ترک و درمان اعتیاد به محرک کریستال شیشه با ترکیبات تریپتامین تز ما که هیپوتز دیگران است ؟
آخرین روش درمان و ترک اعتیاد مواد مخدر ومحرک (شیشه ) که من پیشنهاد می کنم
زمانی که اردیبهشت امسال من پستی درباره ترک متامفتامین (شیشه ) با استفاده از داروهای سایکدلیک (ترکیبات سایلوسبین ) نوشتم بسیاری نگاه ناباورانه به ان داشتند
امروز تازه دیگران در دانشگاه های خارج از کشور به فکر هیپوتز دادن درباره روش ترک اعتیاد به شیشه (متامفتامین ) هستند که من قبلا هم تز ان را داده ام و هم انرا عملا بر روی معتادان به شیشه بطور موفقیت امیز انجام دادم
سایلوسبین دارای یک حلقه تریپتامین و اگونیست گیرنده 5-HT است
سایلوسبین دارای یک حلقه تریپتامین و اگونیست گیرنده 5-HT است
چکیده
. شواهد قانع کننده ای برای این نظریه که گیرنده 2B 5-HT نقش مستقیم و مهمی در مکانیسم های اعمال متامفتامین (مت) و اکستاسی (3،4-متیلن دی (MDMA) وجود دارند که منجر به اعتیاد به انها می شود .. دخالت گیرنده های 5-HT 1A در تمام عواقب بیوشیمیایی و رفتاری مانند اضطراب، افسردگی، اختلال در حافظه، و اختلال شناختی، ناشی از مصرف طولانی مدت و اعتیاد به MDMA، نیز به صراحت مشخص شده است. . بر اساس این حقایق، یک فرضیه گیرنده دو ب اساس آنتاگونیست postsynaptic 5-HT گیرنده 2B و 5-HT 1A فعالیت آگونیست گیرنده در سیستم عصبی مرکزی (CNS)، ارائه شده است.
Dual, Postsynaptic 5-HT2B Antagonist and 5-HT1A Agonist Approach to the Treatment of METH/MDMA Addiction and Related Behavioral Disorders. Part 1. The Hypothesis.
Abstract
Abstract
There is compelling evidence to the theory that the 5-HT2B receptor plays a direct and crucial role in the mechanisms of actions of methamphetamine (METH) and of 3,4-methylenedioxymethamphetamine (MDMA) leading to addiction. The involvement of 5-HT1A receptors in all of the biochemical and behavioural consequences such as anxiety, depression, memory impairment, and cognitive dysfunction, resulting from long-term METH/MDMA abuse, has also been unequivocally established. On the basis of these facts, a dual receptor hypothesis based on postsynaptic 5-HT2B receptor antagonist and 5-HT1A receptor agonist activities in the central nervous system (CNS), is proposed.
There is compelling evidence to the theory that the 5-HT2B receptor plays a direct and crucial role in the mechanisms of actions of methamphetamine (METH) and of 3,4-methylenedioxymethamphetamine (MDMA) leading to addiction. The involvement of 5-HT1A receptors in all of the biochemical and behavioural consequences such as anxiety, depression, memory impairment, and cognitive dysfunction, resulting from long-term METH/MDMA abuse, has also been unequivocally established. On the basis of these facts, a dual receptor hypothesis based on postsynaptic 5-HT2B receptor antagonist and 5-HT1A receptor agonist activities in the central nervous system (CNS), is proposed.
Full Text:
PDFReferences
Report on Methamphetamine. National Institute of Drug Abuse (NIH). Addiction Science: From Molecules to Managed Care (Third Edition). 2013.
Itzhak, Y, Achat-Mendez, C. Methamphetamine and MDMA (Ecstacy) neurotoxicity: 'Of mice and men.' IUBMB Life 2004; 56:249-255.
http://dx.doi.org/10.1080/15216540410001727699
PMid:15370888
ReichelCM, Schwendt M, McGinty JF, See RE. Loss of object recognition memory produced by extended access to methamphetamine self-administration is reversed by positive allosteric modulation of metabotropic glutamate receptor Neuropsychopharm 2011; 36:782.
Report on MDMA. National Institute of Drug Abuse (NIH). Research Reports Service. 2006. Publication Number 06-4728.
Methamphetamine abuse in 2009. National Institute of Drug Abuse (NIH), The Science of Drug Abuse and Health. Drug Facts: Treatment Statistics. 2011.
The economic impact of illicit drug use on American Society. National Drug Intelligence Center. U.S. Department of Justice. 2011
Rudnic G, Wall SC. The molecular mechanism of 'Ecstasy' [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proc Natl Acad SciUSA 1992;89:1817-1821.
http://dx.doi.org/10.1073/pnas.89.5.1817
Crespi D, Mennini T, Gobbi M. Carrier-dependent and Ca ion-dependent 5-HT and dopamine release induced by (+)-amphetamine, 3,4-methylenedioxymethamphetamine, p-chloroamphetamine, and (+)-fenfluramine. Br J Pharmacol 1997;121:1735-1743.
http://dx.doi.org/10.1038/sj.bjp.0701325
PMid:9283711 PMCid:PMC1564879
Fleckstein AE, Volz TJ, Riddle EL, Gibb JW, Hanson GR. New insights into the mechanism of action of amphetamines. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
http://dx.doi.org/10.1146/annurev.pharmtox.47.120505.105140
PMid:17209801
Cruickshank CC, Dyer KR. A review of the clinical pharmacology of methamphetamine Addiction 2009;104:1985-1099.
http://dx.doi.org/10.1111/j.1360-0443.2009.02564.x
PMid:19426289
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. Plos One 2009;4:e7952.
http://dx.doi.org/10.1371/journal.pone.0007952
PMid:19956756 PMCid:PMC2775951
Ago Y, Nakamura S, Baba A, Matsuda, T. Neuropsychotoxicity of abused drugs: effects of serotonin receptors ligands on methamphetamine- and cocaine-induced behavioral sensitization in mice. J Pharm Sci Japan 2008; 106:15-21.
http://dx.doi.org/10.1254/jphs.FM0070121
Ball KT, Rebec GV. Role of 5-HT2A and 5-HT2B/C receptors in the acute effects of 3,4-methylenedioxymethamphetamine (MDMA) on striatal single-unit activity and locomotion in freely moving rats. Psychopharmacol. (Berlin) 2005;181:676-687.
http://dx.doi.org/10.1007/s00213-005-0038-z
PMid:16001122
Bankson MG, Yamamoto BK. Serotonin-GABA interactions modulate MDMA-induced mesolimbic dopamine release. J Neurochem. 2004;91:852-859.
http://dx.doi.org/10.1111/j.1471-4159.2004.02763.x
PMid:15525339
Auclair AL, Cathala A, Sarazzin F, Depoortere R, Piazza PV, Newmn-Tancredi A, Spampinato U. The central serotonin2B receptor: a new pharmacological target to modulate mesoaccumbens dopaminergic pathway activity. J Neurochem 2010;114:1323-1332.
PMid:20534001
Fleckstein AE, Volz TJ, Riddle EL, Gibb JE. New insight into the mechanism of action of amphetamine. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
http://dx.doi.org/10.1146/annurev.pharmtox.47.120505.105140
PMid:17209801
Bevilacqua L, Doly S, Kaprio J, Yuan Q,Tikkanen R, Paunio T, ZhouZ, et al. A population-specific HTR2B stop codon predisposes to severe impulsivity. Nature 2010;468:1061-1068.
http://dx.doi.org/10.1038/nature09629
PMid:21179162 PMCid:PMC3183507
Bonhaus WB, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Brit J Pharmacol 1995;
Cohen I, Fuller ML, Kurz RW, Mabry TE, Nelson DL, Audia JE. LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J Ser Res 1996; 3:131-134.
Poissonnet G, ParmentierJG, Boutin JA, Goldstein S. The Emergence of Selective 5-HT2B Antagonists. Structures, Activities, Potential Therapeutic Applications. Mini-Reviews Med Chem 2004; 4:325-330.
http://dx.doi.org/10.2174/1389557043487312
Watts SW, Fink GD. LY272015 is antihypertensive in DOCA-salt-hypersentive rats. Am J Physiol 1999; 276:944-952.
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. J Neurosci 2008;28:2933-2940.
http://dx.doi.org/10.1523/JNEUROSCI.5723-07.2008
PMid:18337424
Muller CP, Carey RJ, Huston JP, DeSouza Silva MA. Prog Neurobiol 2007;81:133-178.
http://dx.doi.org/10.1016/j.pneurobio.2007.01.001
PMid:17316955
Fresquet A, Sust, M. L. A. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. The Annals of Pharmcotherapy 2000;34:147-153.
http://dx.doi.org/10.1345/aph.19041
Graf P, Joffe R, Kennedy S, Persad E, Syrotiuk J, Bradford D. An open study of Flesinoxan, a 5-HT1A agonist, in treatment of of resistant depression. International Clinical Psychopharmacology 1993; 8:167-172.
http://dx.doi.org/10.1097/00004850-199300830-00005
Mauler F, Horvath E. Neuroprotective efficay of repinotan hydrochloride in models of stroke and traumatic brain injury. Journal of Central Flow and Metabolism 2005; 25:451-459.
http://dx.doi.org/10.1038/sj.jcbfm.9600038
PMid:15674237
Rawls SM, Shah A, Ayoub G, Raffa RB. 5-HT1A-like receptor activation inhibits abstinence-induced methamphetamine withdrawal in planarians. Neurosci Lett 2010; 484: 113-117.
http://dx.doi.org/10.1016/j.neulet.2010.08.027
PMid:20709144 PMCid:PMC2942978
Bandyopadhyaya A, Rajagopalan DR, Rath NP, Herrold A, Rajagopalan R, Napier TC, Tedford CE, Rajagopalan P. The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic. Med Chem Comm 2012; 3:580-583.
http://dx.doi.org/10.1039/c2md00311b
Margolis BJ, Swidorski JJ, Rogers BN. An efficient assembly of heterobenzazepine ring system utilizing an intramolecular palladium-catalyzed cycloamination. J Org Chem 2003; 68:644-647.
http://dx.doi.org/10.1021/jo026546g
PMid:12530903
The binding studies were conducted by the Psychoactive Drug Screening Program (PDSP) of University of North Carolina Chapel Hill sponsored by the National Institute of Mental Health (NIMH). National Institues of Health, USA.
Porsolt RD, Bertin A, Jaffre M.Animal model of depression. Biomedicine 1979; 30:139-140.
PMid:573643
Petit-Demouliere B, Chenu F, Bouri M. Forced swimming test in mice: a review of antidepressant activity. Pyschopharm 2005; 177:245-255.
http://dx.doi.org/10.1007/s00213-004-2048-7
PMid:15609067
Itzhak, Y, Achat-Mendez, C. Methamphetamine and MDMA (Ecstacy) neurotoxicity: 'Of mice and men.' IUBMB Life 2004; 56:249-255.
http://dx.doi.org/10.1080/15216540410001727699
PMid:15370888
ReichelCM, Schwendt M, McGinty JF, See RE. Loss of object recognition memory produced by extended access to methamphetamine self-administration is reversed by positive allosteric modulation of metabotropic glutamate receptor Neuropsychopharm 2011; 36:782.
Report on MDMA. National Institute of Drug Abuse (NIH). Research Reports Service. 2006. Publication Number 06-4728.
Methamphetamine abuse in 2009. National Institute of Drug Abuse (NIH), The Science of Drug Abuse and Health. Drug Facts: Treatment Statistics. 2011.
The economic impact of illicit drug use on American Society. National Drug Intelligence Center. U.S. Department of Justice. 2011
Rudnic G, Wall SC. The molecular mechanism of 'Ecstasy' [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proc Natl Acad SciUSA 1992;89:1817-1821.
http://dx.doi.org/10.1073/pnas.89.5.1817
Crespi D, Mennini T, Gobbi M. Carrier-dependent and Ca ion-dependent 5-HT and dopamine release induced by (+)-amphetamine, 3,4-methylenedioxymethamphetamine, p-chloroamphetamine, and (+)-fenfluramine. Br J Pharmacol 1997;121:1735-1743.
http://dx.doi.org/10.1038/sj.bjp.0701325
PMid:9283711 PMCid:PMC1564879
Fleckstein AE, Volz TJ, Riddle EL, Gibb JW, Hanson GR. New insights into the mechanism of action of amphetamines. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
http://dx.doi.org/10.1146/annurev.pharmtox.47.120505.105140
PMid:17209801
Cruickshank CC, Dyer KR. A review of the clinical pharmacology of methamphetamine Addiction 2009;104:1985-1099.
http://dx.doi.org/10.1111/j.1360-0443.2009.02564.x
PMid:19426289
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. Plos One 2009;4:e7952.
http://dx.doi.org/10.1371/journal.pone.0007952
PMid:19956756 PMCid:PMC2775951
Ago Y, Nakamura S, Baba A, Matsuda, T. Neuropsychotoxicity of abused drugs: effects of serotonin receptors ligands on methamphetamine- and cocaine-induced behavioral sensitization in mice. J Pharm Sci Japan 2008; 106:15-21.
http://dx.doi.org/10.1254/jphs.FM0070121
Ball KT, Rebec GV. Role of 5-HT2A and 5-HT2B/C receptors in the acute effects of 3,4-methylenedioxymethamphetamine (MDMA) on striatal single-unit activity and locomotion in freely moving rats. Psychopharmacol. (Berlin) 2005;181:676-687.
http://dx.doi.org/10.1007/s00213-005-0038-z
PMid:16001122
Bankson MG, Yamamoto BK. Serotonin-GABA interactions modulate MDMA-induced mesolimbic dopamine release. J Neurochem. 2004;91:852-859.
http://dx.doi.org/10.1111/j.1471-4159.2004.02763.x
PMid:15525339
Auclair AL, Cathala A, Sarazzin F, Depoortere R, Piazza PV, Newmn-Tancredi A, Spampinato U. The central serotonin2B receptor: a new pharmacological target to modulate mesoaccumbens dopaminergic pathway activity. J Neurochem 2010;114:1323-1332.
PMid:20534001
Fleckstein AE, Volz TJ, Riddle EL, Gibb JE. New insight into the mechanism of action of amphetamine. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
http://dx.doi.org/10.1146/annurev.pharmtox.47.120505.105140
PMid:17209801
Bevilacqua L, Doly S, Kaprio J, Yuan Q,Tikkanen R, Paunio T, ZhouZ, et al. A population-specific HTR2B stop codon predisposes to severe impulsivity. Nature 2010;468:1061-1068.
http://dx.doi.org/10.1038/nature09629
PMid:21179162 PMCid:PMC3183507
Bonhaus WB, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Brit J Pharmacol 1995;
Cohen I, Fuller ML, Kurz RW, Mabry TE, Nelson DL, Audia JE. LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J Ser Res 1996; 3:131-134.
Poissonnet G, ParmentierJG, Boutin JA, Goldstein S. The Emergence of Selective 5-HT2B Antagonists. Structures, Activities, Potential Therapeutic Applications. Mini-Reviews Med Chem 2004; 4:325-330.
http://dx.doi.org/10.2174/1389557043487312
Watts SW, Fink GD. LY272015 is antihypertensive in DOCA-salt-hypersentive rats. Am J Physiol 1999; 276:944-952.
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. J Neurosci 2008;28:2933-2940.
http://dx.doi.org/10.1523/JNEUROSCI.5723-07.2008
PMid:18337424
Muller CP, Carey RJ, Huston JP, DeSouza Silva MA. Prog Neurobiol 2007;81:133-178.
http://dx.doi.org/10.1016/j.pneurobio.2007.01.001
PMid:17316955
Fresquet A, Sust, M. L. A. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. The Annals of Pharmcotherapy 2000;34:147-153.
http://dx.doi.org/10.1345/aph.19041
Graf P, Joffe R, Kennedy S, Persad E, Syrotiuk J, Bradford D. An open study of Flesinoxan, a 5-HT1A agonist, in treatment of of resistant depression. International Clinical Psychopharmacology 1993; 8:167-172.
http://dx.doi.org/10.1097/00004850-199300830-00005
Mauler F, Horvath E. Neuroprotective efficay of repinotan hydrochloride in models of stroke and traumatic brain injury. Journal of Central Flow and Metabolism 2005; 25:451-459.
http://dx.doi.org/10.1038/sj.jcbfm.9600038
PMid:15674237
Rawls SM, Shah A, Ayoub G, Raffa RB. 5-HT1A-like receptor activation inhibits abstinence-induced methamphetamine withdrawal in planarians. Neurosci Lett 2010; 484: 113-117.
http://dx.doi.org/10.1016/j.neulet.2010.08.027
PMid:20709144 PMCid:PMC2942978
Bandyopadhyaya A, Rajagopalan DR, Rath NP, Herrold A, Rajagopalan R, Napier TC, Tedford CE, Rajagopalan P. The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic. Med Chem Comm 2012; 3:580-583.
http://dx.doi.org/10.1039/c2md00311b
Margolis BJ, Swidorski JJ, Rogers BN. An efficient assembly of heterobenzazepine ring system utilizing an intramolecular palladium-catalyzed cycloamination. J Org Chem 2003; 68:644-647.
http://dx.doi.org/10.1021/jo026546g
PMid:12530903
The binding studies were conducted by the Psychoactive Drug Screening Program (PDSP) of University of North Carolina Chapel Hill sponsored by the National Institute of Mental Health (NIMH). National Institues of Health, USA.
Porsolt RD, Bertin A, Jaffre M.Animal model of depression. Biomedicine 1979; 30:139-140.
PMid:573643
Petit-Demouliere B, Chenu F, Bouri M. Forced swimming test in mice: a review of antidepressant activity. Pyschopharm 2005; 177:245-255.
http://dx.doi.org/10.1007/s00213-004-2048-7
PMid:15609067
Dual, Postsynaptic 5-HT2B Antagonist and 5-HT1A Agonist Approach to the Treatment of METH/MDMA Addiction and Related Behavioral Disorders. Part 2. Proof of Concept.
Abstract
The synthesis, in vitro, and preliminary in vivo pharmacology of DDD-024, a novel, pentacyclic compound, is described. It exhibits high affinity to the 5-HT1A and good affinity to the 5-HT2B receptors and is an agonist of the former and antagonist of the latter receptor, a profile which meets with the requirements delineated in our hypothesis proposed in Part 1 (see previous paper). Further, in vivo, it was quite active in METH-seeking behavior test in rats, MDMA-induced hyperlocomotion test in mice, and Porsolt’s forced swim test in rats for antidepressant activity thereby providing definite proof of concept for our hypothesis.
Full Text:
PDFReferences
Report on Methamphetamine. National Institute of Drug Abuse (NIH). Addiction Science: From Molecules to Managed Care (Third Edition). 2013.
Itzhak, Y, Achat-Mendez, C. Methamphetamine and MDMA (Ecstacy) neurotoxicity: ‘Of mice and men.’ IUBMB Life 2004; 56:249-255.
ReichelCM, Schwendt M, McGinty JF, See RE. Loss of object recognition memory produced by extended access to methamphetamine self-administration is reversed by positive allosteric modulation of metabotropic glutamate receptor Neuropsychopharm 2011; 36:782.
Report on MDMA. National Institute of Drug Abuse (NIH). Research Reports Service. 2006. Publication Number 06-4728.
Methamphetamine abuse in 2009. National Institute of Drug Abuse (NIH), The Science of Drug Abuse and Health. Drug Facts: Treatment Statistics. 2011.
The economic impact of illicit drug use on American Society. National Drug Intelligence Center. U.S. Department of Justice. 2011
Rudnic G, Wall SC. The molecular mechanism of ‘Ecstasy’ [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proc Natl Acad SciUSA 1992;89:1817-1821.
Crespi D, Mennini T, Gobbi M. Carrier-dependent and Ca ion-dependent 5-HT and dopamine release induced by (+)-amphetamine, 3,4-methylenedioxymethamphetamine, p-chloroamphetamine, and (+)-fenfluramine. Br J Pharmacol 1997;121:1735-1743.
Fleckstein AE, Volz TJ, Riddle EL, Gibb JW, Hanson GR. New insights into the mechanism of action of amphetamines. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
Cruickshank CC, Dyer KR. A review of the clinical pharmacology of methamphetamine Addiction 2009;104:1985-1099.
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. Plos One 2009;4:e7952.
Ago Y, Nakamura S, Baba A, Matsuda, T. Neuropsychotoxicity of abused drugs: effects of serotonin receptors ligands on methamphetamine- and cocaine-induced behavioral sensitization in mice. J Pharm Sci Japan 2008; 106:15-21.
Ball KT, Rebec GV. Role of 5-HT2A and 5-HT2B/C receptors in the acute effects of 3,4-methylenedioxymethamphetamine (MDMA) on striatal single-unit activity and locomotion in freely moving rats. Psychopharmacol. (Berlin) 2005;181:676-687.
Bankson MG, Yamamoto BK. Serotonin-GABA interactions modulate MDMA-induced mesolimbic dopamine release. J Neurochem. 2004;91:852-859.
Auclair AL, Cathala A, Sarazzin F, Depoortere R, Piazza PV, Newmn-Tancredi A, Spampinato U. The central serotonin2B receptor: a new pharmacological target to modulate mesoaccumbens dopaminergic pathway activity. J Neurochem 2010;114:1323-1332.
Fleckstein AE, Volz TJ, Riddle EL, Gibb JE. New insight into the mechanism of action of amphetamine. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
Bevilacqua L, Doly S, Kaprio J, Yuan Q,Tikkanen R, Paunio T, ZhouZ, et al. A population-specific HTR2B stop codon predisposes to severe impulsivity. Nature 2010;468:1061-1068.
Bonhaus WB, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Brit J Pharmacol 1995;
Cohen I, Fuller ML, Kurz RW, Mabry TE, Nelson DL, Audia JE. LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J Ser Res 1996; 3:131-134.
Poissonnet G, ParmentierJG, Boutin JA, Goldstein S. The Emergence of Selective 5-HT2B Antagonists. Structures, Activities, Potential Therapeutic Applications. Mini-Reviews Med Chem 2004; 4:325-330.
Watts SW, Fink GD. LY272015 is antihypertensive in DOCA-salt-hypersentive rats. Am J Physiol 1999; 276:944-952.
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. J Neurosci 2008;28:2933-2940.
Muller CP, Carey RJ, Huston JP, DeSouza Silva MA. Prog Neurobiol 2007;81:133-178.
Fresquet A, Sust, M. L. A. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. The Annals of Pharmcotherapy 2000;34:147-153.
Graf P, Joffe R, Kennedy S, Persad E, Syrotiuk J, Bradford D. An open study of Flesinoxan, a 5-HT1A agonist, in treatment of of resistant depression. International Clinical Psychopharmacology 1993; 8:167-172.
Mauler F, Horvath E. Neuroprotective efficay of repinotan hydrochloride in models of stroke and traumatic brain injury. Journal of Central Flow and Metabolism 2005; 25:451-459.
Rawls SM, Shah A, Ayoub G, Raffa RB. 5-HT1A-like receptor activation inhibits abstinence-induced methamphetamine withdrawal in planarians. Neurosci Lett 2010; 484: 113-117.
Bandyopadhyaya A, Rajagopalan DR, Rath NP, Herrold A, Rajagopalan R, Napier TC, Tedford CE, Rajagopalan P. The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic. Med Chem Comm 2012; 3:580-583.
Margolis BJ, Swidorski JJ, Rogers BN. An efficient assembly of heterobenzazepine ring system utilizing an intramolecular palladium-catalyzed cycloamination. J Org Chem 2003; 68:644-647.
The binding studies were conducted by the Psychoactive Drug Screening Program (PDSP) of University of North Carolina Chapel Hill sponsored by the National Institute of Mental Health (NIMH). National Institues of Health, USA.
Porsolt RD, Bertin A, Jaffre M.Animal model of depression. Biomedicine 1979; 30:139-140.
Petit-Demouliere B, Chenu F, Bouri M. Forced swimming test in mice: a review of antidepressant activity. Pyschopharm 2005; 177:245-255.
Itzhak, Y, Achat-Mendez, C. Methamphetamine and MDMA (Ecstacy) neurotoxicity: ‘Of mice and men.’ IUBMB Life 2004; 56:249-255.
ReichelCM, Schwendt M, McGinty JF, See RE. Loss of object recognition memory produced by extended access to methamphetamine self-administration is reversed by positive allosteric modulation of metabotropic glutamate receptor Neuropsychopharm 2011; 36:782.
Report on MDMA. National Institute of Drug Abuse (NIH). Research Reports Service. 2006. Publication Number 06-4728.
Methamphetamine abuse in 2009. National Institute of Drug Abuse (NIH), The Science of Drug Abuse and Health. Drug Facts: Treatment Statistics. 2011.
The economic impact of illicit drug use on American Society. National Drug Intelligence Center. U.S. Department of Justice. 2011
Rudnic G, Wall SC. The molecular mechanism of ‘Ecstasy’ [3,4-methylenedioxy-methamphetamine (MDMA)]: serotonin transporters are targets for MDMA-induced serotonin release. Proc Natl Acad SciUSA 1992;89:1817-1821.
Crespi D, Mennini T, Gobbi M. Carrier-dependent and Ca ion-dependent 5-HT and dopamine release induced by (+)-amphetamine, 3,4-methylenedioxymethamphetamine, p-chloroamphetamine, and (+)-fenfluramine. Br J Pharmacol 1997;121:1735-1743.
Fleckstein AE, Volz TJ, Riddle EL, Gibb JW, Hanson GR. New insights into the mechanism of action of amphetamines. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
Cruickshank CC, Dyer KR. A review of the clinical pharmacology of methamphetamine Addiction 2009;104:1985-1099.
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. Plos One 2009;4:e7952.
Ago Y, Nakamura S, Baba A, Matsuda, T. Neuropsychotoxicity of abused drugs: effects of serotonin receptors ligands on methamphetamine- and cocaine-induced behavioral sensitization in mice. J Pharm Sci Japan 2008; 106:15-21.
Ball KT, Rebec GV. Role of 5-HT2A and 5-HT2B/C receptors in the acute effects of 3,4-methylenedioxymethamphetamine (MDMA) on striatal single-unit activity and locomotion in freely moving rats. Psychopharmacol. (Berlin) 2005;181:676-687.
Bankson MG, Yamamoto BK. Serotonin-GABA interactions modulate MDMA-induced mesolimbic dopamine release. J Neurochem. 2004;91:852-859.
Auclair AL, Cathala A, Sarazzin F, Depoortere R, Piazza PV, Newmn-Tancredi A, Spampinato U. The central serotonin2B receptor: a new pharmacological target to modulate mesoaccumbens dopaminergic pathway activity. J Neurochem 2010;114:1323-1332.
Fleckstein AE, Volz TJ, Riddle EL, Gibb JE. New insight into the mechanism of action of amphetamine. Ann Rev Pharmacol Toxicol 2007; 47:681-698.
Bevilacqua L, Doly S, Kaprio J, Yuan Q,Tikkanen R, Paunio T, ZhouZ, et al. A population-specific HTR2B stop codon predisposes to severe impulsivity. Nature 2010;468:1061-1068.
Bonhaus WB, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Brit J Pharmacol 1995;
Cohen I, Fuller ML, Kurz RW, Mabry TE, Nelson DL, Audia JE. LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J Ser Res 1996; 3:131-134.
Poissonnet G, ParmentierJG, Boutin JA, Goldstein S. The Emergence of Selective 5-HT2B Antagonists. Structures, Activities, Potential Therapeutic Applications. Mini-Reviews Med Chem 2004; 4:325-330.
Watts SW, Fink GD. LY272015 is antihypertensive in DOCA-salt-hypersentive rats. Am J Physiol 1999; 276:944-952.
Doly S, Valjent E, Setola V, Callebert J, Herve D, Launay J.-L, Maroteaux L. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymetamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. J Neurosci 2008;28:2933-2940.
Muller CP, Carey RJ, Huston JP, DeSouza Silva MA. Prog Neurobiol 2007;81:133-178.
Fresquet A, Sust, M. L. A. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. The Annals of Pharmcotherapy 2000;34:147-153.
Graf P, Joffe R, Kennedy S, Persad E, Syrotiuk J, Bradford D. An open study of Flesinoxan, a 5-HT1A agonist, in treatment of of resistant depression. International Clinical Psychopharmacology 1993; 8:167-172.
Mauler F, Horvath E. Neuroprotective efficay of repinotan hydrochloride in models of stroke and traumatic brain injury. Journal of Central Flow and Metabolism 2005; 25:451-459.
Rawls SM, Shah A, Ayoub G, Raffa RB. 5-HT1A-like receptor activation inhibits abstinence-induced methamphetamine withdrawal in planarians. Neurosci Lett 2010; 484: 113-117.
Bandyopadhyaya A, Rajagopalan DR, Rath NP, Herrold A, Rajagopalan R, Napier TC, Tedford CE, Rajagopalan P. The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic. Med Chem Comm 2012; 3:580-583.
Margolis BJ, Swidorski JJ, Rogers BN. An efficient assembly of heterobenzazepine ring system utilizing an intramolecular palladium-catalyzed cycloamination. J Org Chem 2003; 68:644-647.
The binding studies were conducted by the Psychoactive Drug Screening Program (PDSP) of University of North Carolina Chapel Hill sponsored by the National Institute of Mental Health (NIMH). National Institues of Health, USA.
Porsolt RD, Bertin A, Jaffre M.Animal model of depression. Biomedicine 1979; 30:139-140.
Petit-Demouliere B, Chenu F, Bouri M. Forced swimming test in mice: a review of antidepressant activity. Pyschopharm 2005; 177:245-255.
