Confirmation of fenfluramine effect on 5-HT 1B receptor binding of 11CAZ10419369 using an equilibrium approach

Journal of Cerebral Blood Flow and Metabolism

Volumn 32, Issue 4, 2012, Pages 685-695

  Finnema, Sjoerd J ^a   Varrone, Andrea ^a   Hwang, Tzung Jeng ^a,c   Halldin, Christer ^a   Farde, Lars ^a,b  

^a KAROLINSKA INSTITUTE   (Sweden)

^b ASTRAZENECA R AND D   (Sweden)

^c NATIONAL TAIWAN UNIVERSITY   (Taiwan)

Author keywords

5 HT1B; fenfluramine; nonhuman primate; PET; serotonin

Indexed keywords

AZ 10419369; CARBON 11; FENFLURAMINE; RADIOLIGAND; SEROTONIN; SEROTONIN 1B ANTAGONIST; SEROTONIN 1B RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; FEMALE; IN VIVO STUDY; METHODOLOGY; NONHUMAN; OCCIPITAL CORTEX; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RECEPTOR BINDING; SEROTONIN BLOOD LEVEL;

ANIMALS; AZABICYCLO COMPOUNDS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; FENFLURAMINE; MACACA FASCICULARIS; OCCIPITAL LOBE; POSITRON-EMISSION TOMOGRAPHY; RECEPTOR, SEROTONIN, 5-HT1B; SEROTONIN; SEROTONIN AGENTS; SPIRO COMPOUNDS;

EID: 84859430139     PISSN: 0271678X     EISSN: 15597016     Source Type: Journal    
DOI: 10.1038/jcbfm.2011.172     Document Type: Article

References (40)

1. Andersson JD, Pierson ME, Finnema SJ, Gulyas B, Heys R, Elmore CS, Farde L, Halldin C (2010) Development of a PET radioligand for the central 5-HT1B receptor: radiosynthesis and characterization in cynomolgus monkeys of eight radiolabeled compounds. Nucl Med Biol 38: 261-72
2. Barnes NM, Sharp T (1999) A review of central 5-HT receptors and their function. Neuropharmacology 38:1083-152 (Pubitemid 29292403)
3. Breier A, Su TP, Saunders R, Carson RE, Kolachana BS, de Bartolomeis A, Weinberger DR, Weisenfeld N, Malhotra AK, Eckelman WC, Pickar D (1997) Schizophrenia is associated with elevated amphetamine-induced synaptic dopamine concentrations: evidence from a novel positron emission tomography method. Proc Natl Acad Sci USA 94:2569-74 (Pubitemid 27136916)
4. Carson RE, Channing MA, Blasberg RG, Dunn BB, Cohen RM, Rice KC, Herscovitch P (1993) Comparison of bolus and infusion methods for receptor quantitation: application to [18F]cyclofoxy and positron emission tomography. J Cereb Blood Flow Metab 13:24-42 (Pubitemid 23016600)
5. Carson RE, Breier A, de Bartolomeis A, Saunders RC, Su TP, Schmall B, Der MG, Pickar D, Eckelman WC (1997) Quantification of amphetamine-induced changes in [11C]raclopride binding with continuous infusion. J Cereb Blood Flow Metab 17:437-47 (Pubitemid 27188540)
6. Clark JD, Baldwin RL, Bayne KA, Brown MJ, Gebhart GF, Gonder JC, Gwathmey JK, Keeling ME, Kohn DF, Robb JW, Smith OA, Steggerda J-AD, Vande Bergh JL (1996) Guide for the Care and Use of Laboratory Animals. Washington, DC: The National Academies Press
7. Cosgrove KP, Kloczynski T, Nabulsi N, Weinzimmer D, Lin SF, Staley JK, Bhagwagar Z, Carson RE (2011) Assessing the sensitivity of [(11) C]p943, a novel 5-HT(IB) radioligand, to endogenous serotonin release. Synapse 65:1113-7
8. Engel G, Gothert M, Hoyer D, Schlicker E, Hillenbrand K (1986) Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites. Naunyn Schmiedebergs Arch Pharmacol 332:1-7 (Pubitemid 16149704)
9. Finnema SJ, Varrone A, Hwang TJ, Gulyas B, Pierson ME, Halldin C, Farde L (2010) Fenfluramine-induced serotonin release decreases [11C]AZ10419369 binding to 5-HT1B-receptors in the primate brain. Synapse 64:573-7
10. Garattini S, Mennini T, Bendotti C, Invernizzi R, Samanin R (1986) Neurochemical mechanism of action of drugs which modify feeding via the serotoninergic system. Appetite 7(Suppl):15-38 (Pubitemid 16030862)
11. Göthert M, Schlicker E, Fink K, Classen K (1987) Effects of RU 24969 on serotonin release in rat brain cortex: further support for the identity of serotonin autoreceptors with 5-HT1B sites. Arch Int Pharmacodyn Ther 288:31-42 (Pubitemid 17134784)
12. Hume S, Hirani E, Opacka-Juffry J, Myers R, Townsend C, Pike V, Grasby P (2001) Effect of 5-HT on binding of [(11)C] WAY 100635 to 5-HT(IA) receptors in rat brain, assessed using in vivo microdialysis nd PET after fenfluramine. Synapse 41:150-9
13. Innis RB, Cunningham VJ, Delforge J, Fujita M, Gjedde A, Gunn RN, Holden J, Houle S, Huang SC, Ichise M, Iida H, Ito H, Kimura Y, Koeppe RA, Knudsen GM, Knuuti J, Lammertsma AA, Laruelle M, Logan J, Maguire RP, Mintun MA, Morris ED, Parsey R, Price JC, Slifstein M, Sossi V, Suhara T, Votaw JR, Wong DF, Carson RE (2007) Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab 27:1533-9 (Pubitemid 47301451)
14. Ito H, Hietala J, Blomqvist G, Halldin C, Farde L (1998) Comparison of the transient equilibrium and continuous infusion method for quantitative PET analysis of [11C]raclopride binding. J Cereb Blood Flow Metab 18:941-50
15. Karlsson P, Farde L, Halldin C, Swahn CG, Sedvall G, Foged C, Hansen KT, Skrumsager B (1993) PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor. Psychopharmacology (Berl) 113:149-56 (Pubitemid 24001986)
16. Koepp MJ, Gunn RN, Lawrence AD, Cunningham VJ, Dagher A, Jones T, Brooks DJ, Bench CJ, Grasby PM (1998) Evidence for striatal dopamine release during a video game. Nature 393:266-8 (Pubitemid 28261725)
17. Laruelle M (2000) Imaging synaptic neurotransmission with in vivo binding competition techniques: a critical review. J Cereb Blood Flow Metab 20:423-51 (Pubitemid 30164887)
18. Laruelle M, Abi-Dargham A, van Dyck CH, Gil R, D'Souza CD, Erdos J, McCance E, Rosenblatt W, Fingado C, Zoghbi SS, Baldwin RM, Seibyl JP, Krystal JH, Charney DS, Innis RB (1996) Single photon emission computerized tomography imaging of amphetamineinduced dopamine release in drug-free schizophrenic subjects. Proc Natl Acad Sci USA 93:9235-40
19. Lassen NA (1992) Neuroreceptor quantitation in vivo by the steady-state principle using constant infusion or bolus injection of radioactive tracers. J Cereb Blood Flow Metab 12:709-16
20. Maier DL, Sobotka-Briner C, Ding M, Powell ME, Jiang Q, Hill G, Heys JR, Elmore CS, Pierson ME, Mrzljak L (2009) [N-methyl-3H3]AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy. J Pharmacol Exp Ther 330:342-51
21. Maura G, Roccatagliata E, Raiteri M (1986) Serotonin autoreceptor in rat hippocampus: pharmacological characterization as a subtype of the 5-HT1 receptor. Naunyn Schmiedebergs Arch Pharmacol 334:323-6 (Pubitemid 17056372)
22. Mennini T, Bizzi A, Caccia S, Codegoni A, Fracasso C, Frittoli E, Guiso G, Padura IM, Taddei C, Uslenghi A, Garattini S (1991) Comparative studies on the anorectic activity of d-fenfluramine in mice, rats, and guinea pigs. Naunyn Schmiedebergs Arch Pharmacol 343:483-90
23. Milak MS, Severance AJ, Prabhakaran J, Kumar JS, Majo VJ, Ogden RT, Mann JJ, Parsey RV (2010) In vivo serotoninsensitive binding of [11C]CUMI-101: a serotonin 1A receptor agonist positron emission tomography radiotracer. J Cereb Blood Flow Metab 31:243-9
24. Paterson LM, Tyacke RJ, Nutt DJ, Knudsen GM (2010) Measuring endogenous 5-HT release by emission tomography: promises and pitfalls. J Cereb Blood Flow Metab 30:1682-706
25. Pierson ME, Andersson J, Nyberg S, McCarthy DJ, Finnema SJ, Varnas K, Takano A, Karlsson P, Gulyas B, Medd AM, Lee CM, Powell ME, Heys JR, Potts W, Seneca N, Mrzljak L, Farde L, Halldin C (2008) [11C]AZ10419369: a selective 5-HT1B receptor radioligand suitable for positron emission tomography (PET). Characterization in the primate brain. Neuroimage 41:1075-85
26. Ridler K, Plisson C, Rabiner EA, Gunn RN, Easwaramoorthy B, Abi-Dargham A, Laruelle M, Slifstein M (2011) Characterization of in vivo pharmacological properties and sensitivity to endogenous serotonin of [(11) C] P943: a positron emission tomography study in Papio anubis. Synapse 65:1119-27
27. Rudnick G, Clark J (1993) From synapse to vesicle: the reuptake and storage of biogenic amine neurotransmitters. Biochim Biophys Acta 1144:249-63 (Pubitemid 23290252)
28. Sarhan H, Fillion G (1999) Differential sensitivity of 5-HT1B auto and heteroreceptors. Naunyn Schmiedebergs Arch Pharmacol 360:382-90 (Pubitemid 29502986)
29. Sarhan H, Grimaldi B, Hen R, Fillion G (2000) 5-HT1B receptors modulate release of [3H]dopamine from rat striatal synaptosomes: further evidence using 5-HT moduline, polyclonal 5-HT1B receptor antibodies and 5-HT1B receptor knock-out mice. Naunyn Schmiedebergs Arch Pharmacol 361:12-8 (Pubitemid 30064648)
30. Sari Y, Miquel MC, Brisorgueil MJ, Ruiz G, Doucet E, Hamon M, Verge D (1999) Cellular and subcellular localization of 5-hydroxytryptamine1B receptors in the rat central nervous system: immunocytochemical, autoradiographic and lesion studies. Neuroscience 88: 899-915 (Pubitemid 28518266)
31. Tomasi G, Nabulsi N, Weinzimmer D, Sandiego C, Gallezot JD, Wang E, McLean S, Huang Y, Ding Y, Carson RE (2008) In vivo Scatchard analysis of bolus/infusion 5-HT1B studies with [11C]P943: comparison between SRTM and equilibrium methods. Neuroimage 41:T16
32. Udo de Haes JI, Bosker FJ, Van Waarde A, Pruim J, Willemsen AT, Vaalburg W, Den Boer JA (2002) 5-HT(1A) receptor imaging in the human brain: effect of tryptophan depletion and infusion on [(18)F]MPPF binding. Synapse 46:108-15
33. Udo de Haes JI, Harada N, Elsinga PH, Maguire RP, Tsukada H (2006) Effect of fenfluramine-induced increases in serotonin release on [18F]MPPF binding: a continuous infusion PET study in conscious monkeys. Synapse 59:18-26 (Pubitemid 41706151)
34. Varnäs K, Hall H, Bonaventure P, Sedvall G (2001) Autoradiographic mapping of 5-HT(1B) and 5-HT(1D) receptors in the post mortem human brain using [(3)H]GR 125743. Brain Res 915:47-57 (Pubitemid 32907491)
35. Varnäs K, Halldin C, Hall H (2004) Autoradiographic distribution of serotonin transporters and receptor subtypes in human brain. Hum Brain Mapp 22:246-60 (Pubitemid 38891003)
36. Varnäs K, Nyberg S, Halldin C, Varrone A, Takano A, Karlsson P, Andersson J, McCarthy D, Smith M, Pierson ME, Soderstrom J, Farde L (2011a) Quantitative analysis of [11C]AZ10419369 binding to 5-HT1B receptors in human brain. J Cereb Blood Flow Metab 31:113-23
37. Varnäs K, Nyberg S, Karlsson P, Pierson ME, Kagedal M, Cselenyi Z, McCarthy D, Xiao A, Zhang M, Halldin C, Farde L (2011b) Dose-dependent binding of AZD3783 to brain 5-HT1B receptors in non-human primates and human subjects: a positron emission tomography study with [11C]AZ10419369. Psychopharmacology (Berl) 213:533-45
38. Varrone A, Sjoholm N, Eriksson L, Gulyas B, Halldin C, Farde L (2009) Advancement in PET quantification using 3D-OP-OSEM point spread function reconstruction with the HRRT. Eur J Nucl Med Mol Imaging 36:1639-50
39. Volkow ND, Wang GJ, Fowler JS, Logan J, Schlyer D, Hitzemann R, Lieberman J, Angrist B, Pappas N, MacGregor R, Burr G, Cooper T, Wolf AP (1994) Imaging endogenous dopamine competition with [11C]raclopride in the human brain. Synapse 16:255-62 (Pubitemid 24111524)
40. Zimmer L, Mauger G, Le Bars D, Bonmarchand G, Luxen A, Pujol JF (2002) Effect of endogenous serotonin on the binding of the 5-hT1A PET ligand 18F-MPPF in the rat hippocampus: kinetic beta measurements combined with microdialysis. J Neurochem 80:278-86 (Pubitemid 34809373)