*  Baclofen | CAS#1134-47-0 | GABA-B Antagonist | MedKoo
Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to ... Description: Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid ... positive allosteric modulators in the DBA/2J audiogenic seizure test: Comparison to baclofen and utility as a pharmacodynamic ... 5-HT Receptor * 19 GPCR & G Protein * Adenosine Receptor * Adrenergic Receptor * cAMP ...
  http://www.medkoo.com/products/7150
*  CALM2 calmodulin 2 [Homo sapiens (human)] - Gene - NCBI
... receptors form a family of heterodimeric receptors that have specific alpha chains but share a common beta... ... Adrenergic signaling in cardiomyocytes, organism-specific biosystemCardiac myocytes express at least six subtypes of adrenergic ... biosystemNMDA receptors are a subtype of ionotropic glutamate receptors that are specifically activated by a glutamate agonist ... as once it enters the cytoplasm it exerts allosteric regulatory affects on many enzymes and proteins. Calcium can act in signal ...
  https://www.ncbi.nlm.nih.gov/gene/805
*  Chronic Treatment with Escitalopram but Not R-Citalopram Translocates Gαs from Lipid Raft Domains and Potentiates Adenylyl...
2005) Beta-adrenergic receptor stimulation promotes G alpha s internalization through lipid rafts: a study in living cells. Mol ... 1989) Guanosine-5′-O-thiodiphosphate functions as a partial agonist for the receptor-independent stimulation of neural ... 2007) Allosteric effects of R- and S-citalopram on the human 5-HT transporter: evidence for distinct high- and low-affinity ... citalopram was not seen to alter β-receptor-elicited cyclic AMP accumulation or β-receptor density (Sapena et al., 1994). We ...
  http://jpet.aspetjournals.org/content/332/3/977.full
*  5-HT2B receptor - Wikipedia
... failing heart and antagonists of 5-HT2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic agonist- ... positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor ... and tumor necrosis factor-alpha cytokine production by ventricular fibroblasts". Circulation. 110 (8): 969-74. doi:10.1161/01. ... "The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo". British Journal of ...
  https://en.wikipedia.org/wiki/5-HT2B_receptor
*  Δ-opioid receptor - Wikipedia
Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl- ... opioid receptors have been shown to interact with β2 adrenergic receptors, arrestin β1 and GPRASP1. K-opioid receptor μ-opioid ... Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E (Feb 2006). "Cannabidiol is an allosteric modulator at mu- and delta- ... The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR, is an inhibitory 7- ...
  https://en.wikipedia.org/wiki/%CE%94-opioid_receptor
*  Frontiers | Targeting protein-protein interactions in complexes organized by A kinase anchoring proteins | Pharmacology
Lbc-signaling complex mediates alpha1 adrenergic receptor-induced cardiomyocyte hypertrophy. Proc. Natl. Acad. Sci. U.S.A. 104 ... Kenakin, T., and Miller, L. J. (2010). Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric ... 2004). Protein kinases C and D mediate agonist-dependent cardiac hypertrophy through nuclear export of histone deacetylase. Mol ... It was also shown that due to α-adrenergic receptor stimulation, AKAP-Lbc assembles RhoA effectors PKNα, MLTK, MKK3 leading to ...
  https://www.frontiersin.org/articles/10.3389/fphar.2015.00192/full
*  Frontiers | Citicoline: A Food Beneficial for Patients Suffering from or Threated with Glaucoma | Frontiers in Aging...
... and a selective α2 adrenergic receptor agonist (brimonidine). However, treatment of POAG is frequently ineffective. Randomized ... 2015). Soluble tumor necrosis factor alpha promotes retinal ganglion cell death in glaucoma via calcium-permeable AMPA receptor ... a positive allosteric modulator of these receptors, has been proposed as a new approach to schizophrenia treatment (Deutsch et ... Choline is a selective agonist of alpha7 nicotinic acetylcholine receptors in the rat brain neurons. Eur. J. Neurosci. 9, 2734- ...
  https://www.frontiersin.org/articles/10.3389/fnagi.2016.00073/full
*  G protein-coupled receptor - Mashpedia Free Video Encyclopedia
The human beta-2 adrenergic receptor in complex with the partial inverse agonist carazolol.[1] ... The rate of GTP hydrolysis is often accelerated due to the actions of another family of allosteric modulating proteins called ... the GPCR reorganizes to allow activation of G-alpha proteins. The side perspective is a view from above and to the side of the ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors ( ...
  http://www.mashpedia.com/G-protein_coupled_receptor
*  Publications | Paul Scherrer Institut (PSI)
Backbone NMR reveals allosteric signal transduction networks in the beta1-adrenergic receptor Isogai S, Deupi X, Opitz C, ... Structural insights into agonist-induced activation of G-protein-coupled receptors Deupi X, Standfuss J CURRENT OPINION IN ... Pironetin Binds Covalently to alpha Cys316 and Perturbs a Major Loop and Helix of alpha-Tubulin to Inhibit Microtubule ... Structure of beta-Adrenergic Receptors Brueckner Florian, Piscitelli Chayne L, Tsai Ching-Ju, Standfuss Joerg, Deupi Xavier, ...
  https://www.psi.ch/lbr/publications
*  The endogenous molecular clock orchestrates the temporal separation of substrate metabolism in skeletal muscle | Skeletal...
actinin alpha 3. Adrb2: β2-adrenergic receptor. Adrbk1: adrenergic receptor kinase, beta 1 ... A potent allosteric activator of PFKM is fructose-2,6-bisphosphate, which is the product of the other phosphofructokinase ... Agonist (that is, catecholamine) binding is well established to evoke a cell-signaling cascade that promotes glucose uptake, ... The beta-adrenergic receptor is a substrate for the insulin receptor tyrosine kinase. J Biol Chem. 1996;271:1061-4.PubMedView ...
  https://skeletalmusclejournal.biomedcentral.com/articles/10.1186/s13395-015-0039-5
*  Muscarinic Acetylcholine Receptor Function - Proteins > Membrane Proteins > Plasma Membrane Proteins > Receptors > Muscarinic...
Muscarinic Acetylcholine Receptor Function - Proteins > Membrane Proteins > Plasma Membrane Proteins > Receptors > Muscarinic ... Acetylcholine Receptor - Reviews - Review Articles on Protein Expression, Structure, Function, and Interactions ... has been used to demonstrate that the m4 receptor preferentially couples to Gi alpha-2 or Go alpha over Gi alpha-1 or Gi alpha- ... This system has also been used to demonstrate that beta-arrestin1 and beta-adrenergic receptor kinase-1 act synergistically to ...
  http://biologicalworld.com/articles/modules/smartsection/item.php?itemid=133
*  Plus it
These receptors, also termed G protein-coupled receptors (GPCRs), act as guanine nucleotide exchange factors upon agonist ... 1998) The beta2-adrenergic receptor interacts with the Na+/H+-exchanger regulatory factor to control Na+/H+ exchange. Nature ... 1997) The juxtamembrane, cytosolic region of the epidermal growth factor receptor is involved in association with alpha-subunit ... This interaction mediates cell-cell adhesion (dotted arrow). Gα12/13 interaction with E-cadherin produces an allosteric effect ...
  http://molpharm.aspetjournals.org/content/78/1/12
*  Joseph (Jody) Puglisi | Stanford Medicine Profiles
... adrenergic receptor: a salt bridge linking extracellular loops 2 and 3. Small-molecule drugs that bind within the transmembrane ... Allosteric coupling of GTP hydrolysis by elongation factor Tu (EF-Tu) at the ribosomal GTPase center to messenger RNA (mRNA) ... The solution structure is composed of three major alpha-helices packed in a bundle with three additional short helices in ... core and exhibit different efficacies towards G-protein activation (agonist, neutral antagonist and inverse agonist) also ...
  https://med.stanford.edu/profiles/joseph-puglisi
*  Frontiers | Cannabinoids Modulate Neuronal Activity and Cancer by CB1 and CB2 Receptor-Independent Mechanisms | Pharmacology
Considering the CNS and cancer together allows identification of non-cannabinoid receptor targets that are shared and divergent ... Considering the CNS and cancer together allows identification of non-cannabinoid receptor targets that are shared and divergent ... other receptor types; ion channels; transporters; enzymes, and other protein- and non-protein cellular structures. This review ... other receptor types; ion channels; transporters; enzymes, and other protein- and non-protein cellular structures. This review ...
  https://www.frontiersin.org/articles/10.3389/fphar.2017.00720/full
*  Protocols and Video Articles Authored by Junmin Peng
Retinoid receptor agonists reversed this phenotype, partly by inducing expression of IKZF1, resulting in abrogation of adhesion ... PHD2/3-dependent Hydroxylation Tunes Cardiac Response to β-adrenergic Stress Via Phospholamban The Journal of Clinical ... and a positive allosteric modulator (PAM), ML382, of MRGPRX1. Cellular studies suggested that ML382 enhances the ability of ... alpha-, beta-, and delta-catenins, and CDKL5. Mutations of CDKL5 are associated with early infantile epileptic encephalopathy-2 ...
  https://www.jove.com/author/Junmin_Peng
*  pharm Flashcards - Cram.com
binds at DIFFERENT site from agonist. Can increase (allosteric activator) or decrease (allosteric antagonist)agonist activity. ... serpentine receptor snakes across the membrane 7 times--type of adrenergic receptor. EXTRACELLULAR--n terminal binds to NE, E, ... NE-catechol group, amino side chain α,β receptors. i.e. more potent at alpha receptor. EPINEPHRINE--same as NE, but w/ methyl ... How do chronic agonists alter a receptor? What about a chronic antagonist? Give examples of each. What are synonyms for each? ...
  http://www.cram.com/flashcards/pharm-322241
*  Structural Basis of CXCR4 Sulfotyrosine Recognition by the Chemokine SDF-1/CXCL12
Allosteric modulation of heterodimeric G-protein-coupled receptors. Trends Pharmacol Sci. 2007;28:615. [PubMed] ... High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science. 2007;318:1258. [ ... As a full agonist, wild-type SDF-1 induces a Ca2+ mobilization response and chemotactic migration. In measurements of THP-1 ... Three-dimensional structures of alpha and beta chemokines. Faseb J. 1995;9:57. [PubMed] ...
  http://pubmedcentralcanada.ca/pmcc/articles/PMC2692298/?lang=en-ca
*  USE OF NK-1 RECEPTOR ANTAGONIST SERLOPITANT IN PRURITUS - Patent application
... adrenergic agonists (e.g., clonidine), and carbonic anhydrase inhibitors (e.g., acetazolamide and topiramate), and analogs and ... at the GABAA receptor by positive allosteric modulation of the receptor, such as adinazolam, alprazolam, chlordiazepoxide, ... alpha Serotonin receptor antagonist (e.g., ondansetron) Spinal opioid-induced pruritus (concurrent with opioid) + opioid ... 0103] opioid receptor agonists, including but not limited to selective kappa opioid receptor agonists (e.g., asimadoline, ...
  http://www.patentsencyclopedia.com/app/20160143882
*  Protocols and Video Articles Authored by John Disterhoft (Translated to Hebrew)
GLYX-13 is a tetrapeptide (Thr-Pro-Pro-Thr) which acts as a NMDAR receptor partial agonist at the glycine site. GLYX-13 was ... a beta-adrenergic agonist that activates PKA, significantly reduced the AHP in CA1 neurons from control animals, but not from ... In the present study, we examined the effects of galantamine (3 mg/kg), a cholinesterase inhibitor and nAChR allosteric ... Jul, 2009 , Pubmed ID: 19245842 It has been well documented that alpha-calcium/calmodulin-dependent protein kinase II ( ...
  https://www.jove.com/author/John_Disterhoft?language=Hebrew
*  Frontiers | Palmitic Acid: Physiological Role, Metabolism and Nutritional Implications | Physiology
... increased ectopic fat accumulation and increased inflammatory tone via toll-like receptor 4. It is therefore likely that the ... 2005). The nuclear receptor peroxisome proliferator-activated receptor-alpha mediates the anti-inflammatory actions of ... it has been shown that treatment with endocannabinoid receptor agonist increased DNL in the mouse liver or in isolated ... Palmitoylation regulates intracellular trafficking of beta2 adrenergic receptor/arrestin/phosphodiesterase 4D complexes in ...
  https://www.frontiersin.org/articles/10.3389/fphys.2017.00902/full
*  Discovery of a Novel General Anesthetic Chemotype Using High-throughput Screening | Anesthesiology | ASA Publications
... the alpha(2) adrenergic sedative dexmedetomidine, and cannabinoid agonists.. J Pharmacol Exp Ther. (2006). 317 615-26 [Article] ... This probably represents allosteric inhibition, as is seen with bicuculline, but it could also reflect direct competition at ... Li, GD, Chiara, DC, Sawyer, GW, Husain, SS, Olsen, RW, Cohen, JB Identification of a GABAA receptor anesthetic binding site at ... We used an alpha value of 0.05 for significance (all significant findings had P , 0.05) and all analyses were two-tailed. ...
  http://anesthesiology.pubs.asahq.org/article.aspx?articleid=2091855
*  Insulin - New World Encyclopedia
The sympathetic nervous system (via α2-adrenergic agonists such as norepinephrine) inhibits the release of insulin. ... Effect of insulin on glucose uptake and metabolism. Insulin binds to its receptor (1) which in turn starts many protein ... alpha cells) forces release of glucose into the blood from cellular stores, primarily liver cell stores of glycogen. By ... Modification of the activity of numerous enzymes (allosteric effect).. The actions of insulin on cells include:. *Increased ...
  http://www.newworldencyclopedia.org/entry/Insulin
*  Plus it
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor ... α1D-adrenergic receptor, the GABAA receptor, phosphodiesterase 4, and the cardiac sodium channel NaV1.5. However, compound A ... d-alpha tocopheryl polyethylene glycol 1000 succinate (10:85:5). Plasma was sampled out to 24 hours (Fig. 4; Table 4). ... 2007) Allosteric enhancers, allosteric agonists and ago-allosteric modulators: where do they bind and how do they act? Trends ...
  http://jpet.aspetjournals.org/content/356/2/293
*  Hypnotic - Wikipedia
Zotepine Alpha-adrenergic agonist Clonidine Guanfacine Cannabinoids Cannabidiol Tetrahydrocannabinol Orexin receptor antagonist ... The principal mechanism of action of barbiturates is believed to be positive allosteric modulation of GABAA receptors. Examples ... In common use, the term antihistamine refers only to compounds that inhibit action at the H1 receptor (and not H2, etc.). ... Their mechanism of action is primarily at GABAA receptors. Nonbenzodiazepines are a class of psychoactive drugs that are very " ...
  https://en.wikipedia.org/wiki/Hypnotic
*  A New Molecular Mechanism To Engineer Protean Agonism at a G Protein-Coupled Receptor | Molecular Pharmacology
1996) Agonist-induced modulation of inverse agonist efficacy at the beta 2-adrenergic receptor. Mol Pharmacol 50:662-669. ... 1994) Determinants of alpha 2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state ... 1B). As the allosteric fragments are derived from allosteric antagonists/inverse agonists, the purely allosteric binding pose ... 2008) Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors. Br J Pharmacol 153:1353-1363. ...
  http://molpharm.aspetjournals.org/content/91/4/348