Research Topics
| J W DalySummaryAffiliation: National Institutes of Health Country: USA Publications
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Publications
Flexible synthesis of poison-frog alkaloids of the 5,8-disubstituted indolizidine-class. II: Synthesis of (-)-209B, (-)-231C, (-)-233D, (-)-235B", (-)-221I, and an epimer of 193E and pharmacological effects at neuronal nicotinic acetylcholine receptoSoushi Kobayashi
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama, Sugitani 2630, Toyama, 930 0194, Japan
Beilstein J Org Chem 3:30. 2007....
Caffeine analogs: biomedical impactJ W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892 0820, USA
Cell Mol Life Sci 64:2153-69. 2007..Adverse effects can include anxiety, hypertension, certain drug interactions, and withdrawal symptoms...- Biologically active substances from amphibians: preliminary studies on anurans from twenty-one genera of ThailandJohn W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, DHHS, NIH, Bldg 8, Rm 1A17, Bethesda, MD 20892 USA
Toxicon 44:805-15. 2004..Trace amounts of pumiliotoxin alkaloids were detected in a ranid frog (Limnonectes kuhli). A further 18 species did not exhibit noxious or toxic properties to a significant extent... - Nicotinic agonists, antagonists, and modulators from natural sourcesJohn W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892, USA
Cell Mol Neurobiol 25:513-52. 2005..3. Clearly, research on acetylcholine receptors and functions has been dependent on key natural products and the synthetic agents that they inspired... - Marine toxins and nonmarine toxins: convergence or symbiotic organisms?John W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892 0820, USA
J Nat Prod 67:1211-5. 2004..The occurrence and possible origin of tetrodotoxin and congeners, including chiriquitoxin, and of the saxitoxin analogue zetekitoxin in amphibians are reviewed... - Alkaloids from amphibian skin: a tabulation of over eight-hundred compoundsJohn W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892 0820, USA
J Nat Prod 68:1556-75. 2005.... 
Evidence for an enantioselective pumiliotoxin 7-hydroxylase in dendrobatid poison frogs of the genus DendrobatesJohn W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892 0820, USA
Proc Natl Acad Sci U S A 100:11092-7. 2003..Thus, the evolutionary development of a pumiliotoxin 7-hydroxylase would have provided frogs of the genus Dendrobates with a means of enhancing the antipredator potency of ingested PTXs...- Bioactive alkaloids of frog skin: combinatorial bioprospecting reveals that pumiliotoxins have an arthropod sourceJohn W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Proc Natl Acad Sci U S A 99:13996-4001. 2002.... - Alkaloids in bufonid toads (melanophryniscus): temporal and geographic determinants for two argentinian speciesJ W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institute Health, DHHS, Bethesda, MD 20892 0820, USA
J Chem Ecol 33:871-87. 2007..Furthermore, alkaloid profiles of M. stelzneri and M. rubriventris strongly differed, probably reflecting differences in the ecosystem and hence in availability of alkaloid-containing arthropods... 
Individual and geographic variation of skin alkaloids in three species of Madagascan poison frogs (Mantella)John W Daly
Laboratory of Bioorganic Chemistry, HHS, NIDDK, NIH, Bethesda, MD 20892, USA
J Chem Ecol 34:252-79. 2008..Alkaloid compositions in mantellid poison frogs are diverse and highly dependent on geographic location that appear to be largely determined by the nature and availability of alkaloid-containing prey items...- Ernest Guenther award in chemistry of natural products. Amphibian skin: a remarkable source of biologically active arthropod alkaloidsJohn W Daly
Chief, Section of Pharmacodynamics, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892-0820, USA
J Med Chem 46:445-52. 2003 - Stimulation of phosphoinositide breakdown in brain synaptoneurosomes by agents that activate sodium influx: antagonism by tetrodotoxin, saxitoxin, and cadmiumF Gusovsky
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, Maryland 20892
Mol Pharmacol 32:479-87. 1987..However, cadmium also may in some way inhibit phosphoinositide breakdown elicited by sodium channel agents at a point subsequent to sodium influx... - Voltage-dependent sodium channels in synaptoneurosomes: studies with 22Na+ influx and [3H]saxitoxin and [3H]batrachotoxinin-A 20-alpha-benzoate binding. Effects of proparacaine isothiocyanateF Gusovsky
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892
Brain Res 518:101-6. 1990..The results indicate that virtual elimination of binding sites labeled by [3H]BTX-B in the presence of scorpion venom by PROPRIT has little effect on sodium influx induced by BTX.(ABSTRACT TRUNCATED AT 250 WORDS).. - Syntheses and adrenergic activities of ring-fluorinated epinephrinesA Adejare
Laboratory of Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, Bethesda, Maryland 20892
J Med Chem 31:1972-7. 1988..Thus, 2-FEpi is a relatively selective beta-adrenergic ligand, while 6-FEpi is a relatively selective alpha-adrenergic ligand. Fluorine substitution of Epi also can markedly increase potency at either alpha- or beta-adrenergic receptors... - 8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptorsM T Shamim
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, Maryland 20892
J Med Chem 31:613-7. 1988..8-Piperidinyl and 8-pyrazinyl analogues had very low activities as adenosine receptor antagonists... - Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positionsM T Shamim
Laboratory of Bioorganic Chemistry, National Institutes of Health, Bethesda, Maryland 20892
J Med Chem 32:1231-7. 1989..Such A2 selectivity is in contrast to the marked A1 selectivity of 8-cycloalkyltheophyllines and 8-cycloalkyl-1,3-dipropulxanthines. The apparent selectivity of certain xanthines is dependent on the assay systems that are compared... - Local anesthetics: comparison of effects on batrachotoxin-elicited sodium flux and phosphoinositide breakdown in guinea pig cerebral cortical synaptoneurosomesY Nishizawa
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, Maryland 20892
Mol Pharmacol 34:707-13. 1988.... - Adenosine analogs with covalently attached lipids have enhanced potency at A1-adenosine receptorsK A Jacobson
Laboratory of Chemistry, NIDDK, Bethesda, MD 20892
FEBS Lett 225:97-102. 1987..The very high affinity of adenosine-lipid conjugates may be due to stabilization of these adducts in the phospholipid microenvironment of the receptor protein... - Structure of alkaloid 275A, a novel 1-azabicyclo[5.3.0]decane from a dendrobatid frog, Dendrobates lehmanni: synthesis of the tetrahydrodiastereomersH M Garraffo
Laboratory of Bioorganic Chemistry, NIDDK, NIH, Bethesda, Maryland 20892 0820, USA
J Nat Prod 64:421-7. 2001..Alkaloid 1 is often accompanied by other congeners, in particular a 5Z,10Z diastereomer 15, a dihydro analogue 16, and a ketone 17. Such izidines in frogs may arise from dietary ants, as do other classes of izidines... - 7-Deaza-2-phenyladenines: structure-activity relationships of potent A1 selective adenosine receptor antagonistsC E Muller
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892
J Med Chem 33:2822-8. 1990..Chloro substitution of the 2-phenyl ring appeared to improve the solubility as well as the solubility over A1 affinity ratio of 9-phenyl- and 9-(1-phenylethyl)-substituted 7-deazadenines... - Procaine isothiocyanate: an irreversible inhibitor of the specific binding of [3H]batrachotoxinin-A benzoate to sodium channelsC R Creveling
Laboratory of Bioorganic, Chemistry National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892
Neurochem Res 15:441-8. 1990..Protection studies with procaine and other local anesthetics suggest that only the 68 kDa species was related to local anesthetic binding... - Imidazodiazepinediones: a new class of adenosine receptor antagonistsJ W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892
J Med Chem 33:2818-21. 1990..The imidazodiazepinediones had low affinity for brain benzodiazepine sites... - Alkaloids from frog skins: selective probes for ion channels and nicotinic receptorsJ W Daly
Laboratory of Bioorganic Chemistry, National Institutes of Health, Bethesda, MD 20892 0820, USA
Braz J Med Biol Res 28:1033-42. 1995..The origins of the batrachotoxins, histrionicotoxins, pumiliotoxins and epibatidine are of particular interest in view of their remarkable biological activities... - 6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptorsJ W Daly
National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
J Med Chem 43:2514-22. 2000..The antagonist/agonist binding ratio method is clearly not always reliable for predicting agonist activity at muscarinic receptors... - N-methyldecahydroquinolines: an unexpected class of alkaloids from Amazonian poison frogs (Dendrobatidae)John W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892 0820, USA
J Nat Prod 72:1110-4. 2009..The alkaloids in skin extracts of three species of another genus of Amazonian poison frog, Adelphobates, were also characterized, but N-methyldecahydroquinolines were not detected... - A stereospecific synthesis of (+/-)-5,8-disubstituted indolizidines and (+/-)-1,4-disubstituted quinolizidines found in poison frog skinsP Michel
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892 0820, USA
J Org Chem 65:8908-18. 2000..The structures of the natural alkaloids were thereby established by chiral GC comparison with the exception of indolizidine 209B (I) for which a natural 209B could no longer be detected... - Ammonia chemical ionization tandem mass spectrometry in structural determination of alkaloids. II. Tetraponerines from pseudomyrmecine antsH M Garraffo
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0820, USA
Rapid Commun Mass Spectrom 15:1409-15. 2001..allaborans) had T-2, T-4 and T-8, while a Chinese ant (T. binghami) had T-5, T-6, T-7 and T-8. Four other ants, T. rufonigra (India), T. penzigi (Africa), T. clypeata (Africa) and T. sp. cf. emeryi (Africa), had no tetraponerines... - Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanolA Adejare
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892
J Med Chem 34:1063-8. 1991.... - Bioassay-guided isolation of epiquinamide, a novel quinolizidine alkaloid and nicotinic agonist from an Ecuadoran poison frog, Epipedobates tricolorRichard W Fitch
Section on Pharmacodynamics, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892, USA
J Nat Prod 66:1345-50. 2003..The off-line screening technique was found to be very sensitive for the detection of compounds active at nicotinic receptors... - Phantasmidine: an epibatidine congener from the ecuadorian poison frog Epipedobates anthonyiRichard W Fitch
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892, USA
J Nat Prod 73:331-7. 2010..After synthesis, this novel rigid agonist may serve as a selective probe for beta4-containing nicotinic receptors and potentially lead to useful pharmaceuticals... - Frog secretions and hunting magic in the upper Amazon: identification of a peptide that interacts with an adenosine receptorJ W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892
Proc Natl Acad Sci U S A 89:10960-3. 1992..The vasoactive peptide sauvagine, the opioid peptides, and adenoregulin and related peptides affect behavior in mice and presumably contribute to the behavioral sequelae observed in humans... - Multiple effects of caffeine on Ca2+ release and influx in human B lymphocytesY Sei
Department of Anesthesiology, Uniformed Services University of the Health Sciences, Bethesda, MD 20814 4799, USA
Cell Calcium 29:149-60. 2001..Our results suggest the need for caution regarding use of caffeine simply as a RYR-activator to study Ca2+ homeostasis in eucaryotic cells... - Indolizidine 239Q and quinolizidine 275I. Major alkaloids in two Argentinian bufonid toads (Melanophryniscus)John W Daly
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, MD 20892, USA
Toxicon 52:858-70. 2008..A third alkaloid, 249F (3), is postulated to be a homopumiliotoxin with an unprecedented conjugated exocyclic diene moiety... - Roughing it: a mantellid poison frog shows greater alkaloid diversity in some disturbed habitatsNirina R Andriamaharavo
Laboratory of Bioorganic Chemistry, NIDDK, NIH, DHHS, Bethesda, Maryland 20892, USA
J Nat Prod 73:322-30. 2010..This constancy of skin alkaloid composition likely reflects a constancy of dietary prey items consumed by frogs at undisturbed sites... - Loperamide: novel effects on capacitative calcium influxJ W Daly
Laboratory of Bioorganic Chemistry, National Institutes of Health Bethesda, Maryland 20892, USA
Cell Mol Life Sci 57:149-57. 2000..The mechanism whereby loperamide enhances levels of intracellular calcium elevated by capacitative calcium influx is, as yet, undefined... - Functional characterization of the A2b adenosine receptor in NIH 3T3 fibroblastsL E Brackett
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892
Biochem Pharmacol 47:801-14. 1994..In a series of non-xanthine antagonists, most compounds were equipotent or slightly more potent at the A2a receptor except for alloxazine, which was approximately 9-fold selective for the A2b receptor... - Mouse beta-TC6 insulinoma cells: high expression of functional alpha3beta4 nicotinic receptors mediating membrane potential, intracellular calcium, and insulin releaseMasahiro Ohtani
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0820, USA
Mol Pharmacol 69:899-907. 2006..The binding and functional data suggest that the major nicotinic receptor is composed of alpha3 and beta4 subunits. The beta-TC6 cells thus provide a model system for pharmacological study of such nicotinic receptors... - Co-existence of muscarinic and nicotinic receptors and their functional interaction in mouse Beta-TC6 cellsMasahiro Ohtani
Chemical Biology, National Institutes of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Eur J Pharmacol 604:150-7. 2009.... - Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptorsRichard W Fitch
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892, USA
Bioorg Med Chem Lett 15:1221-4. 2005..Caulophylline methiodide was less potent than cytisine, but retained significant activity. Thiocytisine was relatively weak in potency and efficacy, but was significantly selective for the alpha4beta2 subtype... - The husbandry and care of dendrobatid frogsMark B St Claire
Laboratory Animal Science Section and Laboratory of Bioorganic Chemistry, NIDDK, DHHS, NIH, Bethesda, Maryland, USA
Contemp Top Lab Anim Sci 44:8-14. 2005..A brief summary of dendrobatid research highlights is provided... - Phosphorimaging detection and quantitation for isotopic ion flux assaysRichard W Fitch
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892, USA
Anal Biochem 342:260-70. 2005..Phosphorimaging detection allows for reliable beta counting of up to 1,200 simultaneous samples with excellent sensitivity and is amenable for application to high-throughput screening... - Synthesis of 2',5'-dideoxy-2-fluoroadenosine and 2',5'-dideoxy-2,5'-difluoroadenosine: potent P-site inhibitors of adenylyl cyclaseSong Ye
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, Maryland 20892, USA
J Med Chem 47:1207-13. 2004..The presence of fluorine on the purine ring increased potency of inhibition, and the most potent compound, beta-2',5'-dideoxy-2-fluoroadenosine (1b), was 3 times more potent than beta-2',5'-dideoxyadenosine... - Membrane potential fluorescence: a rapid and highly sensitive assay for nicotinic receptor channel functionRichard W Fitch
Section on Pharmacodynamics, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Proc Natl Acad Sci U S A 100:4909-14. 2003..Thus, membrane potential serves as a sensitive measure of nicotinic activity, and the resulting depolarization may be as important as calcium in cell signaling... - Reserpine: interactions with batrachotoxin and brevetoxin sites on voltage-dependent sodium channelsAndrew Flowers
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
Cell Mol Neurobiol 22:1-12. 2002..Local anesthetics also may bind to the brevetoxin site... - Homoepiboxidines: further potent agonists for nicotinic receptorsRichard W Fitch
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Kidney and Digestive Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Bioorg Med Chem 12:179-90. 2004..The time course at such ip doses was significantly longer for homoepiboxidine 3 with marked analgesia still manifest at 30 min post-injection. Epiboxidine and the homoepiboxidines were less toxic than epibatidine... - Melyrid beetles (Choresine): a putative source for the batrachotoxin alkaloids found in poison-dart frogs and toxic passerine birdsJohn P Dumbacher
Smithsonian Conservation Research Center, Front Royal, VA 22630, USA
Proc Natl Acad Sci U S A 101:15857-60. 2004..The family Melyridae is cosmopolitan, and relatives in Colombian rain forests of South America could be the source of the batrachotoxins found in the highly toxic Phyllobates frogs of that region... - Geographic and seasonal variation in alkaloid-based chemical defenses of Dendrobates pumilio from Bocas del Toro, PanamaRalph A Saporito
Department of Biological Sciences, Florida International University, Miami, FL 33199, USA
J Chem Ecol 32:795-814. 2006..However, a variety of frog skin alkaloids was recently detected in mites, suggesting that mites may also play an important role in chemical defense... - Spatial and temporal patterns of alkaloid variation in the poison frog Oophaga pumilio in Costa Rica and Panama over 30 yearsRalph A Saporito
Department of Biological Sciences, Florida International University, Miami, FL 33199, USA
Toxicon 50:757-78. 2007..The results of this study indicate that chemical defense in a dendrobatid poison frog is dependent on geographic location and habitat type, which presumably controls the abundance and nature of alkaloid-containing arthropods... - Venom chemistry of the ant Myrmicaria melanogaster from BruneiTappey H Jones
Department of Chemistry, Virginia Military Institute, Lexington, Virginia 24450, USA
J Nat Prod 70:160-8. 2007..A biogenetic relationship between the mono- and bicyclic ring systems is proposed... - A common pumiliotoxin from poison frogs exhibits enantioselective toxicity against mosquitoesPaul J Weldon
Conservation and Research Center, Smithsonian Institution, Front Royal, VA 22630, USA
Proc Natl Acad Sci U S A 103:17818-21. 2006..This value is substantially lower than that estimated for the cutaneous abundance of this compound in some frogs, an observation consistent the function of PTX 251D in anuran chemical defense against ectoparasitic arthropods... - Alkaloids of anuran skin: antimicrobial function?Cyrus Macfoy
Biology Department, American Universitym Washington, DC, USA
Z Naturforsch C 60:932-7. 2005..albicans. The results suggest that certain of the skin alkaloids of poison frogs, in addition to being noxious to predators, may also benefit the frog through protection against skin infections... - A revised structure for alkaloid 235C isolated from skin extracts of mantellid (Mantella) frogs of MadagascarN Rabe Andriamaharavo
Laboratoire de Chimie Organique Produits Naturels, , Antananarivo 1001, Madagascar, School of Chemistry, Queen's University, Belfast BT9 5AG, Northern Ireland, UK
J Nat Prod 68:1743-8. 2005..A comparison is presented between the mass, infrared, and (1)H NMR spectra of 235C (2) and a synthetic dehydrohomopumiliotoxin (1), initially proposed incorrectly as the structure for 235C... - Formicine ants: An arthropod source for the pumiliotoxin alkaloids of dendrobatid poison frogsRalph A Saporito
Department of Biological Sciences, Florida International University, Miami, FL 33199, USA
Proc Natl Acad Sci U S A 101:8045-50. 2004..These findings further support the significance of ant-specialization and alkaloid sequestration in the evolution of bright warning coloration in poison frogs and toads... - N,N-acetals as N-acyliminium ion precursors: synthesis and absolute stereochemistry of epiquinamideMarloes A Wijdeven
Radboud University Nijmegen, Institute for Molecules and Materials, Toernooiveld 1, NL 6525 ED Nijmegen, The Netherlands
Org Lett 10:4001-3. 2008.... - Synthesis of alkaloid 223A and a structural revisionNaoki Toyooka
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Sugitani 2630, 930 0194, Japan
Org Lett 4:1715-7. 2002..The proposed structure for natural 223A (A, absolute configuration unknown) was revised to B, and the relative stereostructure was determined to be 5R*,6R*,8R*,9S* by the present synthesis... - Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonistsChrista E Muller
Pharmaceutical Institute Poppelsdorf, University of Bonn, Bonn, Germany
J Med Chem 45:3440-50. 2002..The most potent A(3) antagonist of the present series was (R)-4-methyl-8-ethyl-2-phenyl-imidazo[2,1-i]purin-5-one (R-24) exhibiting a K(i) value of 2.3 nM and high selectivity for A(3) receptors vs all other AR subtypes... - 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonistsAlaa M Hayallah
University of Bonn, Pharmaceutical Institute Poppelsdorf, Bonn, Germany
J Med Chem 45:1500-10. 2002..30-fold selectivity versus rat A1, and greater than 400-fold selectivity versus human A2A and A3 ARs. The new potent, selective, water-soluble A2B antagonists may be useful research tools for investigating A2B receptor function... - Patients with malignant hyperthermia demonstrate an altered calcium control mechanism in B lymphocytesYoshitatsu Sei
Uniformed Services University of the Health Sciences, Bethesda, Maryland 20814 4799, USA
Anesthesiology 97:1052-8. 2002..Because human B lymphocytes express the RYR1, it is hypothesized that Ca2+ homeostasis in B lymphocytes is altered in MHS individuals... - Dihydropyridines as inhibitors of capacitative calcium entry in leukemic HL-60 cellsJacquie L Harper
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, Bldg. 8, Rm. 1A17, National Institutes of Health, Bethesda, MD 20892, USA
Biochem Pharmacol 65:329-38. 2003..N-Methylnitrendipine (IC(50) 2.6 microM, MRS 1844) and N-propargylnifrendipine (IC(50) 1.7 microM, MRS 1845) represent possible lead compounds for the development of selective SOC channel inhibitors... - Oribatid mites as a major dietary source for alkaloids in poison frogsRalph A Saporito
Department of Biological Sciences, Florida International University, Miami, FL 33199, USA
Proc Natl Acad Sci U S A 104:8885-90. 2007..pumilio, as well as in the diets of other poison frogs. The results of this study indicate that mites are a significant arthropod repository of a variety of alkaloids and represent a major dietary source of alkaloids in poison frogs... - Caffeine analogs: effects on ryanodine-sensitive calcium-release channels and GABAA receptorsDan Shi
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland, USA
Cell Mol Neurobiol 23:331-47. 2003..6. Structure-activity relationships for xanthines do differ for calcium-release channels and and for different sites on GABAA receptors, but no highly selective lead compounds were identified... - Factors associated with frequent admissions to an acute geriatric psychiatric inpatient unitBenjamin K P Woo
Senior Behavioral Health Program, University of California, San Diego, CA 92103-8631, USA
J Geriatr Psychiatry Neurol 19:226-30. 2006.... - The structure of zetekitoxin AB, a saxitoxin analog from the Panamanian golden frog Atelopus zeteki: a potent sodium-channel blockerMari Yotsu-Yamashita
Graduate School of Agricultural Science, Tohoku University, Sendai 981 8555, Japan
Proc Natl Acad Sci U S A 101:4346-51. 2004..The IC50 values were 280 pM for human heart channels, 6.1 pM for rat brain IIa channels, and 65 pM for rat skeletal muscle channels, thus being roughly 580-, 160-, and 63-fold more potent at these channels than saxitoxin... - Synthesis of poison-frog alkaloids 233A, 235U, and 251AA and their inhibitory effects on neuronal nicotinic acetylcholine receptorsNaoki Toyooka
Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama, Sugitani 2630, Toyama 930 0194, Japan
Bioorg Med Chem Lett 17:5872-5. 2007..Thus, based on these studies, it would appear that C4 substituents greater in length than the allyl of 1-epi-207I reduce alpha7-potency without affecting alpha4beta2-potency...