DOCSLIB.ORG

Human Neurogenesis Assay: MKC-231 + AMPA

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Human Neurogenesis Assay: MKC-231 + AMPA US 20080064671 A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2008/0064671 A1 Barlow et al. (43) Pub. Date: Mar. 13, 2008 (54) COMBINATIONS CONTAINING A on Dec. 4, 2006, provisional application No. 60/884, 4-ACYLAMINOPYRIDINE DERVATIVE 584, filed on Jan. 11, 2007. (75) Inventors: Carrolee Barlow, Del Mar, CA (US); Todd A. Carter, San Diego, CA (US); Andrew Morse, San Publication Classification Diego, CA (US); Kai Treuner, San Diego, CA (US); Kym I. Lorrain, (51) Int. Cl. San Diego, CA (US) A6II 3/56 (2006.01) A6II 3/44 (2006.01) Correspondence Address: A6IP 25/00 (2006.01) TOWNSEND AND TOWNSEND AND CREW, CI2N 5/00 (2006.01) LLP A6II 3/47 (2006.01) TWO EMBARCADERO CENTER, EIGHTH FLOOR SAN FRANCISCO, CA 94111-3834 (52) U.S. Cl. ......... 514/171; 435/375; 514/314: 514/352 (73) Assignee: BrainCells, Inc., San Diego, CA (US) (21) Appl. No.: 11/766,721 (57) ABSTRACT The instant disclosure describes compositions and methods (22) Filed: Jun. 21, 2007 for treating diseases and conditions of the central and peripheral nervous system. The disclosure includes compo Related U.S. Application Data sitions and methods based on use of a 4-acylaminopyridine (60) Provisional application No. 60/825,080, filed on Sep. derivative in combination with one or more other neurogenic 8, 2006, provisional application No. 60/868,510, filed agents. One 4-acylaminopyridine derivative is MKC-231. Human Neurogenesis Assay: MKC-231 + AMPA Neuronal Differentiation (TUJ1) O 110 100 H MKC-231 IO MKC-231 + O.316 UM AMPA 70 60 50 40 30 20 O O.316 AWPA -19. 10-8.0 10-7.5 10-7.0 10-6.5 10-6-0 10-55 10-5.0 10-4.5 10-40 Conc (M) Patent Application Publication Mar. 13, 2008 Sheet 1 of 10 US 2008/006.4671 A1 Figure 1: Human Neurogenesis Assay: MKC-231 + AMPA Neuronal Differentiation (TUJ1) H MKC-231 IO MKC-231 + O.316 UM AMPA 5 O O ar- - 0.316 unt AMPA 19. 10-8.0 10-7.5 10-7.0 10-6.5 10-6-0 10-55 10-50 10-45 10-40 Conc (M) Patent Application Publication Mar. 13, 2008 Sheet 2 of 10 US 2008/006.4671 A1 Figure 2: Human Neurogenesis Assay: MKC-231 + EStradio Neuronal Differentiation (TUJ1) 100 O'MKC-231 90 '' EStradio 80 -- COmbination 1 O -8.5 1 O -7.5 1 O -6.5 1 O -5.5 1 O -4.5 MKC-231 Conc (M) 10 9.5 10 -8.5 10 7.5 10 -6.5 10 -5.5 Estradiol Conc (M) Patent Application Publication Mar. 13, 2008 Sheet 3 of 10 US 2008/006.4671 A1 Figure 3: Human Neurogenesis Assay: MKC-231 + TamOXifen Neuronal Differentiation (TUJ1) 110 100- O MKC-231 90- Tam Oxifen 80- -0- COmbination 10-8.5 10-7.5 10-6.5 10-5.5 10-4.5 Patent Application Publication Mar. 13, 2008 Sheet 4 of 10 US 2008/006.4671 A1 Figure 4: Human Neurogenesis ASSay: MKC-231 + Azakenpaullone Neuronal Differentiation (TUJ1) '''MKC-231 to Azakenpaulone 3150 Combination -9.5 -9.0 -8.5 -8.0 -7.5 -7.0 -6.5 -6.0 -5.5 -5.0 Azakenpaullone Conc (M) -8.5 -8.0 -7.5 -7.0 -6.5 -6.0 -5.5 -5.0 -4.5 -4.0 MKC-231 Conc (M) Patent Application Publication Mar. 13, 2008 Sheet 5 of 10 US 2008/006.4671 A1 Figure 5: Human Neurogenesis Assay: MKC-231 + Naltrexone Neuronal Differentiation (TUJ1) 110 100- - O - MKC-231 90 -- NaltrexOne -0- Combination 5 O 10-8.5 107.5 10-6.5 10-5.5 10-4.5 Patent Application Publication Mar. 13, 2008 Sheet 6 of 10 US 2008/006.4671 A1 Figure 6: Human Neurogenesis Assay: MKC-231 + Methylfolate Neuronal Differentiation (TUJ1) 110 100 -O-MKC-231 --Methylfolate -0- COmbination 50 10-8.5 10-7.5 10-6.5 10-5.5 10-4.5 Patent Application Publication Mar. 13, 2008 Sheet 7 of 10 US 2008/006.4671 A1 Figure 7: Human Neurogenesis Assay: MKC-231 + ACetazolamide Neuronal Differentiation (TUJ1) 110 100- - O - MKC-231 90- ACetaZOlamide 80- -- Combination 10-8.5 10-7.5 10-6.5 10-5.5 10-4.5 Patent Application Publication Mar. 13, 2008 Sheet 8 of 10 US 2008/006.4671 A1 Figure 8: Human Neurogenesis Assay: MKC-231 + AtOrVastatin Neuronal Differentiation (TUJ1) O'MKC-231 AtOrVastatin -- COmbination . : 1050 -1 1 O -8.5 10 -7.5 1 O -6.5 10 -5.5 10 -4.5 MKC-231 Conc (M) 10 11.5 10 - 10.5 10 -9.5 10 -8.5 10 -7.5 Atorvastatin Conc (M) Patent Application Publication Mar. 13, 2008 Sheet 9 of 10 US 2008/006.4671 A1 Figure 9: Human Neurogenesis Assay: MKC-231 + MOOdafinil Neuronal Differentiation (TUJ1) 110 100- - O - MKC-231 90- - - - MOCafinil 80- -0- Combination 10-8.5 10-7.5 10-6.5 10-5.5 10-4.5 Patent Application Publication Mar. 13, 2008 Sheet 10 of 10 US 2008/0064671 A1 Figure 10: Human Neurogenesis Assay: MKC-231 + Rosiglitazone Neuronal Differentiation (TUJ1) 110 100- - O - MKC-231 90- --Rosiglitazone -0- COmbination 50 10-8.5 10-7.5 10-6.5 10-5.5 10-4.5 US 2008/0064671 A1 Mar. 13, 2008 COMBINATIONS CONTAINING A additional neurogenic agent may be another 4-acylaminopy 4-ACYLAMINOPYRIDINE DERVATIVE ridine derivative or a neurogenic agent that acts through a mechanism independent from the 4-acylaminopyridine derivative. An additional neurogenic agent as described 0001 May: 17(10): 2042-6, Gould. Science. 1999 Oct. herein may be one which acts through a known receptor or 15; 286(5439):548-51, Malberg. J Neurosi. 2000 Dec. 15: one which is known for the treatment of a disease or 20(24):9104-10, Santarelli. Science. 2003 Aug. 8: condition. 301 (5634):805-9). Other factors, such as adrenal hormones, 0007 Embodiments of the disclosure are based upon a stress, age and drugs of abuse negatively influence neuro combination of a 4-acylaminopyridine derivative and one or genesis (Cameron. Neuroscience. 1994 July; 61(2):203-9. more other neurogenic agents disclosed herein or known to McEwen. Neuropsychopharmacology. 1999 Oct.: the skilled person. Compositions disclosed herein include 21(4):474-84, Kuhn. J. Neurosci. 1996 Mar. 15: 16(6):2027 Such combinations of a 4-acylaminopyridine derivative in 33, Eisch. Am J Psychiatry. 2004 March; 161(3):426). combination with one or more other neurogenic agents. 0002 U.S. Pat. No. 5,397,785 describes a number of 0008. In a second aspect, the disclosure includes a 4-acylaminopyridine derivatives and compositions as well method of lessening and/or reducing a decline or decrease of as their use in the treatment of senile dementia and Alzhe cognitive function in a subject or patient. In some cases, the imer's Disease. U.S. Pat. No. 6,884.805 describes poly method may be applied to maintain and/or stabilize cogni morph crystals of a 4-acylaminopyridine derivative and their tive function in the subject or patient. The method may use in activating a malfunctioned cholinergic neuron that is comprise administering a 4-acylaminopyridine derivative in associated with memory loss disturbances. combination with one or more other neurogenic agents to a 0003 Citation of the above documents is not intended as Subject or patient in an amount effective to lessen or reduce an admission that any of the foregoing is pertinent prior art. a decline or decrease of cognitive function. Statements about these documents do not constitute any 0009. In another aspect, the disclosed methods include admission as to the correctness of the dates or contents of identifying a patient Suffering from one or more diseases, these documents. disorders, or conditions, or a symptom thereof, and admin istering to the patient a 4-acylaminopyridine derivative in BRIEF SUMMARY OF THE DISCLOSURE combination with one or more other neurogenic agents as 0004 Disclosed herein are compositions and methods for described herein. In some embodiments, a method including the prophylaxis and treatment of diseases, conditions and identification of a subject as in need of an increase in injuries of the central and peripheral nervous systems by neurogenesis, and administering to the Subject a 4-acylami stimulating or increasing neurogenesis. Aspects of the meth nopyridine derivative in combination with one or more other ods, and activities of the compositions, include increasing or neurogenic agents is disclosed herein. In other embodi potentiating neurogenesis in cases of a disease, disorder, or ments, the Subject is a patient, Such as a human patient. condition of the nervous system. Embodiments of the dis 0010. Additional embodiments describe a method includ closure include methods of treating a neurodegenerative ing administering a 4-acylaminopyridine derivative in com disorder, neurological trauma including brain or central bination with one or more other neurogenic agents to a nervous system trauma and/or recovery therefrom, depres subject exhibiting the effects of insufficient amounts of, or Sion, anxiety, psychosis, learning and memory disorders, and inadequate levels of neurogenesis. In some embodiments, ischemia of the central and/or peripheral nervous systems. In the Subject may be one that has been subjected to an agent other embodiments, the disclosed methods are used to that decreases or inhibits neurogenesis. Non-limiting improve cognitive outcomes. examples of an inhibitor of neurogenesis include opioid 0005. In one aspect, methods of modulating, such as by receptor agonists, such as a mu receptor Subtype agonist like stimulating or increasing, neurogenesis are disclosed.
Load more

Recommended publications
  • WHO Drug Information Vol. 12, No. 3, 1998
    WHO DRUG INFORMATION VOLUME 12 NUMBER 3 • 1998 RECOMMENDED INN LIST 40 INTERNATIONAL NONPROPRIETARY NAMES FOR PHARMACEUTICAL SUBSTANCES WORLD HEALTH ORGANIZATION • GENEVA Volume 12, Number 3, 1998 World Health Organization, Geneva WHO Drug Information Contents Seratrodast and hepatic dysfunction 146 Meloxicam safety similar to other NSAIDs 147 Proxibarbal withdrawn from the market 147 General Policy Issues Cholestin an unapproved drug 147 Vigabatrin and visual defects 147 Starting materials for pharmaceutical products: safety concerns 129 Glycerol contaminated with diethylene glycol 129 ATC/DDD Classification (final) 148 Pharmaceutical excipients: certificates of analysis and vendor qualification 130 ATC/DDD Classification Quality assurance and supply of starting (temporary) 150 materials 132 Implementation of vendor certification 134 Control and safe trade in starting materials Essential Drugs for pharmaceuticals: recommendations 134 WHO Model Formulary: Immunosuppressives, antineoplastics and drugs used in palliative care Reports on Individual Drugs Immunosuppresive drugs 153 Tamoxifen in the prevention and treatment Azathioprine 153 of breast cancer 136 Ciclosporin 154 Selective serotonin re-uptake inhibitors and Cytotoxic drugs 154 withdrawal reactions 136 Asparaginase 157 Triclabendazole and fascioliasis 138 Bleomycin 157 Calcium folinate 157 Chlormethine 158 Current Topics Cisplatin 158 Reverse transcriptase activity in vaccines 140 Cyclophosphamide 158 Consumer protection and herbal remedies 141 Cytarabine 159 Indiscriminate antibiotic
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2012/0190743 A1 Bain Et Al
    US 2012O190743A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0190743 A1 Bain et al. (43) Pub. Date: Jul. 26, 2012 (54) COMPOUNDS FOR TREATING DISORDERS Publication Classification OR DISEASES ASSOCATED WITH (51) Int. Cl NEUROKININ 2 RECEPTORACTIVITY A6II 3L/23 (2006.01) (75) Inventors: Jerald Bain, Toronto (CA); Joel CD7C 69/30 (2006.01) Sadavoy, Toronto (CA); Hao Chen, 39t. ii; C Columbia, MD (US); Xiaoyu Shen, ( .01) Columbia, MD (US) A6IPI/00 (2006.01) s A6IP 29/00 (2006.01) (73) Assignee: UNITED PARAGON A6IP II/00 (2006.01) ASSOCIATES INC., Guelph, ON A6IPI3/10 (2006.01) (CA) A6IP 5/00 (2006.01) A6IP 25/00 (2006.01) (21) Appl. No.: 13/394,067 A6IP 25/30 (2006.01) A6IP5/00 (2006.01) (22) PCT Filed: Sep. 7, 2010 A6IP3/00 (2006.01) CI2N 5/071 (2010.01) (86). PCT No.: PCT/US 10/48OO6 CD7C 69/33 (2006.01) S371 (c)(1) (52) U.S. Cl. .......................... 514/552; 554/227; 435/375 (2), (4) Date: Apr. 12, 2012 (57) ABSTRACT Related U.S. Application Data Compounds, pharmaceutical compositions and methods of (60) Provisional application No. 61/240,014, filed on Sep. treating a disorder or disease associated with neurokinin 2 4, 2009. (NK) receptor activity. Patent Application Publication Jul. 26, 2012 Sheet 1 of 12 US 2012/O190743 A1 LU 1750 15OO 1250 OOO 750 500 250 O O 20 3O 40 min SampleName: EM2OO617 Patent Application Publication Jul. 26, 2012 Sheet 2 of 12 US 2012/O190743 A1 kixto CFUgan <tro CFUgan FIG.2 Patent Application Publication Jul.
    [Show full text]
  • Product List March 2019 - Page 1 of 53
    Wessex has been sourcing and supplying active substances to medicine manufacturers since its incorporation in 1994. We supply from known, trusted partners working to full cGMP and with full regulatory support. Please contact us for details of the following products. Product CAS No. ( R)-2-Methyl-CBS-oxazaborolidine 112022-83-0 (-) (1R) Menthyl Chloroformate 14602-86-9 (+)-Sotalol Hydrochloride 959-24-0 (2R)-2-[(4-Ethyl-2, 3-dioxopiperazinyl) carbonylamino]-2-phenylacetic 63422-71-9 acid (2R)-2-[(4-Ethyl-2-3-dioxopiperazinyl) carbonylamino]-2-(4- 62893-24-7 hydroxyphenyl) acetic acid (r)-(+)-α-Lipoic Acid 1200-22-2 (S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 207557-35-5 1,1'-Carbonyl diimidazole 530-62-1 1,3-Cyclohexanedione 504-02-9 1-[2-amino-1-(4-methoxyphenyl) ethyl] cyclohexanol acetate 839705-03-2 1-[2-Amino-1-(4-methoxyphenyl) ethyl] cyclohexanol Hydrochloride 130198-05-9 1-[Cyano-(4-methoxyphenyl) methyl] cyclohexanol 93413-76-4 1-Chloroethyl-4-nitrophenyl carbonate 101623-69-2 2-(2-Aminothiazol-4-yl) acetic acid Hydrochloride 66659-20-9 2-(4-Nitrophenyl)ethanamine Hydrochloride 29968-78-3 2,4 Dichlorobenzyl Alcohol (2,4 DCBA) 1777-82-8 2,6-Dichlorophenol 87-65-0 2.6 Diamino Pyridine 136-40-3 2-Aminoheptane Sulfate 6411-75-2 2-Ethylhexanoyl Chloride 760-67-8 2-Ethylhexyl Chloroformate 24468-13-1 2-Isopropyl-4-(N-methylaminomethyl) thiazole Hydrochloride 908591-25-3 4,4,4-Trifluoro-1-(4-methylphenyl)-1,3-butane dione 720-94-5 4,5,6,7-Tetrahydrothieno[3,2,c] pyridine Hydrochloride 28783-41-7 4-Chloro-N-methyl-piperidine 5570-77-4
    [Show full text]
  • Strategies for Managing Sexual Dysfunction Induced by Antidepressant Medication
    King’s Research Portal DOI: 10.1002/14651858.CD003382.pub3 Document Version Publisher's PDF, also known as Version of record Link to publication record in King's Research Portal Citation for published version (APA): Taylor, M. J., Rudkin, L., Bullemor-Day, P., Lubin, J., Chukwujekwu, C., & Hawton, K. (2013). Strategies for managing sexual dysfunction induced by antidepressant medication. Cochrane Database of Systematic Reviews, (5). https://doi.org/10.1002/14651858.CD003382.pub3 Citing this paper Please note that where the full-text provided on King's Research Portal is the Author Accepted Manuscript or Post-Print version this may differ from the final Published version. If citing, it is advised that you check and use the publisher's definitive version for pagination, volume/issue, and date of publication details. And where the final published version is provided on the Research Portal, if citing you are again advised to check the publisher's website for any subsequent corrections. General rights Copyright and moral rights for the publications made accessible in the Research Portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognize and abide by the legal requirements associated with these rights. •Users may download and print one copy of any publication from the Research Portal for the purpose of private study or research. •You may not further distribute the material or use it for any profit-making activity or commercial gain •You may freely distribute the URL identifying the publication in the Research Portal Take down policy If you believe that this document breaches copyright please contact [email protected] providing details, and we will remove access to the work immediately and investigate your claim.
    [Show full text]
  • A Role for Sigma Receptors in Stimulant Self Administration and Addiction
    Pharmaceuticals 2011, 4, 880-914; doi:10.3390/ph4060880 OPEN ACCESS pharmaceuticals ISSN 1424-8247 www.mdpi.com/journal/pharmaceuticals Review A Role for Sigma Receptors in Stimulant Self Administration and Addiction Jonathan L. Katz *, Tsung-Ping Su, Takato Hiranita, Teruo Hayashi, Gianluigi Tanda, Theresa Kopajtic and Shang-Yi Tsai Psychobiology and Cellular Pathobiology Sections, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, Baltimore, MD, 21224, USA * Author to whom correspondence should be addressed; E-Mail: [email protected]. Received: 16 May 2011; in revised form: 11 June 2011 / Accepted: 13 June 2011 / Published: 17 June 2011 Abstract: Sigma1 receptors (σ1Rs) represent a structurally unique class of intracellular proteins that function as chaperones. σ1Rs translocate from the mitochondria-associated membrane to the cell nucleus or cell membrane, and through protein-protein interactions influence several targets, including ion channels, G-protein-coupled receptors, lipids, and other signaling proteins. Several studies have demonstrated that σR antagonists block stimulant-induced behavioral effects, including ambulatory activity, sensitization, and acute toxicities. Curiously, the effects of stimulants have been blocked by σR antagonists tested under place-conditioning but not self-administration procedures, indicating fundamental differences in the mechanisms underlying these two effects. The self administration of σR agonists has been found in subjects previously trained to self administer cocaine. The reinforcing effects of the σR agonists were blocked by σR antagonists. Additionally, σR agonists were found to increase dopamine concentrations in the nucleus accumbens shell, a brain region considered important for the reinforcing effects of abused drugs.
    [Show full text]
  • Cyproterone Art. 31
    Приложение I Списък на лекарствените продукти и форми 1 Държава членка Притежател на Наименование на INN/Активно Фармацевтична Начин на (ЕИП) разрешението за продукта вещество + форма приложение употреба Количество на активното вещество (в дозова единица) Австрия Bayer Austria Gmbh Androcur Depot Cyproterone Acetate Инжекционен Интрамускулно 300mg/3ml разтвор приложение Австрия Bayer Austria Gmbh Climen Cyproterone Acetate 1mg Обвита таблетка Перорално таблетка, Estradiol приложение Valerate 2mg таблетка| Estradiol Valerate 2mg таблетка Австрия Bayer Austria Gmbh Climen 28-Tage Cyproterone Acetate 1mg Обвита таблетка Перорално таблетка, Estradiol приложение Valerate 2mg таблетка| Estradiol Valerate 2mg таблетка Австрия Bayer Austria Gmbh Diane Mite Cyproterone Acetate 2mg Обвита таблетка Перорално таблетка, Ethinylestradiol приложение 35μg таблетка Австрия Bayer Austria Gmbh Minerva Cyproterone Acetate 2mg Обвита таблетка Перорално таблетка, Ethinylestradiol приложение 0,035mg таблетка Австрия Bayer Austria Gmbh Andro-Diane Cyproterone Acetate Таблетка Перорално 10mg таблетка приложение Австрия Bayer Austria Gmbh Androcur Cyproterone Acetate Таблетка Перорално 100mg таблетка приложение Австрия Bayer Austria Gmbh Androcur Cyproterone Acetate Таблетка Перорално 50mg таблетка приложение Австрия Gynial Gmbh Alisma Cyproterone Acetate 2mg Филмирана таблетка Перорално таблетка, Ethinylestradiol приложение 35μg таблетка 2 Държава членка Притежател на Наименование на INN/Активно Фармацевтична Начин на (ЕИП) разрешението за продукта вещество +
    [Show full text]
  • Download Drug Labels List
    Syringe Labelling System Price Per Label Description/Drug Name Item No. Quanitiy Per Pack Pack Abciximab 99801 2 x 500 roll's £6.30 Abidec 100602 2 x 500 roll's £6.30 Acepromazine 99802 2 x 500 roll's £6.30 Acetazolamide 99803 2 x 500 roll's £6.30 Acetylcholine 99804 2 x 500 roll's £6.30 Acetylcysteine 99805 2 x 500 roll's £6.30 Acetylsalicylic Acid 99806 2 x 500 roll's £6.30 Aciclovir 99807 2 x 500 roll's £6.30 ACP/Buprenorphine 100208 2 x 500 roll's £6.30 Actrapid Insulin 99808 2 x 500 roll's £6.30 Adenosine 99809 2 x 500 roll's £6.30 Adrenaline (Top Half Black, Bottom Violet, Violet Text) 99810 2 x 500 roll's £6.30 Adrenaline/Epinephrine 99811 2 x 500 roll's £6.30 Albumin Solution 99812 2 x 500 roll's £6.30 Alchol 99813 2 x 500 roll's £6.30 Alemtuzmab 99814 2 x 500 roll's £6.30 ALERT 100243 2 x 500 roll's £6.30 Alfaxalone 99815 2 x 500 roll's £6.30 Alfentanil 99816 2 x 500 roll's £6.30 Alfentanil 99817 2 x 500 roll's £6.30 Alteplase 99818 2 x 500 roll's £6.30 Amikacin 99819 2 x 500 roll's £6.30 Aminophylline 99820 2 x 500 roll's £6.30 Amiodarone 100194 2 x 500 roll's £6.30 Amoxicillin 100195 2 x 500 roll's £6.30 Amphotericin 99821 2 x 500 roll's £6.30 Ampicillin 99822 2 x 500 roll's £6.30 Antibiotic 99823 2 x 500 roll's £6.30 Anticoagulant 99824 2 x 500 roll's £6.30 Antifungal 100228 2 x 500 roll's £6.30 Antiseptic 99825 2 x 500 roll's £6.30 Aprotinin 99826 2 x 500 roll's £6.30 Aqueous Iodine 99827 2 x 500 roll's £6.30 Arterial 100259 2 x 500 roll's £6.30 Arterial ( Line Label - White with Red Writing) 100176 2 x 500 roll's £6.30 Arterial
    [Show full text]
  • 52Nd Annual Meeting
    ACNP 52nd Annual Meeting Final Program December 8-12, 2013 The Westin Diplomat Resort & Spa Hollywood, Florida President: David A. Lewis, M.D. Program Committee Chair: Randy D. Blakely, Ph.D. Program Committee Co-Chair: Pat R. Levitt, Ph.D. This meeting is jointly sponsored by the Vanderbilt University School of Medicine Department of Psychiatry and the American College of Neuropsychopharmacology. Dear ACNP Members and Guests, It is a distinct pleasure to welcome you to the 2014 meeting of the American College of Neuropsychopharmacology! This 52nd annual meeting will again provide opportunities for the exercise of the College’s core values: the spirit of Collegiality, promoting in each other the best in science, training and service; participation in Community, pursuing together the goals of understanding the neurobiology of brain diseases and eliminating their burden on individuals and our society; and engaging in Celebration, taking the time to recognize and enjoy the contributions and accomplishments of our members and guests. Under the excellent leadership of Randy Blakely and Pat Levitt, the Program Committee has done a superb job in assembling an outstanding slate of scientific presentations. Based on membership feedback, the meeting schedule has been designed with the goals of achieving an optimal mix of topics and types of sessions, increasing the diversity of participating scientists and creating more time for informal interactions. The presentations will highlight both the breadth of the investigative interests of ACNP membership
    [Show full text]
  • Aldosterone Enhances Renal Calcium Reabsorption by Two Types of Channels
    View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Elsevier - Publisher Connector Kidney International, Vol. 66 (2004), pp. 242–250 Aldosterone enhances renal calcium reabsorption by two types of channels MARIE LECLERC,MICHELE` G. BRUNETTE, and DENIS COUCHOUREL Maisonneuve-Rosemont Hospital and University of Montreal, Canada Aldosterone enhances renal calcium reabsorption by two types transepithelial potential difference in the late segments of channels. of the nephron, reflecting a stimulation of the amiloride- Background. Aldosterone has been known for many years + + sensitive Na transport by the apical membranes. to increase sodium (Na ) reabsorption by the distal nephron. The present in vitro experiments investigated the effect of the In contrast to the abundant literature dealing with the + hormone on calcium (Ca2 ) transport by the luminal membrane antinatriuretic effect of aldosterone, data concerning its + of the rabbit nephron, independent of any systemic influence. action on Ca2 transport are relatively scarce. Clearance Methods. Proximal and distal tubules were incubated with studies showed either an increase in calciuria [2] or an + either aldosterone or the carrier. The luminal membranes of absence of significant change of Ca2 excretion [3, 4] af- these tubules were purified, vesiculated, and 45Ca uptake by these vesicles was subsequently measured. ter aldosterone administration. In a randomized study in Results. Treatment of the distal tubules with 10−8 mol/L al- male volunteers, Van Hamersvelt et al [5] compared the + + dosterone enhanced both 0.1 and 0.5 mmol/L Ca2 transport. effect of the Ca2 channel blocker felodipine, alone or The hormone action was abolished by tyrosine kinase inhibitors.
    [Show full text]
  • Customs Tariff - Schedule
    CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2020 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, UST, following to be employed in commercial fishing or the commercial MT, MUST, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2003/0171347 A1 Matsumoto (43) Pub
    US 2003.0171347A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0171347 A1 Matsumoto (43) Pub. Date: Sep. 11, 2003 (54) SIGMA RECEPTOR ANTAGONISTS HAVING Publication Classification ANT-COCANE PROPERTIES AND USES THEREOF (51) Int. Cl." ......................... A61K 31/55; A61K 31/33; A61K 31/397; A61K 31/445; (76) Inventor: Rae R. Matsumoto, Edmond, OK (US) A61K 31/40; A61K 31/137 (52) U.S. Cl. .............. 514/183; 514/210.01; 514/217.12; Correspondence Address: 514/317; 514/408; 514/649 DUNLAP, CODDING & ROGERS PC. PO BOX 16370 OKLAHOMA CITY, OK 73114 (US) (57) ABSTRACT (21) Appl. No.: 10/178,859 The present invention relates to novel Sigma receptor antagonist compounds that have anti-cocaine properties. (22) Filed: Jun. 21, 2002 These Sigma receptor antagonists are useful in the treatment Related U.S. Application Data of cocaine overdose and addiction as well as movement disorders. The Sigma receptor antagonists of the present (63) Continuation of application No. 09/715,911, filed on invention may also be used in the treatment of neurological, Nov. 17, 2000, now abandoned, which is a continu psychiatric, gastrointestinal, cardiovascular, endocrine and ation of application No. 09/316,877, filed on May 21, immune System disorders as well as for imaging procedures. 1999, now abandoned. The present invention also relates to novel pharmaceutical compounds incorporating Sigma receptor antagonists which (60) Provisional application No. 60/086,550, filed on May can be used to treat overdose and addiction resulting from 21, 1998. the use of cocaine and/or other drugs of abuse.
    [Show full text]
  • WO 2012/044761 Al
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date _ . 5 April 2012 (05.04.2012) WO 2012/044761 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 47/48 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, (21) International Application Number: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, PCT/US201 1/053876 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, 29 September 201 1 (29.09.201 1) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (25) Filing Language: English NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, (26) Publication Langi English RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, (30) Priority Data: ZM, ZW. 12/893,344 29 September 2010 (29.09.2010) US (84) Designated States (unless otherwise indicated, for every (71) Applicant (for all designated States except US): UNI¬ kind of regional protection available): ARIPO (BW, GH, VERSITY OF NORTH CAROLINA AT WILMING¬ GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, TON [US/US]; 601 South College Road, Wilmington, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, NC 28403 (US).
    [Show full text]