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Tuesday, November 17, 2020 | History

1 edition of Development and characterisation of selective ion or molecular receptors. found in the catalog.

Development and characterisation of selective ion or molecular receptors.

Rachel F. Wall

Development and characterisation of selective ion or molecular receptors.

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Published .
Written in English


Edition Notes

Thesis (PhD) -- Dublin City University, 2003.

ID Numbers
Open LibraryOL15506523M

  Mulryan et al. () stated that P2X1 receptors are essential for normal male reproductive function and suggested that the development of selective P2X1 receptor antagonists may provide an effective nonhormonal male contraceptive pill. In addition, agents that potentiate the actions of ATP at P2X1 receptors may be useful in the treatment of.   Further studies have then directed toward pharmacological characterization of the 5-HT receptors in the nervous system and peripheral organs using radiolabelled ligands [7, 8] until the first molecular identity of the 5-HT receptor. In –s, 5-HT neurons have localized in the nervous system and peripheral organs (including gonad) of.


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Development and characterisation of selective ion or molecular receptors. by Rachel F. Wall Download PDF EPUB FB2

Development and characterisation of selective ion or molecular receptors Wall, Rachel F () Development and characterisation of selective ion or molecular receptors. PhD thesis, Dublin City University.

Full text available as: PDF - Requires a PDF viewer such as GSview, Xpdf or. Development and characterisation of selective ion or. Development and characterisation of selective ion or molecular receptors.

By Rachel F Wall. Get PDF (5 MB) Abstract. The research entailed the Synthesis and Charactensation of a range of Molecular Receptors The target receptor was a calix[4]arene denvative, possessing a tetrahedral ’pocket’ at the lower rim defined by four p endant Author: Rachel F Wall.

Recently, design and development of ion receptors that are capable of detection of bisulphate anion has recently been developed for potential applications in biological and chemical processes [, ]. The more hydrophilic bisulphate anion dissociates at elevated pH values to create toxic sulfate ions, which causes irritation of the mucosa, skin Author: Dhanushkodi Mohanasundaram, Gujuluva Gangatharan Vinoth Kumar, Senthuran Karthick Kumar, Balaji Madd.

1. Introduction. Selective recognition of lanthanides by molecular receptors or materials is an emerging field of research due to applications in imaging, MRI, catalysis, pharmaceutical therapies, etc.Lanthanides and metal complexes have been inspected as agents for different applications such as photonics, sensing, photodynamic therapy and radiation therapy.Author: Brij Mohan, Sandeep Kumar, Harish Kumar Sharma.

Ion channels are molecular pores that facilitate the passage of ions across cell membranes and participate in a range of biological processes, from excitatory signal transmission in the mammalian.

Metal Ion Recognition by 1α, 1β, and 1γ. First, to evaluate the response function of modified CyDs toward metal ions, the fluorescence spectra of 1α, 1β, and 1γ were measured in the presence of Mg 2+, Fe 3+, Co 2+, Ni 2+, Cu 2+, Zn 2+, Cd 2+, Pt 2+, and Pb 2+.The addition of Zn 2+ and Cd 2+ possessing full d-orbitals enhanced the fluorescence intensity on the basis of the PET.

The synthesis, characterization, and membrane-transport properties of a series of benzocrown and p-tert-butylcalix[4]arene-substituted polysiloxanes are described.

Receptor-functionalized po. The selective functionalization of macrocyclic receptors remains extremely challenging because it generally requires the transformation of one and only one functional group among several identical groups.

Recently, some of us described that the host–guest properties of a calix[6]arene-based Zn complex could be exploited for its selective monofunctionalization. To address the molecular basis for the striking allosteric effect of sodium on opioid receptor function, we crystallized the human δ-OR (residues 36–) with an N-terminal BRIL fusion protein [BRIL-δOR(ΔN/ΔC)] and determined the crystal structure in complex with the subtype-selective ligand naltrindole 7 at Å resolution (Fig.

1 and. New information from the structural characterization of ion channels, along with better understanding of ion channel function, may allow for more selective targeting. For example, Na+ channels underlying persistent Na+ currents or GABA(A) receptor isoforms responsible for tonic (extrasynaptic) currents represent attractive targets.

Because P2X receptors are not related to other ion channel proteins of known structure, there is at present no molecular foundation for mechanisms of ligand-gating, allosteric modulation and ion. Mammalian tachykinin receptors consist of three types based upon current pharmacological, biochemical, and molecular characterization.

These receptors have been named neurokinin-1 (NK 1), the receptor with highest affinity for SP; neurokinin-2 (NK 2), the receptor with highest affinity for NKA, NPK, and NPy; and neurokinin-3 (NK 3), the.

Background: Kappa opioid receptor (KOR) signaling may produce antinociception through G protein or dysphoria through βarrestin pathways. Results: Two highly selective, brain penetrant agonist scaffolds bias KOR signaling toward G protein coupling and produce antinociception in mice.

Conclusion: Described are first-in-class small molecule agonists that bias KOR signaling through G proteins. This book traces the origins of anion recognition chemistry as a unique sub-field in supramolecular chemistry, while illustrating the basic approaches currently being used to effect receptor.

Purchase Molecular Biology of Receptors and Transporters: Receptors, Volume B - 1st Edition. Print Book & E-Book.

ISBNThe common feature that allows neurons and other cells to respond to extracellular signals is the presence of specific receptors in the plasma membrane, which may be similar in their structure and functional properties in different kinds of cells.

There may be several different kinds of receptors for individual neurotransmitters. Many receptors can be grouped into families based on structural. Most recently, he has identified a new class of drugs, pharmacoperones, which act by regulating the intracellular trafficking of receptors, enzymes and ion channels.

He has authored or co-authored over publications in this area and written or edited over books, including texts in neurosciences, molecular biology and endocrinology. The selectivity of SB was defined by broad receptor profiling and other cellular assays in which it showed little or no activity versus a wide range of ion channels, receptors, and enzymes.

SB therefore represents a potent and selective multimodal TRPV1 antagonist, a pharmacological profile that has contributed to its definition. Rigorous characterization of the receptor-response system in the intact target cell is a crucial prerequisite for ultimately understanding the molecular basis for the physiological response observed in vivo, as it is only to the extent that the purified and reconstituted assembly mimics the native receptor-response system that the in vitro.

RECEPTORS Def: specific molecules in a biologic system with which drugs interact to produce changes in the function of the system. Receptors must be selective in their ligand -binding characteristics. Receptors also must be modified as a result of binding an agonist molecule.

The majority of the receptors characterized to date are proteins. N-methyl-d-aspartate receptors (NMDARs) are excitatory glutamatergic receptors that are fundamental for many neuronal processes, including synaptic plasticity.

NMDARs are comprised of four subunits derived from heterogeneous subunit families, yielding a complex diversity in NMDAR form and function. The quadruply-liganded state of binding of two glutamate and two glycine molecules to.

Further characterization of this particular molecule showed that the molecule selectively antagonized the B2-receptor relative to a panel with more than one hundred different molecular targets including G protein-coupled receptors, such as the bradykinin B1 receptor.

N-methyl-D-aspartate receptors (NMDARs) are glutamate-gated ion channels widely expressed in the central nervous system that play key roles in excitatory synaptic transmission. Because of their involvement in numerous neurological disorders, NMDARs.

The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor implicated in long term memory, consisting entirely of α7 subunits.

As with other nicotinic acetylcholine receptors, functional α7 receptors are pentameric [i.e., (α7) 5 stoichiometry]. It is located in the brain, spleen, and lymphocytes of lymph nodes where activation yields post. Theories Proposed Receptor occupancy theory: Clark () propounded a theory of drug action based on occupation of receptors by specific drugs.

The interaction between the two molecular species, viz. drug (D) and receptor (R) to be governed by the law of mass action, and the effect (E) to be a direct function of the drug-receptor complex (DR. The Androgen Receptor (AR), a member of the steroid hormone receptor family, plays important roles in the physiology and pathology of diverse tissues.

AR ligands, which include circulating testosterone and locally synthesized dihydrotestosterone, bind to and activate the AR to elicit their effects.

Published research papers, IUPHAR ('compendium of receptor characterisation and classification') i.e different receptors for same agonist found in same cells. IUPHAR International Union of Pharmacological Sciences - classification between receptors in isolation/tissue, agonist/antagonist effects.

Biological Activity. Potent and highly selective kainate receptor agonist, with an IC 50 for inhibition of [3 H]-kainate binding of 35 nM and almost 3, and fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.

Also selectively inhibits the cloned excitatory amino acid transporter EAAT2 at higher concentrations. Further characterization of this particular molecule showed that the molecule selectively antagonized the B2-receptor relative to a panel with more than one hundred different molecular.

Start studying molecular basis of receptors. Learn vocabulary, terms, and more with flashcards, games, and other study tools.

Search. ligand-gated ion, receptor tyrosine kinase, and cytosolic receptors. Selectivity- cation selective, exclusively on neurons. The tachykinin receptor 1 (TACR1) also known as neurokinin 1 receptor (NK1R) or substance P receptor (SPR) is a G protein coupled receptor found in the central nervous system and peripheral nervous endogenous ligand for this receptor is Substance P, although it has some affinity for other protein is the product of the TACR1 gene.

Molecular dynamics predicts that when proteins such as receptors change conformation, different regions of the receptor change independently (i.e., the protein does not form uniform global conformation) Signaling protein s interact with different regions of the receptor Unique receptor conformations stabilized by agonists most likely will.

Such receptors are tailored for efficient and selective crystallization, solvent extraction, ion exchange, and membrane transport. Applied efforts focus on optimizing promising receptors to perform practical separations for such applications as CO 2 capture, recovery and recycle of critical materials, recycle of used nuclear fuel, desalination.

@article{osti_, title = {Molecular mechanism of ATP binding and ion channel activation in P2X receptors}, author = {Hattori, Motoyuki and Gouaux, Eric}, abstractNote = {P2X receptors are trimeric ATP-activated ion channels permeable to Na{sup +}, K{sup +} and Ca{sup 2+}.

The seven P2X receptor subtypes are implicated in physiological processes that include modulation of synaptic. Ion channels are gated pores that open and close either intrinsically or in response to regulators such as changes in membrane voltage gradients.

They are found in the membranes of virtually all cell types throughout the human body. They regulate passage of ions like calcium, chloride, sodium, and potassium through cell membranes, in and out of cell organelles and play a roll in cell-to-cell. Support for the N-methyl-d-aspartate receptor (NMDAR) hypofunction hypothesis of schizophrenia has led to increasing focus on restoring proper glutamatergic signaling as an approach for treatment of this devastating disease.

The ability of metabotropic glutamate (mGlu) receptors to modulate glutamatergic neurotransmission has thus attracted considerable attention for the development. The amino acid sequences of many different ion channel proteins have been determined, and in a few cases the X-ray crystal structure of the channel is known as well.

Based on their structure, the majority of ion channels can be classified into six or seven superfamilies. For potassium-selective channels, which are among the best-characterized ion channels, four homologous transmembrane. A new Mg2+-selective fluorescent probe P was synthesized and characterized.

With optimal conditions, the proposed probe P showed good selectivity to Mg2+ compared to other common metal ions, and worked in a wide linear range of × 10−7– × 10−6 M with a detection limit of × 10−7 M Mg2+ in ethanol-water solution (, v/v, 20 mM HEPES, pH = ).

This book is geared to every student in biology, pharmacy and medicine who needs to become familiar with receptor mediated signaling. The text starts with explaining some basics in membrane biochemistry, hormone biology and the concept of receptor based signaling as the main form of communication between cells and of cells with the environment.

We are developing novel optogenetic reagents that allow us to systematically perturb specific ion channels and signaling receptors in a time- and amplitude-variant manner. We combine these molecular reagents into an experimental framework in which all families of ion channels and receptors can be independently controlled, and their contribution.Electronic books Conference papers and proceedings Congresses: Additional Physical Format: Print version: Molecular and functional diversity of ion channels and receptors.

New York: New York Academy of Sciences, (DLC) (OCoLC) Material Type: Conference publication, Document, Internet resource: Document Type.Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU (ML): a novel molecular probe.

ChemMedChem. Aug;9(8)