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Relevant bibliographies by topics / Structure of histamines

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Academic literature on the topic 'Structure of histamines'

Author: Grafiati

Published: 4 June 2021

Last updated: 3 February 2022

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Journal articles on the topic "Structure of histamines"

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Sukamoto, Takayuki, and Tadayuki Saito. "The structure-activity relationship of anti-histamines." Japanese Journal of Pharmacology 71 (1996): 18. http://dx.doi.org/10.1016/s0021-5198(19)36336-x.

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Dave, Shikha S., and Anjali M. Rahatgaonkar. "Computational Evaluation of 2-Phenyl-4H-chromen-4-one Analogues as Antihistamines: Potential HistamineN-Methyltransferase (HMT) Inhibitors." E-Journal of Chemistry 6, no. 4 (2009): 1009–16. http://dx.doi.org/10.1155/2009/497124.

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Abnormal release of histamine, which is present in relatively high concentration in the lungs, causes serious allergic vasoconstriction and anaphylactic manifestation in human beings. In mammals, a major pathway of histamine metabolism in the lungs is mediated by histamineN-methyl transferase (HMT) and diamine oxidase. The need to design a strategy of mechanistic computational evaluation of protein-ligand affinityi.e. HMT- 2-phenyl-4H-chromen-4-ones, protein complex binding energy has been established. A library of synthesized 2-phenyl-4H-chromen-4-ones was docked into the active site cavity of target protein, HMT (Pdb: 2aot). The high-resolution crystal structure of HMT complex with the competitive inhibitorN[2 (benzhydryloxy)ethyl]N N-Dimethylamine (Diphenhydramine) revealed a protein with a highly confined binding region that could be targeted in the design of specific anti-histamines. The validation of docking programme by Potential Mean Force was compared with binding energy results of known ligands in the active sites of HMT, diphenhydramine / benadryl, promethazine, cyproheptadine, trimeton / aviletc. All the synthesized chromone derivatives showed comparable negative binding energies pointing towards the fact that these molecules could be potent antihistamines.

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Kubota, Katsumi, Hirotaka Kurebayashi, Hirotaka Miyachi, Masanori Tobe, Masako Onishi, and Yoshiaki Isobe. "Synthesis and structure–activity relationship of tricyclic carboxylic acids as novel anti-histamines." Bioorganic & Medicinal Chemistry 19, no. 9 (May 2011): 3005–21. http://dx.doi.org/10.1016/j.bmc.2011.03.003.

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Kljun, Jakob, Saša Petriček, Dušan Žigon, Rosana Hudej, Damijan Miklavčič, and Iztok Turel. "Synthesis and Characterization of Novel Ruthenium(III) Complexes with Histamine." Bioinorganic Chemistry and Applications 2010 (2010): 1–6. http://dx.doi.org/10.1155/2010/183097.

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Novel ruthenium(III) complexes with histamine[RuCl4(dmso-S)(histamineH)]⋅O(1a) and[RuCl4(dmso-S)(histamineH)](1b) have been prepared and characterized by X-ray structure analysis. Their crystal structures are similar and show a protonated amino group on the side chain of the ligand which is not very common for a simple heterocyclic derivative such as histamine. Biological assays to test the cytotoxicity of the compound1bcombined with electroporation were performed to determine its potential for future medical applications in cancer treatment.

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Wang, Wentao, Fadi Aldeek, Xin Ji, Birong Zeng, and Hedi Mattoussi. "A multifunctional amphiphilic polymer as a platform for surface-functionalizing metallic and other inorganic nanostructures." Faraday Discuss. 175 (2014): 137–51. http://dx.doi.org/10.1039/c4fd00154k.

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We designed a new set of polymer ligands that combine multiple metal-coordinating groups and short polyethylene glycol (PEG) moieties in the same structure. The ligand design relies on the controlled grafting of a large number of amine-terminated histamines and PEG short chains onto a poly(isobutylene-alt-maleic anhydride) backbone,viaa one-step nucleophilic addition reaction. This addition reaction is highly efficient, can be carried out in organic media and does not require additional reagents. We show that when imidazole groups are used the resulting polymer ligand can strongly ligate onto metal nanostructures such as nanoparticles (NPs) and nanorods (NRs) made of gold cores. The resulting polymer-coated NPs and NRs exhibit good colloidal stability to pH changes and added electrolytes. This constitutes a departure from the use of thiol-based ligands to coordinate on Au surfaces. The present chemical approach also opens up additional opportunities for designing hydrophilic and reactive platforms where the polymer coating can be adjusted to various metal and metal oxide surfaces by simply modifying or combining the addition reaction with other metal coordinating groups. These could include iron oxide NPs and semiconductor QDs. These polymer-capped NPs and NRs can be used to develop biologically-active platforms with potential use for drug delivery and sensing.

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Suki, B., Q. Zhang, and K. R. Lutchen. "Relationship between frequency and amplitude dependence in the lung: a nonlinear block-structured modeling approach." Journal of Applied Physiology 79, no. 2 (August 1, 1995): 660–71. http://dx.doi.org/10.1152/jappl.1995.79.2.660.

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During lung constriction, there is an increase in both the frequency and tidal volume (VT) dependences of lung tissue resistance (Rti) and elastance (Eti). This suggests that 1) significant alterations take place in the mechanisms contributing to both the linear and nonlinear characteristics of lung tissues; and 2) the frequency and VT dependences of Rti and Eti are coupled. We examined these issues for the case of sine wave and special pseudorandom inputs by utilizing the theory of nonlinear block-structured systems. Two basic model structures were considered: the Hammerstein and the Wiener structures. The Hammerstein structure is a cascade connection of a nonlinear zero-memory (N) system and a linear dynamic process (L). This structure predicts that frequency and VT dependences of Rti and Eti are decoupled. The Wiener structure is an inverse cascade of these two blocks (i.e., L-N) in which the frequency and VT dependences of Rti and Eti are coupled. These two structures were combined with a nonlinear airway compartment and fitted to measured airway opening and alveolar capsule pressure-flow time domain data in dogs before and after histamine-induced constriction. The best lung model was a linear airway compartment combined with a Wiener structure consisting of a constant-phase linear tissue impedance in cascade with a polynomial nonlinearity, suggesting that frequency and VT dependences of Rti and Eti are indeed coupled during control and constricted conditions. Moreover, histamine caused much larger changes in the linear tissue parameters than in the nonlinear coefficients.

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Rangachari, P. K., T. Prior, R. A. Bell, and T. Huynh. "Histamine potentiation by hydroxylamines: structure-activity relations; inhibition of diamine oxidase." American Journal of Physiology-Gastrointestinal and Liver Physiology 263, no. 5 (November 1, 1992): G632—G641. http://dx.doi.org/10.1152/ajpgi.1992.263.5.g632.

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Hydroxylamines potentiated the responses of the canine colonic epithelium to histamine but not to other agonists such as serotonin or carbachol. We tested the hypothesis that an inhibition of histamine catabolism could explain the observed potentiation. A clear structure activity relation was defined, active compounds having the structure NH2-O-R, R being a simple uncharged aliphatic group. Active compounds delayed the disappearance of histamine from the bathing solutions and inhibited colonic diamine oxidase, an effect mimicked by standard inhibitors aminoguanidine and semicarbazide. Histamine agonists that possessed an imidazole nucleus (2- and 4-methylhistamine) were affected, whereas impromidine, 2 pyridylethylamine, and dimaprit were not. Agonist specificity combined with the enzyme data suggest an inhibition of histamine catabolism as a possible mechanism for the potentiating effects observed.

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Cole, L. B., and E. M. Holt. "Structure of (histamine.2H+)(ZnCl4)." Acta Crystallographica Section C Crystal Structure Communications 46, no. 9 (September 15, 1990): 1737–39. http://dx.doi.org/10.1107/s0108270190002773.

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Jin, Cong-Yu, Hong Wei, Kaj Karlstedt, and Antti Pertovaara. "Histamine in the locus coeruleus attenuates neuropathic hypersensitivity." Scandinavian Journal of Pain 4, no. 4 (October 1, 2013): 259–60. http://dx.doi.org/10.1016/j.sjpain.2013.07.015.

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AbstractAimsAmong brain structures receiving efferent projections from the histaminergic tuberomammillary nucleus is the pontine locus coeruleus (LC), a structure involved in descending noradrenergic control of pain. Here we studied whether histamine in the LC is involved in descending regulation of neuropathic hypersensitivity.MethodsPeripheral neuropathy was induced by unilateral spinal nerve ligation (SNL) in the rat with a chronic intracerebral and intrathecal catheter for drug administrations. Mechanical hypersensitivity in the injured limb was assessed by monofilaments. Heat nociception was assessed by determining radiant heat-induced paw flick.ResultsHistamine in the LC (ipsilateral to nerve injury) produced a dose-related (1–10 μg) mechanical antihypersensitivity effect (maximum effect at 15 min and duration of effect 30 min), without influence on heat nociception. Pretreatment of LC with zolantidine (H2 receptor antagonist), but not with pyrilamine (H1 receptor antagonist), reversed the antihypersensitivity effect of histamine. Zolantidine or pyrilamine alone in LC failed to influence pain behavior. The antihypersensitivity effect induced by histamine in LC was reduced also by spinal administration of atipamezole (an α2-adrenoceptor antagonist).ConclusionsThe results indicate that histamine acting on H2 receptors in the LC attenuates mechanical hypersensitivity in peripheral neuropathy. The histamine-induced descending antihypersensitivity effect is at least partly mediated by noradrenergic pathways acting on the spinal α2-adrenoceptor.

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Tikhonov, Denis S., Anatolii N. Rykov, Olga E. Grikina, and Leonid S. Khaikin. "Gas phase equilibrium structure of histamine." Physical Chemistry Chemical Physics 18, no. 8 (2016): 6092–102. http://dx.doi.org/10.1039/c5cp07719b.

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Dissertations / Theses on the topic "Structure of histamines"

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Bannister, C. "Structural relationships in H1 and H2 histamine antagonists and some other compounds of interest to the medicinal chemist." Thesis, University of Oxford, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.379939.

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Geng, Tian. "Structural studies on histamine receptors." Thesis, Imperial College London, 2015. http://hdl.handle.net/10044/1/56628.

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The work presented in this thesis concerns a sub-family of the biologically important family of G-protein coupled receptors (GPCRs) known as histamine receptors. They are recognized as important drug targets for many disorders in mankind, such as allergic rhinitis and Alzheimer’s disease. This thesis has its roots in the first structure of histamine receptor H1, determined in complex with a first generation antihistamine (doxepin) in 2011. Here, extensive biological, computational and structural investigations have been carried out for H1 in complex with two second-generation antihistamines (cetirizine and fexofenadine). Crystal structures of H1-cetirizine (3.1 Å) and H1-fexofenadine (3.4 Å) show the binding modes of second-generation antihistamines correspond well with the previous docking studies. The so-called “anion binding site” on H1 is responsible for the high specificity of the ligands. Some regions on the receptor were difficult to define in the crystal structures. These regions were characterized by radioligand binding assays, together with molecular dynamic simulations (carried out by our collaborators from Oxford University) suggested that, second generation ligands have a significantly large impact on receptor dynamics. While H1 mediates many immune-related disorders, the histamine receptor H3 is a drug target to many mental disorders. In addition to the H1 work presented here, it is also reported the initial work done on the histamine receptor H3. With extensive screenings on various H3 constructs (from human and turkey organisms) and expression systems, it was observed that the best construct was from turkey. An optimal expression protocol in insect cells was obtained. This has established a secure starting point for future structural studies on H3.

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Cooper, David Gwyn. "Structure-activity in pyridine-containing histamine receptor antagonists." Thesis, Imperial College London, 1987. http://hdl.handle.net/10044/1/38269.

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Adams, Peter Laurence. "Structural biology of some proteins involved in some pathogenic states." Thesis, University of Oxford, 1999. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.301785.

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Thaw, Paul. "Structural studies of p23'f'y'p : a translationally controlled tumour protein." Thesis, University of Sheffield, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.341815.

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Gajda, Tamas Pal. "Équilibres et structure des complexes de métaux de transition avec des peptidoamines contenant l'histamine." Nancy 1, 1993. http://www.theses.fr/1993NAN10141.

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Nous avons synthétisé de nouvelles molécules pseudo-peptidiques a base d'histamine: -alanyl-histamine, glycyl-histamine, sarcosyl-histamine etglycyl-glycyl-histamine. Les études cristallographique, RMN solide et liquide de ces molécules sous forme de chlorhydrates ont été réalisées. L'utilisation des différentes techniques (ph-métrie, rmn #1h, #1#3c et #1#4n) nous a offert la possibilité d'étudier la protonation, micro-protonation et le tautomerisme des produits synthétisés. La complexation des ligands avec les ions cobalt(II), nickel(II), cuivre(ii) et zinc(II) a été examinée. La richesse des informations obtenues par ph-métrie, spectrométrie UV-visible, RPE et RMN nous a permis de déterminer la nature et la structure des espèces formées en solution. Quoique de formulation très voisine, les divers ligands conduisent à une gamme très variée de complexes, parfois très différents soit par leur nature soit par leur stabilité

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Igel, Patrick. "Synthesis and structure-activity relationships of N G -acylated arylalkylguanidines and related compounds as histamine receptor ligands : searching for selective H4R agonists." kostenfrei, 2008. http://www.opus-bayern.de/uni-regensburg/volltexte/2009/1107/.

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Geyer, Roland [Verfasser], and Armin [Akademischer Betreuer] Buschauer. "Hetarylalkyl(aryl)cyanoguanidines as histamine H4 receptor ligands: Synthesis, chiral separation, pharmacological characterization, structure-activity and -selectivity relationships / Roland Geyer. Betreuer: Armin Buschauer." Regensburg : Universitätsbibliothek Regensburg, 2011. http://d-nb.info/1023276240/34.

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Arnould, Jean-Marie. "De la carcirine des crabes à la carnosine des vertébrés : De nouvelles voies métaboliques de l'histamine." Nancy 1, 1987. http://www.theses.fr/1987NAN10126.

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Birnkammer, Tobias [Verfasser], and Armin [Akademischer Betreuer] Buschauer. "Highly potent and selective acylguanidine-type histamine H2 receptor agonists: synthesis and structure-activity relationships of mono- and bivalent ligands / Tobias Birnkammer. Betreuer: Armin Buschauer." Regensburg : Universitätsbibliothek Regensburg, 2011. http://d-nb.info/1022872559/34.

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Book chapters on the topic "Structure of histamines"

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Yamatodani, A., N. Inagaki, P. Panula, N. Itowi, T. Watanabe, and H. Wada. "Structure and Functions of the Histaminergic Neurone System." In Histamine and Histamine Antagonists, 243–83. Berlin, Heidelberg: Springer Berlin Heidelberg, 1991. http://dx.doi.org/10.1007/978-3-642-75840-9_16.

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van der Goot, H., A. Bast, and H. Timmerman. "Structural Requirements for Histamine H2 Agonists and H2 Antagonists." In Histamine and Histamine Antagonists, 573–748. Berlin, Heidelberg: Springer Berlin Heidelberg, 1991. http://dx.doi.org/10.1007/978-3-642-75840-9_27.

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Buschauer, Armin, and Gert Baumann. "Structure-Activity Relationships of Histamine H2-Agonists, a New Class of Positive Inotropic Drugs." In New Perspectives in Histamine Research, 231–56. Basel: Birkhäuser Basel, 1991. http://dx.doi.org/10.1007/978-3-0348-7309-3_15.

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Shiroishi, Mitsunori, and Takuya Kobayashi. "Structural Analysis of the Histamine H1 Receptor." In Handbook of Experimental Pharmacology, 21–30. Cham: Springer International Publishing, 2016. http://dx.doi.org/10.1007/164_2016_10.

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Swenson, R. E., N. A. Mort, F. Haviv, E. N. Bush, G. Diaz, G. Bammert, N. Rhutasel, et al. "Structure-activity relationships of positions 7, 8, and 9 in LHRH antagonists with respect to histamine release, LH, and testosterone suppressions." In Peptides, 452–54. Dordrecht: Springer Netherlands, 1994. http://dx.doi.org/10.1007/978-94-011-0683-2_150.

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Panula, Pertti, CongYu Jin, Kaj Karlstedt, and Remko A. Bakker. "Phylogeny, Gene Structure, Expression, and Signaling." In The Third Histamine Receptor, 83–102. CRC Press, 2008. http://dx.doi.org/10.1201/9781420053937-4.

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Panula, Pertti, CongYu Jin, Kaj Karlstedt, and Remko Bakker. "Phylogeny, Gene Structure, Expression, and Signaling." In The Third Histamine Receptor, 83–101. CRC Press, 2008. http://dx.doi.org/10.1201/9781420053937.secb.

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Parambil Safna Hussan, Kodakkat, Indulekha Jayarajan Jithin Raj, Sailaja Urpayil, and Mohamed Shahin Thayyil. "Studies on Histamine H2-Receptor Antagonists by Using Density Functional Theory." In Drug Design - Novel Advances in the Omics Field and Applications [Working Title]. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.95322.

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Density functional theory (DFT) is a quantum mechanical approach used to investigate the electronic structure (principally the ground state) of many-body systems, in particular atoms, molecules, and the condensed phases. In this work, we have used DFT/B3LYP/6-31+G(d) level of theory to get insight into the molecular geometry and thermochemical properties of histamine H2-receptor antagonists. Histamine H2-receptor antagonists or H2 blockers are a group of pharmaceutical ingredients that reduce the amount of acid produced by the cells in the lining of the stomach. The potential H2 blockers include cimetidine, famotidine, nizatidine, and ranitidine. The detailed theoretical investigation on the listed H2 blockers in terms of their thermochemical parameters and global descriptive parameters revealed that, though famotidine is the best among them with highest Gibbs free energy, nizatidine showed higher biological activity with high softness, low hardness, and high electrophilicity index. The theoretical vibrational spectra of these four Histamine H2-receptor antagonists were analyzed and the infrared spectra of nizatidine was compared with the experimental IR spectra, and found to be good agreement with the experimental values. Further, frontier molecular orbitals especially the highest occupied molecular orbital (HOMO) and the lowest unoccupied molecular orbital (LUMO) were determined and the activation energy of the selected samples were calculated. In addition to this, the amorphisation technique were employed to enhance the solubility and bio availability of the best biologically active H2 blocker nizatidine using broadband dielectric spectroscopy.

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"Structure and Classiﬁcation of H1-Antihistamines and Overview of Their Activities." In Histamine and H1-Antihistamines in Allergic Disease, 81–116. CRC Press, 2002. http://dx.doi.org/10.3109/9780203910375-8.

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Kim, Soo-Kyung, and William A. Goddard III. "Molecular-Docking-Based Drug Design and Discovery." In Pharmaceutical Sciences, 656–82. IGI Global, 2017. http://dx.doi.org/10.4018/978-1-5225-1762-7.ch025.

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Currently 30-50% of drug targets are G Protein-Coupled Receptors (GPCRs). However, the clinical useful drugs for targeting GPCR have been limited by the lack of subtype selectivity or efficacy, leading to undesirable side effects. To develop subtype-selective GPCR ligands with desired molecular properties, better understanding is needed of the pharmacophore elements and of the binding mechanism required for subtype selectivity. To illustrate these issues, we describe here three successful applications to understand the binding mechanism associated with subtype selectivity: 5-HT2B (5-Hydroxytryptamine, 5-HT) serotonin receptor (HT2BR), H3 histamine receptor (H3HR) and A3 adenosine receptor (A3AR). The understanding of structure-function relationships among individual types and subtypes of GPCRs gained from such computational predictions combined with experimental validation and testing is expected the development of new highly selective and effective ligands to address such diseases while minimizing side-effects.

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