Risperidone Dose-Dependently Increases Extracellular Concentrations of Serotonin in the Rat Frontal Cortex
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TABLE 1 Studies of Antagonist Activity in Constitutively Active
TABLE 1 Studies of antagonist activity in constitutively active receptors systems shown to demonstrate inverse agonism for at least one ligand Targets are natural Gs and constitutively active mutants (CAM) of GPCRs. Of 380 antagonists, 85% of the ligands demonstrate inverse agonism. Receptor Neutral Antagonist Inverse Agonist Reference Human β2-adrenergic Dichloroisoproterenol, pindolol, labetolol, timolol, Chidiac et al., 1996; Azzi et alprenolol, propranolol, ICI 118,551, cyanopindolol al., 2001 Turkey erythrocyte β-adrenergic Propranolol, pindolol Gotze et al., 1994 Human β2-adrenergic (CAM) Propranolol Betaxolol, ICI 118,551, sotalol, timolol Samama et al., 1994; Stevens and Milligan, 1998 Human/guinea pig β1-adrenergic Atenolol, propranolol Mewes et al., 1993 Human β1-adrenergic Carvedilol CGP20712A, metoprolol, bisoprolol Engelhardt et al., 2001 Rat α2D-adrenergic Rauwolscine, yohimbine, WB 4101, idazoxan, Tian et al., 1994 phentolamine, Human α2A-adrenergic Napthazoline, Rauwolscine, idazoxan, altipamezole, levomedetomidine, Jansson et al., 1998; Pauwels MPV-2088 (–)RX811059, RX 831003 et al., 2002 Human α2C-adrenergic RX821002, yohimbine Cayla et al., 1999 Human α2D-adrenergic Prazosin McCune et al., 2000 Rat α2-adrenoceptor MK912 RX821002 Murrin et al., 2000 Porcine α2A adrenoceptor (CAM- Idazoxan Rauwolscine, yohimbine, RX821002, MK912, Wade et al., 2001 T373K) phentolamine Human α2A-adrenoceptor (CAM) Dexefaroxan, (+)RX811059, (–)RX811059, RS15385, yohimbine, Pauwels et al., 2000 atipamezole fluparoxan, WB 4101 Hamster α1B-adrenergic -
(12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe Et Al
US 2011 01 05536A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe et al. (43) Pub. Date: May 5, 2011 (54) DOSING REGIMENASSOCATED WITH Publication Classification LONG-ACTING INUECTABLE PALIPERDONE ESTERS (51) Int. Cl. A 6LX 3/59 (2006.01) (76) Inventors: Peter H. Lewyn-Briscoe, A6IP 25/18 (2006.01) Newtown, PA (US); Cristiana Gassmann-Mayer, Pennington, NJ (US); Srihari Gopal, Belle Meade, (52) U.S. Cl. ................................................... S14/259.41 NJ (US); David W. Hough, Wallingford, PA (US); Bart M.M. Remmerie, Gent (BE); Mahesh N. (57) ABSTRACT Samtani, Flemington, NJ (US) The present application provides a method for treating (21) Appl. No.: 12/916,910 patients in need of psychiatric treatment, wherein said patient (22) Filed: Nov. 1, 2010 misses a stabilized dose of a monthly maintenance regimen of paliperidone palmitate. The present application also provides Related U.S. Application Data a method for treating psychiatric patients in need of a Switch (60) Provisional application No. 61/256,696, filed on Oct. ing treatment to paliperidone palmitate in a Sustained release 30, 2009. formulation. Patent Application Publication May 5, 2011 Sheet 1 of 6 US 2011/O105536 A1 FIG. 1 First-Order PrOCeSS Cp V CL Central (2) Zero-Order PrOCeSS Patent Application Publication May 5, 2011 Sheet 2 of 6 US 2011/O105536 A1 FIG. 2 25mgeq 50mgeq m-100mde::::: Missed doSe On WK 4. Patient returns On WK5 Missed doSe On WK 4. Patient returns On WK 6 -8-4 O 4 8 12 16 2024 -8-4 O 4 8 12 1620 24 Missed doSe On WK 4. -
Stems for Nonproprietary Drug Names
USAN STEM LIST STEM DEFINITION EXAMPLES -abine (see -arabine, -citabine) -ac anti-inflammatory agents (acetic acid derivatives) bromfenac dexpemedolac -acetam (see -racetam) -adol or analgesics (mixed opiate receptor agonists/ tazadolene -adol- antagonists) spiradolene levonantradol -adox antibacterials (quinoline dioxide derivatives) carbadox -afenone antiarrhythmics (propafenone derivatives) alprafenone diprafenonex -afil PDE5 inhibitors tadalafil -aj- antiarrhythmics (ajmaline derivatives) lorajmine -aldrate antacid aluminum salts magaldrate -algron alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol combined alpha and beta blockers labetalol medroxalol -amidis antimyloidotics tafamidis -amivir (see -vir) -ampa ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) subgroup: -ampanel antagonists becampanel -ampator modulators forampator -anib angiogenesis inhibitors pegaptanib cediranib 1 subgroup: -siranib siRNA bevasiranib -andr- androgens nandrolone -anserin serotonin 5-HT2 receptor antagonists altanserin tropanserin adatanserin -antel anthelmintics (undefined group) carbantel subgroup: -quantel 2-deoxoparaherquamide A derivatives derquantel -antrone antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine antineoplastics (arabinofuranosyl derivatives) fazarabine fludarabine aril-, -aril, -aril- antiviral (arildone derivatives) pleconaril arildone fosarilate -arit antirheumatics (lobenzarit type) lobenzarit clobuzarit -arol anticoagulants (dicumarol type) dicumarol -
Recent Advances and Concepts in the Search for Biological Correlates of Hallucinogen-Induced Altered States of Consciousness Franz X
The Heffter Review of Psychedelic Research, Volume 1, 1998 3. Recent Advances and Concepts in the Search for Biological Correlates of hallucinogen-induced Altered States of Consciousness Franz X. Vollenweider, M.D. Introduction intrusive mental activity. Specifically, the CSTC loop model suggests that a deficient thalamic “filter” Hallucinogens and related substances constitute function leads to sensory overload of the cortex a powerful experimental basis to investigate which in turn results in cognitive fragmentation and biological correlates of altered states of sensory flooding as seen in hallucinogen-induced consciousness (ASC) (Hermle et al. 1988; Javitt and states and naturally occurring psychoses Zukin 1991; Vollenweider, 1994). In combination (Vollenweider, 1994). with functional brain imaging techniques and The theoretical conception of the “thalamic pharmacological methodologies, they are remarkable filter” theory is comparable to animal models of molecular probes to study the functional sensory gating deficits such as the prepulse organization of the brain and to generate chemical inhibition paradigm (PPI), although the PPI hypotheses of ASC. The study of hallucinogens in paradigm does not explicitly refer to the thalamus as humans is important because these substances affect an anatomical structure responsible for filtering a number of brain functions that typically deficits. However, both the CSTC model and the characterize the human mind, including cognition, PPI paradigm suggest that perturbations in cortico- volition, ego, and self-consciousness. They can elicit striato-thalamic pathways are critical for the loss of a clinical syndrome that resembles in various aspects inhibition processes and the pathogenesis of the first manifestation of schizophrenic disorders, psychotic symptoms. This assumption is supported but is different in other respects (Fischman, 1983; by increasing preclinical evidence demonstrating Gouzoulis et al. -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. -
Download Product Insert (PDF)
PRODUCT INFORMATION Risperidone-d4 Item No. 10010570 CAS Registry No.: 1020719-76-9 Formal Name: 3-[2-[4-(6-fluoro-1,2-benzisoxazol- O 3-yl)-1-piperidinyl]ethyl-1,1,2,2-d4]- N 6,7,8,9-tetrahydro-2-methyl-4H- pyrido[1,2-a]pyrimidin-4-one F D D C H FN O D MF: 23 23 4 2 4 N FW: 414.5 N Chemical Purity: ≥95% (Risperidone) D D O Deuterium N Incorporation: ≥99% deuterated forms (d1-d4); ≤1% d0 Supplied as: A solid Storage: -20°C Stability: ≥2 years Information represents the product specifications. Batch specific analytical results are provided on each certificate of analysis. Laboratory Procedures Risperidone-d4 is intended for use as an internal standard for the quantification of risperidone (Item No. 13629) by GC- or LC-MS. The accuracy of the sample weight in this vial is between 5% over and 2% under the amount shown on the vial. If better precision is required, the deuterated standard should be quantitated against a more precisely weighed unlabeled standard by constructing a standard curve of peak intensity ratios (deuterated versus unlabeled). Risperidone-d4 is supplied as a solid. A stock solution may be made by dissolving the risperidone-d4 in the solvent of choice, which should be purged with an inert gas. Risperidone-d4 is slightly soluble in chloroform and methanol. Description Risperidone is an atypical antipsychotic that binds to dopamine D2 receptors (Ki = 3 nM) and the serotonin 1,2 (5-HT) receptor subtype 5-HT2A (Ki = 0.12 nM). It also binds to dopamine D4, α1- and α2-adrenergic, 5-HT1C, 5-HT1D, and histamine H1 receptors (Kis = 7, 0.81, 7.3, 47, 52, and 2.1 nM, respectively). -
A New Orientation to the Therapeutics of Psychiatric Disorders
Article NIMHANS Journal A New Orientation to the Therapeutics of Psychiatric Disorders Volume: 14 Issue: 04 October 1996 Page: 249-261 N Pradhan, - Department of Psychopharmacology, National Institute of Mental Health & Neuro Sciences, Bangalore 560 029, India Abstract In the context of advances in our knowledge of cellular and molecular neurobiology, the therapeutics of psychiatric disorders demands a new orientation. It is surprising that despite considerable advances in neurobiology, our comprehension of neural basis of behaviour, and hence abnormal states of mind encountered in clinical psychiatry practice, remains rudimentary. The current pharmacological management of psychiatric disorders are vastly empirical in nature. The neurobiological strategy to understand behavioural problems or deducing the etiology of psychiatric illnesses from the specificity of drug action is as misleading as deducing the etiology of enteric fever from the action of antipyretic drugs. The current successes of broad spectrum drugs in the management of intractable disorders like schizophrenia, has freshened the debate on the role of multiple-interacting neurochemical systems underlying the behavioural dysfunctions. Against this background, this review paper aims to generate a new perspective for psychopharmacology research. The prototype psychiatric disorders and pharmacological agents used in their treatment are discussed. Some of the newer drugs in experimental stages are also included in this topic. This new orientation marks the end of one generation of view that advocated neurochemical specificity of drug action in the treatment of psychiatric illness. This may also herald the beginning of the emergence of a comprehensive, global and holistic view of brain, behaviour and mental illness from the pharmacological view point. -
Pharmaceutical Appendix to the Tariff Schedule 2
Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9 -
(12) Patent Application Publication (10) Pub. No.: US 2014/0144429 A1 Wensley Et Al
US 2014O144429A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0144429 A1 Wensley et al. (43) Pub. Date: May 29, 2014 (54) METHODS AND DEVICES FOR COMPOUND (60) Provisional application No. 61/887,045, filed on Oct. DELIVERY 4, 2013, provisional application No. 61/831,992, filed on Jun. 6, 2013, provisional application No. 61/794, (71) Applicant: E-NICOTINE TECHNOLOGY, INC., 601, filed on Mar. 15, 2013, provisional application Draper, UT (US) No. 61/730,738, filed on Nov. 28, 2012. (72) Inventors: Martin Wensley, Los Gatos, CA (US); Publication Classification Michael Hufford, Chapel Hill, NC (US); Jeffrey Williams, Draper, UT (51) Int. Cl. (US); Peter Lloyd, Walnut Creek, CA A6M II/04 (2006.01) (US) (52) U.S. Cl. CPC ................................... A6M II/04 (2013.O1 (73) Assignee: E-NICOTINE TECHNOLOGY, INC., ( ) Draper, UT (US) USPC ..................................................... 128/200.14 (21) Appl. No.: 14/168,338 (57) ABSTRACT 1-1. Provided herein are methods, devices, systems, and computer (22) Filed: Jan. 30, 2014 readable medium for delivering one or more compounds to a O O Subject. Also described herein are methods, devices, systems, Related U.S. Application Data and computer readable medium for transitioning a Smoker to (63) Continuation of application No. PCT/US 13/72426, an electronic nicotine delivery device and for Smoking or filed on Nov. 27, 2013. nicotine cessation. Patent Application Publication May 29, 2014 Sheet 1 of 26 US 2014/O144429 A1 FIG. 2A 204 -1 2O6 Patent Application Publication May 29, 2014 Sheet 2 of 26 US 2014/O144429 A1 Area liquid is vaporized Electrical Connection Agent O s 2. -
Pjp4'2003.Vp:Corelventura
Copyright © 2003 by Institute of Pharmacology Polish Journal of Pharmacology Polish Academy of Sciences Pol. J. Pharmacol., 2003, 55, 543–552 ISSN 1230-6002 NOVEL 4-ALKYL-1-ARYLPIPERAZINES AND 1,2,3,4-TETRAHYDROISOQUINOLINES CONTAINING DIPHENYLMETHYLAMINO OR DIPHENYLMETHOXY FRAGMENT WITH DIFFERENTIATED 5-HT1A/5-HT2A/D2 RECEPTOR ACTIVITY Maria H. Paluchowska1,#, Maria J. Mokrosz 1, Sijka Charakchieva-Minol1, Beata Duszyñska1, Aneta Kozio³1, Anna Weso³owska2, Katarzyna Stachowicz2, Ewa Chojnacka-Wójcik2 Department of Medicinal Chemistry, Department of New Drugs Research, Institute of Pharmacology, Polish Academy of Sciences, Smêtna 12, PL 31-343 Kraków, Poland Novel 4-alkyl-1-arylpiperazines and 1,2,3,4-tetrahydroisoquinolines containing diphenylmethylamino or diphenylmethoxy fragment with dif- ferentiated 5-HT)/5-HT )/D receptor activity. M.H. PALUCHOWSKA, M.J. MOKROSZ , S. CHARAKCHIEVA-MINOL, B. DUSZYÑSKA, A. KOZIO£, A. WESO£OWSKA, K. STACHOWICZ, E. CHOJNACKA- WÓJCIK. Pol. J. Pharmacol., 2003, 55, 543–552. Two series of 4-alkyl-1-arylpiperazines (1–4) and 1,2,3,4-tetrahydroiso- quinolines (5, 6) with diphenylmethylamino (series a) or diphenylmethoxy (series b) fragment were synthesized in order to obtain potential ligands of 5-HT) and/or 5-HT ) and dopamine D receptors. Four new arylpiperazi- nes (1a, 3a, 1b, 3b) were found to demonstrate high 5-HT) receptor affinity (KE = 1.5–35 nM); among them, 3a exhibited satisfactory 5-HT ) receptor affinity (KE = 74 nM). Only compounds 1b and 2b showed moderate affinity for D receptor sites (KE = 123 and 128 nM, respectively). Compounds 1a, 3a, 1b and 3b were investigated in vivo to determine their functional activity at 5-HT) receptors; additionally, 3a was tested for 5-HT ) receptor activity. -
(12) United States Patent (10) Patent No.: US 6,197,764 B1 Bradley Et Al
USOO6197764B1 (12) United States Patent (10) Patent No.: US 6,197,764 B1 Bradley et al. (45) Date of Patent: *Mar. 6, 2001 (54) CLOZAPINE COMPOSITIONS AND USES FOREIGN PATENT DOCUMENTS THEREOF 0599 576A1 1/1994 (EP). (75) Inventors: Matthews O. Bradley, Laytonsville, 693498 1/1996 (EP). MD (US); Victor E. Shashoua, 61204136 11/1984 (JP). Belmont, MA (US); Charles S. 06-072868 3/1994 (JP). Swindell, Merion; Nigel L. Webb, 6072868 3/1994 (JP). Bryn Mawr, both of PA (US) 7082146 3/1996 (JP). 8151334 6/1996 (JP). (73) Assignee: Protarga, Inc., Conshohocken, PA (US) 9030963 2/1997 (JP). (*) Notice: Subject to any disclaimer, the term of this WO 89/07938 9/1989 (WO). patent is extended or adjusted under 35 WO 96/04001 2/1996 (WO). U.S.C. 154(b) by 0 days. WO 96/22303 7/1996 (WO). WO 96/27380 9/1996 (WO). This patent is Subject to a terminal dis WO98/17325 4/1998 (WO). claimer. OTHER PUBLICATIONS (21) Appl. No.: 08/978,541 (22) Filed: Nov. 26, 1997 Bourat, et al., "Long Chain Esters of Pipotiazine as Lon g-Acting Psychotropic Pro-Drug, Med. Chem. Proc. Int. (51) Int. Cl. .............................................. A61K 31/00 Symp. 5th (1976) pp. 105-114. (52) U.S. Cl. ........................... 514/218; 514/219; 514/220 Lohr, et al., “Neuroleptic-Induced Movement Disorders . (58) Field of Search ..................................... 514/218, 219, ..", Psychiatry, vol. 3, (1989). 514/220 Makino, et al., Chemical Abstracts, vol. 106, No. 12, (56) References Cited (90.177x) issued Mar. 23, 1987, “Pharmaceuticals Permeable to Blood-Brain Barrier'. -
Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0