Receptor subtype
Membrane-displayed somatostatin activates somatostatin receptor subtype-2 heterologously produced in Saccharomyces cerevisiae
... G-protein-coupled receptor (GPCR) superfamily, which includes somatostatin receptors (SSTRs), is one of the most important drug targets in the pharmaceutical ...somatostatin receptor subtype-2 ...
8
Antihypertensive effects of selective prostaglandin E2 receptor subtype 1 targeting
... E-prostanoid receptor subtype 1 (EP1) in regulating blood ...EP1 receptor antagonist SC51322 reduced blood pressure in spontaneously hypertensive ...EP1 receptor inhibition, an EP1-null mouse ...
11
Lorcaserin and pimavanserin: emerging selectivity of serotonin receptor subtype–targeted drugs
... 5-HT receptor subtypes has been only occasionally ...5-HT receptor pharmacology and discusses two recent 5-HT receptor subtype–selective drugs, lorcaserin and pimavanserin, which target the ...
7
Prothrombotic effects of tumor necrosis factor alpha in vivo are amplified by the absence of TNF alpha receptor subtype 1 and require TNF alpha receptor subtype 2
... soluble receptor antagonists and mono- clonal antibodies have become a mainstay in therapy of RA and other chronic inflammatory ...regulated receptor subtype TNFR2 mediates tissue damage in chronic ...
13
First in class thyrotropin releasing hormone (TRH) based compound binds to a pharmacologically distinct TRH receptor subtype in human brain and is effective in neurodegenerative models
... Please cite this article as: Kelly, J.A., Boyle, N.T., Cole, N., Slator, G.R., Colivicchi, M.A., Stefanini, C., Gobbo, O.L., Scalabrino, G.A., Ryan, S.M., Elamin, M., Walsh, C., Vajda, A., Goggin, M.M., Campbell, M., ...
49
LRP1 is critical for the surface distribution and internalization of the NR2B NMDA receptor subtype
... performance. As shown in Figures 6B and 6D the ani- mals harboring LRP1 knock-in mutation demonstrate sig- nificant changes in spatial and reversal learning in MWM paradigm compared with the wild type littermates. While ...
16
Valium without dependence? Individual GABA<sub>A</sub> receptor subtype contribution toward benzodiazepine addiction, tolerance, and therapeutic effects
... 1 subtype. Recent investigations actu- ally showed that the α 1 subtype antagonist, α 2 , α 3 , and α 5 subtype partial agonist imidazenil was actually more potent than diazepam at attenuating ...
11
Pircher, Joachim (2011): The TNF-receptor subtype 2 mediates prothrombotic effects in vivo. Dissertation, LMU München: Medizinische Fakultät
... All animal experiments were performed in Wildtype (WT)- or TNF-receptor deficient C57-BL/6 mice. WT mice were purchased from Charles River, Sulzfeld, Germany. TNF-R1-/- and TNF-R2-/- mice were originally obtained ...
69
Evans Blue Attachment Enhances Somatostatin Receptor Subtype-2 Imaging and Radiotherapy
... SSTR2, the most ubiquitous and abundant subtype in tumor tissues, can activate or suppress various signal transduction pathways (2). Specific SSTR subtypes are expressed by a given tumor depending on tumor type, ...
11
Regulation of m4 muscarinic receptor gene expression
... which receptor subtypes mediate this effect but it is presumed to involve the projection from the ventral forebrain to the ...Muscarinic receptor involvement in memory is thought to be mediated, at least in ...
125
Induction of a negative autocrine loop by expression of sst2 somatostatin receptor in NIH 3T3 cells
... somatostatin receptor subtype sst2 mediates both acti- vation of a tyrosine phosphatase activity and inhibition of cell proliferation induced by somatostatin ...
11
Molecular and cellular mechanisms of nociception in equine laminitis: purinergic P2X receptors expression and distribution
... Purinergic receptor expression and function in nervous tissue has received considerable attention, particularly in relation to nerve-tissue injury models and neuronal plasticity (Gu & Heft 2004, Chessell et ...
196
Intestinal lipid–derived signals that sense dietary fat
... 1 receptor subtype — which is particularly abundant in the brain and spinal cord, but is also spread throughout the rest of the body (13) — increases food intake, enhances reward aspects of eating, and ...
9
Gadd45a levels in human breast cancer are hormone receptor dependent
... Figure 2 Gadd45A expression levels in human breast cancer samples are dependent on the hormone receptor subtype. (A) Box and Whisker Plots graphically depict the expression pattern of Gadd45a in the ...
6
Structure–activity study of N ((trans) 4 (2 (7 cyano 3,4 dihydroisoquinolin 2(1H) yl)ethyl)cyclohexyl) 1H indole 2 carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor
... It has become apparent that many class A GPCRs have at least one other topographically distinct, allosteric binding site that can be targeted by small molecules. 3-6 Ligands that behave as allosteric modulators may offer ...
81
Original Article The expression of transcription factor BORIS and its association with the estrogen receptor beta (ER-β) in cervical carcinogenesis
... estrogen receptor subtype expressed in the cervical epithelium and suggest that ER-β is the predominant estrogen receptor subtype ex- pressed in the neoplastic cervical epithelium, and its ...
14
Regulation of density of functional presynaptic terminals by local energy supply
... MgT: Magnesium-L-Threonate; N 5AP : Functional terminal density responding to 5AP bursts stimulation; NR2B: N-methyl D-aspartate receptor subtype 2B; NMDAR: N-methyl-D-aspartate receptor[r] ...
21
Confirmation of subtype of Alpha-1 adrenergic receptor producing relaxation in goat artery strip
... adrenergic receptor is divided into alpha 1 and 2. The alpha 1 receptor is further subdivided into alpha - 1A, 1B and ...adrenergic receptor is less effective in producing contraction in rabbit ...
97
A review of the pharmacoeconomics of eletriptan for the acute treatment of migraine
... Abstract: Migraine is a commonly occurring, chronic disorder that can cause significant disability. Eletriptan, a selective serotonin 5-hydroxytryptamine 1 receptor subtype B/D (5-HT 1B/1D ) agonist, is a ...
10
Clusters of specialized detector cells provide sensitive and high fidelity receptor signaling in intact endothelium
... gic receptor subtypes, each with various affinities, to pro- vide responses to ATP over a concentration range from 1 nM to 1 mM ...single receptor muscarinic receptor subtype (AChRM3) yet ...
14