Loading...


*  Index of biochemistry articles - Wikipedia
Allosteric site - allostery - allotrope - allotropy - alpha adrenergic receptor - Alpha helix - alpha-1 adrenergic receptor - ... adrenergic receptor - adrenodoxin - aequorin - aerobic respiration - agonist - alanine - albumin - alcohol - alcoholic ... alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - ... interferon receptor - interferon type I - interferon type II - interferon-alpha - interferon-beta - interleukin receptor - ...
  https://en.wikipedia.org/wiki/Index_of_biochemistry_articles
*  Etomidate - DrugBank
AAlpha-2B adrenergic receptor. agonist. Human. AGABA-A receptor (anion channel). positive allosteric modulator ... Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins ... Creagh O, Torres H, Rodriguez N, Gatica SR: Alpha-2B adrenergic receptor mediated hemodynamic profile of etomidate. P R Health ... The rank order of potency for agonists of this receptor is clonidine.... Gene Name. ADRA2B. Uniprot ID. P18089. Uniprot Name. ...
  https://www.drugbank.ca/drugs/DB00292
*  Alpha-2A adrenergic receptor - Wikipedia
... and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride ... identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology. 40 (2): ... The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the ... the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor ...
  https://en.wikipedia.org/wiki/Alpha-2A_adrenergic_receptor
*  Agmatine - Scientific Review on Usage, Dosage, Side Effects | Examine.com
Adrenergic Neurotransmission. Agmatine is known to interact with the alpha-2 (α2) subsets of the adrenergic receptors, and has ... Agmatine is an Imidazoline receptor agonist (activator) with fairly high affinity. Downstream of the imidazoline receptor lays ... of imidazoline receptors will augment signalling through the CB1 receptor via positive allosteric modification of the receptor ... Agmatine has high affinity for the alpha-2 adrenergic receptors, with little to no affinity for the alpha-1 subsets nor the ...
  https://examine.com/supplements/agmatine/
*  PAR-11-207: National Cooperative Drug Discovery/Development Groups (NCDDG) for the Treatment of Mental Disorders, Drug or...
Receptors: adenosine; adrenergic: alpha 1, alpha 2; cannabinoid: CB1, CB2; corticotropin releasing hormone: CRF R1, CRF R2; ... allosteric modulators, partial agonists, agonists, or antagonists), solubility, pharmacokinetics, oral or CNS bioavailability, ... receptors: NK1, NK2, NK3; heteromeric neuronal nicotinic receptor subunits; NMDA subunits; opioid receptors: mu, delta, kappa; ... Given the clinical availability of mu-opiate agonists, partial agonists and antagonists and the large number of NIDA-supported ...
  https://grants.nih.gov/grants/guide/pa-files/PAR-11-207.html
*  Evidence for the Role of Membrane Receptor Lateral Movement in GTP-Binding Protein-Mediated Signal Transduction | SpringerLink
... direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid ... Mechanism of agonist and antagonist binding to alpha 2 adrenergic receptors: evidence for a precoupled receptor-guanine ... Schlessinger J. Signal transduction by allosteric receptor oligomerization. Trends Biochem Sci 1988; 13: 443-447.PubMedCrossRef ... Agonist and antagonist binding to alpha 2-adrenergic receptors in purified mem branes from human platelets. Implications of ...
  https://link.springer.com/chapter/10.1007/978-1-4757-0680-2_5
*  Interactions of Hallucinogens with the Glutamatergic System: Permissive Network Effects Mediated Through Cortical Layer V...
Behavioral effects of beta adrenergic agonists and antidepressant drugs after down-regulation of beta-2 adrenergic receptors by ... Koskinen T, Haapalinna A, Sirvio J (2003) Alpha-adrenoceptor-mediated modulation of 5-HT2 receptor agonist induced impulsive ... A range of agonists or positive allosteric modulators (PAMs) for mostly Gi/o-coupled receptors, including metabotropic ... and selective metabotropic glutamate 2/3 receptor agonist: In vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-Amino-2- ...
  https://link.springer.com/chapter/10.1007%2F7854_2017_480
*  Research Interests for Edward D. Levin
Receptor, Serotonin, 5-HT2C, Receptors, Adrenergic, Receptors, Adrenergic, alpha-2, Receptors, Adrenergic, beta, Receptors, ... Serotonin 5-HT2 Receptor Agonists, Serotonin 5-HT2 Receptor Antagonists, Serotonin 5-HT3 Receptor Antagonists, Serotonin Agents ... Allosteric Regulation, alpha-Methyltyrosine, Alzheimer Disease, Amino Acids, Amino Acids, Branched-Chain, Amphetamine, Amygdala ... Receptors, Dopamine D1, Receptors, Dopamine D2, Receptors, GABA-B, Receptors, Glutamate, Receptors, Histamine H1, Receptors, ...
  http://fds.duke.edu/db/aas/pn/faculty/edlevin/research.html
*  Introduction to the Mobile Receptor Hypothesis | SpringerLink
... induces disulfide-linked IL-3 receptor alpha-and beta-chain heterodimerization, which is required for receptor activation but ... Schlessinger J. Signal transduction by allosteric receptor oligomerization. Trends Biochem Sci 1988; 13: 443-447.PubMedCrossRef ... Cassel D, Selinger Z. Mechanism of adenylate activation through the 13-adrenergic receptor: catecholamine-induced displacement ... Modification of fluid lipid and mobile protein fractions of reticulocyte plasma membranes affects agonist-stimulated adenylate ...
  https://link.springer.com/chapter/10.1007/978-1-4757-0680-2_1
*  Receptor antagonist - Wikipedia
Phenoxybenzamine is an example of an irreversible alpha blocker-it permanently binds to α adrenergic receptors, preventing ... as in allosteric binding sites. Antagonists mediate their effects through receptor interactions by preventing agonist-induced ... Agonists and antagonists "compete" for the same binding site on the receptor. Once bound, an antagonist will block agonist ... The rightward shift will occur as a result of a receptor reserve (also known as spare receptors) and inhibition of the agonist ...
  https://en.wikipedia.org/wiki/Receptor_antagonist
*  Methods of use of epsilon inhibitor compounds for the attenuation of pain - Patent # 8492346 - PatentGenius
Hool "Hypoxia increases the sensitivity of the L-type Ca(2+) current to beta-adrenergic receptor stimulation via a C2 region- ... "Rational design of a selective antagonist of epsilon protein kinase C derived from the selective allosteric agonist, pseudo- ... Claro et al., "alpha- and epsilon-protein kinase C activity during smooth muscle cell apoptosis in response to gamma-radiation ... Hodge et al., "Supersensitivity to allosteric GABA(A) receptor modulators and alcohol in mice lacking PKCepsilon", Nat. ...
  http://www.patentgenius.com/patent/8492346.html
*  Allosteric transition: a comparison of two models.
One is an allosteric two-state mechanical model derived in 2000 by David Hall. The other is an extended operational model dev ... Two recent models are in use for analysis of allosteric drug action at receptor sites remote from orthosteric binding sites. ... primary ligand, binds at orthosteric (primary) receptor binding site and covers ligands as agonists, inverse agonists and ( ... Ross EM,Maguire ME,Sturgill TW,Biltonen RL,Gilman AG,Relationship between the beta-adrenergic receptor and adenylate cyclaseJ ...
  http://www.biomedsearch.com/nih/Allosteric-transition-comparison-two-models/23298758.html
*  Adrenergic antagonist - Wikipedia
... allosteric site,allosteric site]]. A receptor's agonist does not bind to its allosteric binding site. The binding of a non- ... Alpha-2 Adrenergic Receptor Agonists: A Review of Current Clinical Applications, Giovannitti Jr, J. A., Thoms, S. M., & ... An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, ... Alpha-2 Adrenergic Receptor Agonists: A Review of Current Clinical Applications, Giovannitti Jr, J. A., Thoms, S. M., & ...
  https://en.wikipedia.org/wiki/Adrenergic_antagonist
*  Pathway and mechanism of drug binding to G-protein-coupled receptors | PNAS
2010) Conserved binding mode of human β2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography ... Homobivalent Conjugation Increases the Allosteric Effect of 9-aminoacridine at the {alpha}1-Adrenergic Receptors ... 1979) Fundamental difference between the molecular interactions of agonists and antagonists with the β-adrenergic receptor. ... β2-adrenergic receptors, initially making contact with a vestibule on each receptor's extracellular surface. Surprisingly, ...
  https://www.pnas.org/content/108/32/13118
*  Olney's lesions - Wikipedia
... barbiturates and agonists at the alpha-2 adrenergic receptor in the brain, such as clonidine. Conversely, coadministration of ... In medical settings, NMDA receptor antagonists are used as anesthetics, so GABAA receptor positive allosteric modulators are ... Jansen writes: Neuroscience portal NMDA receptor NMDA receptor antagonist Dissociative Neurotoxic drug Olney J, Labruyere J, ... NMDA-antagonists with alpha-2 adrenergic antagonists, like yohimbine could theoretically potentiate NAN. In Karl L. R. Jansen's ...
  https://en.wikipedia.org/wiki/Olney's_lesions
*  Metabotropic glutamate receptor 1 - Wikipedia
... highly potent and selective allosteric antagonist/inverse agonist A-841,720: potent non-competitive antagonist; minor hmGluR5 ... as mGluR1 antagonists block adrenergic receptor activation in neurons. Mice lacking functional glutamate receptor 1 were ... Group II and III receptors are linked to the inhibition of the cyclic AMP cascade but differ in their agonist selectivities. ... The metabotropic glutamate receptors are a family of G protein-coupled receptors, that have been divided into 3 groups on the ...
  https://en.wikipedia.org/wiki/Metabotropic_glutamate_receptor_1
*  Biological Profile of L-745,870, a Selective Antagonist with High Affinity for the Dopamine D4 Receptor | Journal of...
... compared to other dopamine receptor subtypes and had moderate affinity for 5HT2, sigma andalpha adrenergic receptors(IC50 , 300 ... 2C). To confirm functional selectivity of L-745,870, the ability of L-745,870 to reverse agonist-mediated inhibition of ... diltiazem allosteric site) was evaluated by displacement of [3H] diltiazem (60-87 Ci/mmol, NEN) binding to rabbit skeletal ... sigma and alphaadrenergic receptors (IC50 , 300 nM). It has been postulated that ion channel blocking properties of some ...
  http://jpet.aspetjournals.org/content/283/2/636
*  Frontiers | IL1R2, CCR2, and CXCR4 May Form Heteroreceptor Complexes with NMDAR and D2R: Relevance for Schizophrenia |...
... into neurons can form heteroreceptor complexes with NMDAR in the plasma membrane with pathological allosteric receptor-receptor ... It is therefore proposed that putative NMDAR- C-C chemokine receptor type 2 (CCR2), NMDAR- C-X-C chemokine receptor type 4 ( ... It is therefore proposed that putative NMDAR- C-C chemokine receptor type 2 (CCR2), NMDAR- C-X-C chemokine receptor type 4 ( ... into neurons can form heteroreceptor complexes with NMDAR in the plasma membrane with pathological allosteric receptor-receptor ...
  https://www.frontiersin.org/articles/10.3389/fpsyt.2017.00024/full
*  Probing Receptor Structure/Function with Chimeric G-Protein-Coupled Receptors | Molecular Pharmacology
Agonist-mediated downregulation of G alpha i via the alpha 2-adrenergic receptor is targeted by receptor-Gi interaction and is ... Galvez T, Duthey B, Kniazeff J, Blahos J, Rovelli G, Bettler B, Prezeau L, and Pin JP (2001) Allosteric interactions between ... α2A/α2C-adrenergic receptor third loop chimera show that agonist interaction with receptor subtype backbone establishes G ... Kobilka BK, Kobilka TS, Daniel K, Regan JW, Caron MG, and Lefkowitz RJ (1988) Chimeric alpha 2-,beta 2-adrenergic receptors: ...
  http://molpharm.aspetjournals.org/content/65/6/1323
*  William Weis | Stanford Medicine Profiles
... by an agonist-occupied receptor. The β(2) adrenergic receptor (β(2)AR) activation of Gs, the stimulatory G protein for adenylyl ... indicating that alpha-catenin is an allosteric protein. Significantly, alpha-catenin directly regulates actin-filament ... Using the inactive structure of the human β(2) adrenergic receptor (β(2)AR) as a guide, we designed a β(2)AR agonist that can ... adrenergic receptor (β(2)AR) that exhibits G protein-like behaviour, and obtained an agonist-bound, active-state crystal ...
  https://med.stanford.edu/profiles/william-weis
*  Physical dependence - Wikipedia
GABA agonists and positive allosteric modulators of both the GABA-A ionotropic receptor and GABA-B metabotropic receptor ... including beta blockers such as propanolol and alpha-adrenergic agonists such as clonidine androgenic-anabolic steroids ... but not agonists specific to non-µ opioid receptors, such as salvinorin A (a k-opioid agonist), nor opioid antagonists or ... The individual agents and drug classes in the anticonvulsant drug category act at many different receptors and it is not ...
  https://en.wikipedia.org/wiki/Physical_dependence
*  The role of the phosphatidyinositol-linked D1 dopamine receptor in the pharmacology of SKF83959. - Semantic Scholar
... mesulergine and was transiently attenuated by alpha1 adrenergic or D2 dopamine receptor antagonists, prazosin or spiperone, ... The present data provide the first evidence that the PI-linked D1 dopamine receptor plays a role in regulating motor activity ... The response was not affected by the serotonin receptor antagonist, ... suggesting that activation of the PI-linked D1 dopamine receptor and the PLC/IP3 pathway may be the underlying mechanism for ...
  https://www.semanticscholar.org/paper/The-role-of-the-phosphatidyinositol-linked-D1-dopa-Zhen-Goswami/78fbb3af10e0c2791e0583a65a57448fc0f00119
*  Specific inhibition of GPCR-independent G protein signaling by a rationally engineered protein | PNAS
2D). The same lack of effect by GBAi was observed when a different Gi-coupled GPCR was used [α2A-adrenergic receptor (α2A-AR)] ... 2006) Minimal determinants for binding activated G alpha from the structure of a G alpha(i1)-peptide dimer. Biochemistry 45: ... 2015) Universal allosteric mechanism for Gα activation by GPCRs. Nature 524:173-179. ... 1999) Overexpression of CALNUC (nucleobindin) increases agonist and thapsigargin releasable Ca2+ storage in the Golgi. J Cell ...
  http://www.pnas.org/content/114/48/E10319
*  Receptors and Centrally Acting Drugs Pharmacokinetics and Drug Metabolism - 1st Edition
Purchase Receptors and Centrally Acting Drugs Pharmacokinetics and Drug Metabolism - 1st Edition. Print Book & E-Book. ISBN ... and Alpha-Adrenergic Receptor Binding In Vitro. Stress, Adrenergic Agents and Infection. Clinical Pharmacology Of Mabuterol; A ... Allosteric Interactions at Convulsant Sites Coupled to GABA Receptor Ionophores. The Effect Of 2,3-Benzodiazepines on the ... Displacement Studies Among Different Opioid Agonists. Relationships Between the Suggested Opioid Receptors. Comparison of the ...
  https://www.elsevier.com/books/receptors-and-centrally-acting-drugs-pharmacokinetics-and-drug-metabolism/vizi/978-0-08-034191-0
*  PRKCH Gene - GeneCards | KPCL Protein | KPCL Antibody
Positive, Allosteric regulator. Protein kinase inhibitor,potent and cell permeable. 50. (-)-Epigallocatechin gallate (EGCG). * ... PKC family members also serve as major receptors for phorbol esters, a class of tumor promoters. Each member of the PKC family ... Conventional PKCs (cPKC alpha-, betaI- , betaII- and gamma-) are activated by phosphatidylserine in a calcium dependent manner ... Beta-agonist/Beta-blocker Pathway, Pharmacodynamics. *Proton Pump Inhibitor Pathway, Pharmacodynamics. *VEGF Signaling Pathway ...
  http://www.genecards.org/cgi-bin/carddisp.pl?gene=PRKCH&keywords=hsa-mir-1343-3p