresser, S.; Wichmann, J.; Woltering, T. and Mutel, V. (1999) Neuropharmacology, 10, A1-0.
151. Stachowicz, K.; Klak, K.; Klodzinska, A.; Chojnacka-Wojcik, E. and Pilc, A. (2004) Eur. J. Pharmacol., 498, 153-156.
152. Kinney, G.G.; O'Brien, J.A.; Lemaire, W.; Burno, M.; Bickel, D.J.; Clements, M.K.; Chen, T.B.; Wisnoski, D.D.; Lindsley, C.W.; Tiller, P.R.; Smith, S.; Jacobson, M.A.; Sur, C.; Duggan, M.E.; Pettibone, D.J.; Conn, P.J. and Williams, D.L., Jr. (2005) J. Pharmacol. Exp. Ther., 313, 199-206.
153. Spooren, W.; Ballard, T.; Gasparini, F.; Amalric, M.; Mutel, V. and Schreiber, R. (2003) Behav. Pharmacol., 14, 257-277.
154. Gasparini, F.; Kuhn, R. and Pin, J.P. (2002) Curr. Opin. Pharmacol., 2, 43-49.
155. Spooren, W. and Gasparini, F. (2004) Drug News Perspect, 17, 251-257.
156. Chiechio, S.; Copani, A.; Melchiorri, D.; Canudas, A.M.; Storto, M.; Calvani, M.; Nicolai, R. and Nicoletti, F. (2004) J. Endocrinol. Invest., 27, 171-176.
157. Moldrich, R.X.; Chapman, A.G.; De Sarro, G. and Meldrum, B.S. (2003) Eur. J. Pharmacol., 476, 3-16.
158. Costantino, G.; Macchiarulo, A. and Pellicciari, R. (2001) Expert Opin Ther Targets, 5, 669-683.
159. Flor, P.J.; Battaglia, G.; Nicoletti, F.; Gasparini, F. and Bruno, V. (2002) Adv. Exp. Med. Biol., 513, 197-223.
160. Wojcik, W.J. and Neff, N.H. (1984) Mol. Pharmacol., 25, 24-28.
161. Karbon, E.W. and Enna, S.J. (1985) Mol. Pharmacol., 27, 53-59.
162. Hill, D.R. (1985) Br. J. Pharmacol., 84, 249-257.
163. Bowery, N.G.; Bettler, B.; Froesti, W.; Gallagher, J.P.; Marshall, F.; Raiteri, M.; Bonner, T.I. and Enna, S.J. (2002) Pharmacol. Rev., 54, 247-264.
164. Froestl, W.; Mickel, S.J.; Hall, R.G.; von Sprecher, G.; Strub, D.; Baumann, P.A.; Brugger, F.; Gentsch, C.; Jaekel, J.; Olpe, H.R.; Rihs, G.; Vassout, A.; Waldmeier, P.C. and Bittiger, H. (1995) J. Med. Chem., 38, 3297-3312.
165. Malitschek, B.; Ruegg, D.; Heid, J.; Kaupmann, K.; Bittiger, H.; Fröstl, W.; Bettler, B. and Kuhn, R. (1998) Mol. Cell. Neurosci., 12, 56-64.
166. Ng, G.Y.; Bertrand, S.; Sullivan, R.; Ethier, N.; Wang, J.; Yergey, J.; Belley, M.; Trimble, L.; Bateman, K.; Alder, L.; Smith, A.; McKernan, R.; Metters, K.; O'Neill, G.P.; Lacaille, J.C. and Hebert, T.E. (2001) Mol. Pharmacol., 59, 144-152.
167. Lanneau, C.; Green, A.; Hirst, W.D.; Wise, A.; Brown, J.T.; Donnier, E.; K, J.C.; Wood, M.; Davies, C.H. and Pangalos, M.N. (2001) Neuropharmacology, 41, 965-975.
168. Jensen, A.A.; Mosbacher, J.; Elg, S.; Lingenhoehl, K.; Lehmann, T.; Johansen, T.N.; Abrahamsen, B.; Mattsson, J.P.; Lehmann, A.; Bettler, B. and Bräuner-Osborne, H. (2002) Mol. Pharmacol., 61, 1377-1384.
169. Kerr, D.I.B.; Ong, J.; Prager, R.H.; Gynther, B.D. and Curtis, D.R. (1987) Brain Res., 405, 150-154.
170. Kerr, D.I.; Ong, J.; Johnston, G.A.; Abbenante, J. and Prager, R.H. (1989) Neurosci. Lett., 107, 239-244.
171. Kerr, D.I.; Ong, J.; Johnston, G.A.; Abbenante, J. and Prager, R.H. (1988) Neurosci. Lett., 92, 92-96.
172. Froestl, W.; Mickel, S.J.; von Sprecher, G.; Diel, P.J.; Hall, R.G.; Maier, L.; Strub, D.; Melillo, V.; Baumann, P.A.; Bemasconi, R.; Gentsch, C.; Hauser, K.; Jaekel, J.; Karlsson, G.; Klebs, K.; Maitre, L.; Marescaux, C.; Pozza, M.F.; Schmutz, M.; Steinmann, M.W.; Riezen, H.; Vassout, A.; Mondadori, C.; Oipe, H.R.; Waldmeier, P.C. and Bittiger, H. (1995) J. Med. Chem., 38, 3313-3331.
173. Froestl, W.; Bettler, B.; Bittiger, H.; Heid, J.; Kaupmann, K.; Mickel, S.J. and Strub, D. (2003) Farmaco, 58, 173-183.
174. Urwyler, S.; Mosbacher, J.; Lingenhoehl, K.; Heid, J.; Hofstetter, K.; Froestl, W.; Bettler, B. and Kaupmann, K. (2001) Mol. Pharmacol., 60, 963-971.
175. Urwyler, S.; Pozza, M.F.; Lingenhoehl, K.; Mosbacher, J.; Lampert, C.; Froestl, W.; Koller, M. and Kaupmann, K. (2003) J. Pharmacol. Exp. Ther., 307, 322-330.
176. Campbell, S.K.; Almeida, G.L.; Penn, R.D. and Corcos, D.M. (1995) Phys. Ther., 75, 352-362.
177. Bettler, B. and Brauner-Osborne, H. (2004) in Molecular Neuropharmacology: Strategies and Methods, (A. Schousboe and H. Bräuner-Osborne), Humana Press, Totowa, NJ, USA, pp. 129-146.
178. Gassmann, M.; Vigot, R.; Shahan, H.; Barbieri, S.; Bräuner-Osborne, H.; Lüthi, A.; Cryan, J.F.; Kaupmann, K. and Bettler, B. (2004) Program No. 959.3. Abstract Viewer/Itenerary Planner. Washington, DC: Society for Neuroscience,
179. Cryan, J.F. and Kaupmann, K. (2005) Trends Pharmacol. Sci., 26, 36-43.
180. Froestl, W.; Gallagher, M.; Jenkins, H.; Madrid, A.; Melcher, T.; Teichman, S.; Mondadori, C.G. and Pearlman, R. (2004) Biochem. Pharmacol., 68, 1479-1487.
181. Cryan, J.F.; Kelly, P.H.; Chaperon, F.; Gentsch, C.; Mombereau, C.; Lingenhoehl, K.; Froestl, W.; Bettler, B.; Kaupmann, K. and Spooren, W.P. (2004) J. Pharmacol. Exp. Ther., 310, 952-963.
182. Mombereau, C.; Kaupmann, K.; Froestl, W.; Sansig, G.; van der Putten, H. and Cryan, J.F. (2004) Neuropsychopharmacology, 29, 1050-1062.
183. Slattery, D.A.; Markou, A.; Froestl, W. and Cryan, J.F. (2005) Neuropsychopharmacology, 30, 2065-2072.
184. Brown, E.M.; Gamba, G.; Riccardi, D.; Lombardi, M.; Butters, R.; Kifor, O.; Sun, A.; Hediger, M.A.; Lytton, J. and Hebert, S.C. (1993) Nature, 366, 575-580.
185. Brown, E.M. and MacLeod, R.J. (2001) Physiol. Rev., 81, 239-297.
186. Brown, E.M. (1997) Horm. Res., 48, 199-208.
187. Brown, E.M. (2005) J. Clin. Endocrinol. Metab., 90, 1246-1248.
188. Pidasheva, S.; D'Souza-Li, L.; Canaff, L.; Cole, D.E. and Hendy, G.N. (2004) Hum. Mutat., 24, 107-111.
189. Pearce, S.H.; Williamson, C.; Kifor, O.; Bai, M.; Coulthard, M.G.; Davies, M.; Lewis-Barned, N.; McCredie, D.; Powell, H.; Kendall-Taylor, P.; Brown, E.M. and Thakker, R.V. (1996) N. Engl. J. Med., 335, 1115-1122.
190. Pollak, M.R.; Brown, E.M.; Chou, Y.H.; Hebert, S.C.; Marx, S.J.; Steinmann, B.; Levi, T.; Seidman, C.E. and Seidman, J.G. (1993) Cell, 75, 1297-1303.
191. Pollak, M.R.; Brown, E.M.; Estep, H.L.;.McLaine, P.N.; Kifor, O.; Park, J.; Hebert, S.C.; Seidman, C.E. and Seidman, J.G. (1994) Nat. Genet., 8, 303-307.
192. Ho, C.; Conner, D.A.; Pollak, M.R.; Ladd, D.J.; Kifor, O.; Warren, H.B.; Brown, E.M.; Seidman, J.G. and Seidman, C.E. (1995) Nat. Genet., 11, 389-394.
193. Kos, C.H.; Karaplis, A.C.; Peng, J.B.; Hediger, M.A.; Goltzman, D.; Mohammad, K.S.; Guise, T.A. and Pollak, M.R. (2003) J. Clin. Invest., 111, 1021-1028.
194. Tu, Q.; Pi, M.; Karsenty, G.; Simpson, L.; Liu, S. and Quarles, L.D. (2003) J. Clin. Invest., 111, 1029-1037.
195. Ruat, M.; Snowman, A.M.; Hester, L.D. and Snyder, S.H. (1996) J. Biol. Chem., 271, 5972-5975.
196. Brown, E.M. and MacLeod, R.J. (2001) Physiol Rev, 81, 239-297.
197. Quinn, S.J.; Ye, C.P.; Diaz, R.; Kifor, O.; Bai, M.; Vassilev, P. and Brown, E. (1997) Am. J Physiol., 273, C1315-1323.
198. Ye, C.; Ho-Pao, C.L.; Kanazirska, M.; Quinn, S.; Rogers, K.; Seidman, C.E.; Seidman, J.G.; Brown, E.M. and Vassilev, P.M. (1997) J. Neurosci. Res., 47, 547-554.
199. Quinn, S.J.; Kifor, O.; Trivedi, S.; Diaz, R.; Vassilev, P. and Brown, E. (1998) J. Biol. Chem., 273, 19579-19596.
200. Conigrave, A.D.; Quinn, S.J. and Brown, E.M. (2000) Proc. Natl. Acad. Sci. USA, 97, 4814-4819.
201. Conigrave, A.D.; Franks, A.H.; Brown, E.M. and Quinn, S.J. (2002) Eur. J. Clin. Nutr., 56, 1072-1080.
202. Nemeth, E.F.; Steffey, M.E.; Hammerland, L.G.; Hung, B.C.P.; Van Wagenen, B.C.; DelMar, E.G. and Balandrin, M.F. (1998) Proc. Natl. Acad. Sci. USA, 95, 4040-4045.
203. Fox, J.; Lowe, S.H.; Petty, B.A. and Nemeth, E.F. (1999) J. Pharmacol. Exp. Ther., 290, 473-479.
204. Silverberg, S.J.; Bone, H.G.; Marriott, T.B.; Locker, F.G.; Thys-Jacobs, S.; Dziem, G.; Kaatz, S.; Sangumetti, E.L. and Bilezikian, J.P. (1997) N. Engl. J. Med., 337, 1506-1510.
205. Nemeth, E.F.; DelMar, E.G.; Heaton, W.L.; Miller, M.A.; Lambert, L.D.; Conklin, R.L.; Gowen, M.; Gleason, J.G.; Bhatnagar, P.K. and Fox, J. (2001) J. Pharmacol. Exp. Ther., 299, 323-331.
206. Miedlich, S.U.; Gama, L.; Seuwen, K.; Wolf, R.M. and Breitwieser, G.E. (2004) J. Biol. Chem, 279, 7254-7263.
207. Petrel, C.; Kessler, A.; Maslah, F.; Dauban, P.; Dodd, R.H.; Rognan, D. and Ruat, M. (2003) J. Biol. Chem., 278, 49487-49494.
208. Arey, B.J.; Seethala, R.; Ma, Z.; Fura, A.; Morin, J.; Swartz, J.; Vyas, V.; Yang, W.; Dickson, J.K., Jr. and Feyen, J.H. (2005) Endocrinology, 146, 2015-2022.
209. Nemeth, E.F.; Steffey, M.E. and Fox, J. (1996) Pediatr. Nephrol, 10, 275-279.
210. Gowen, M.; Stroup, G.B.; Dodds, R.A.; James, I.E.; Votta, B.J.; Smith, B.R.; Bhatnagar, P.K.; Lago, A.M.; Callahan, J.F.; Delmar, E.G.; Miller, M.A.; Nemeth, E.F. and Fox, J. (2000) J. Clin. Invest., 105, 1595-1604.
211. Wellendorph, P. and Bräuner-Osborne, H. (2004) Gene, 335, 37-46.
212. Mitsuma, T.; Rhue, N.; Kayarna, M.; Mori, Y.; Adachi, K.; Yokoi, Y.; Ping, J.; Nogimori, T. and Hirooka, Y. (1999) Endocr. Regul, 33, 55-59.
213. van Sluijters, D.A.; Dubbelhuis, P.F.; Blommaart, E.F. and Meijer, A.J. (2000) Biochem. J, 351 Pt 3, 545-550.
214. Civelli, Q. (2005) Trends Pharmacol. Sci., 26, 15-19.
215. Civelli, O. (2005) Mol. Pharmacol, 67, 583-584.
216. He, W.; Miao, F.J.-P.; Lin, C.-H.; Schwandner, R.T.; Wang, Z.; Gao, J.; Chen, J.-H.; Tian, H. and Ling, L. (2004) Nature, 429, 188-193.
217. Kozikowski, A.P.; Steensma, D.; Araldi, G.L.; Tückmantel, W.; Wang, S.; Pshenichkin, S.; Surina, E. and Wroblewski, J.T. (1998) J. Med. Chem., 41, 1641-1650.
218. Tückmantel, W.; Kozikowski, A.P.; Wang, S.; Pshenichkin, S. and Wroblewski, J.T. (1997) Bioorg. Med. Chem. Lett., 7, 601-606.
219. Wu, S.; Wright, R.A.; Rockey, P.K.; Burgett, S.G.; Arnold, J.S.; Rosteck, P.R., Jr.; Johnson, B.G.; Schoepp, D.D. and Belagaje, R.M. (1998) Brain Res. Mol. Brain Res., 53, 88-97.
220. Brabet, I.; Mary, S.; Bockaert, J. and Pin, J.-P. (1995) Neuropharmacology, 34, 895-903.
221. Gomeza, J.; Mary, S.; Brabet, I.; Parmentier, M.L.; Restituito, S.; Bockaert J. and Pin, J.-P. (1996) Mol. Pharmacol., 50, 923-930.
222. Doherty, A.J.; Palmer, M.J.; Henley, J.M.; Collingridge, G.L. and Jane, D.E. (1997) Neuropharmacology, 36, 265-267.
223. Bräuner-Osborne, H.; Nielsen, B. and Krogsgaard-Larsen, P. (1998) Eur. J. Pharmacol., 350, 311-316.
224. Kingston, A.; Griffey, K.; Johnson, M.; Chamberlain, M.; Kelly, G.; Tomlinson, R.; Wright, R.; Johnson, B.; Schoepp, D.; Harris, J.; Clark, B.; Baker, R. and Tizzano, J. (2002) Neurosci. Lett., 330, 127.
225. Johnson, M.P.; Baez, M.; Jagdmann, G.E., Jr.; Britton, T.C.; Large, T.H.; Callagaro, D.O.; Tizzano, J.P.; Monn, J.A. and Schoepp, D.D. (2003) J. Med. Chem., 46, 3189-3192.
226. Bräuner-Osborne, H. and Krogsgaard-Larsen, P. (1998) Br. J. Pharmacol., 123, 269-274.