Protein coupled receptor 1996 alpha 1 receptor antagonists adrenergic alpha 1 receptor antagonists. Medical search. Frequent questions

The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example. (wikipedia.org)
Albuterol (Ventolin, Proventil), terbutaline (Brethine, Brethaire) and metaproterenol (Metaprel, Alupent) are classified as β 2 -selective adrenergic agonists and as such reduce smooth muscle tone. (pharmacology2000.com)
Natural regulators of brown and beige fat include external conditions like cold temperatures, and exercise, as well as internal mechanisms like thyroid hormones, beta-adrenergic hormones, retinoids, PPARγ and PPARα agonists, and the liver X receptor. (mrsupps.com)

Oxymetazoline is an example of a non-selective α-adrenergic receptor agonist. (pharmacology2000.com)
Isoproterenol (Isuprel, Isoprenaline) is a classical nonselective β-adrenergic agonist, with prominent actions at β 1 and β 2 receptors. (pharmacology2000.com)
Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
However, S1P 4 lies on the edge of the S1P family cluster and has been shown to bind S1P with lower affinity than other S1P receptors and hence it has been suggested that S1P is not the true endogenous agonist of this receptor [ 8 ]. (biomedcentral.com)
The agonist-liganded GPCR is normally at the mercy of phosphorylation by regulatory kinases (GRK1-6, G protein-coupled receptor kinases). (biotechpatents.org)

There are two main groups of adrenoreceptors, α and β, with 9 subtypes in total: α receptors are subdivided into α1 (a Gq coupled receptor) and α2 (a Gi coupled receptor) α1 has 3 subtypes: α1A, α1B and α1D α2 has 3 subtypes: α2A, α2B and α2C β receptors are subdivided into β1, β2 and β3. (wikipedia.org)
Phenoxybenzamine (PB) has been used to probe α-adrenergic receptor subtypes. (pharmacology2000.com)
[8] Other neurokinin subtypes and neurokinin receptors that interact with SP have been reported as well. (wikidoc.org)

We are primarily using cytomegaloviruses to examine how the pathogens alter signaling pathways directed by G-protein coupled receptors (GPCRs) to facilitate robust replication in tissues important for host-host dissemination. (uc.edu)
G protein-coupled receptors (GPCRs) belong to the largest class of drug targets. (mdpi.com)
[7] It belongs to the tachykinin receptor sub-family of GPCRs . (wikidoc.org)

The inhibition could be mimicked by the L-type calcium channel blocker nimodipine (1 μ m ) as well as by protein kinase C (PKC) activators phorbol 12,13-dibutyrate (10 μ m ) and phorbol 12-myristate 13-acetate (500 n m ), and blocked by the PKC inactivator (±)-1-(5-isoquinolinesulfonyl)-2-methylpiperazine (200 μ m ), suggesting a mechanism involving PKC modulation of L-type calcium channels. (jneurosci.org)
We tested the hypothesis that protein kinase C (PKC) participates in stimulus-secretion coupling. (jneurosci.org)
The ↑[Ca 2+ ] i activates a signaling cascade that involves, sequentially, calcium-calmodulin, nitric oxide synthase, guanylyl cyclase, and protein kinase G. This signal transduction pathway enables Cl − to pass through vesicular channels and act as a counterion for the transport of H + , so that the vesicles of secretogogue-stimulated cells become acidic. (jneurosci.org)
A long lasting β1 adrenergic receptor stimulation of cAMP/protein kinase A (PKA) signal in cardiac myocites. (cardiologymedjournal.com)
In 2001, mutations were discovered in the IKB kinase-complex-associated protein ( IKBKAP ) gene, with a major haplotype mutation located in the donor splice site of intron 20. (medscape.com)
In the past 10 years, it was valued that upon internalization, the complicated of GPCR and arrestin sets off a second circular of signals which involves nonreceptor tyrosine kinases from the SRC-family, MAP kinase family (ERK1/2, jun-N-terminal kinase, p38 MAP kinase etc.) and regulators of little G protein [32]. (biotechpatents.org)

The article is devoted to the endogenous sensitizer of beta-adrenergic receptor (ESBAR) - water-soluble low molecular weight substances, analogs of which are histidine, tryptophan, tyrosine, mildronat and preductal. (cardiologymedjournal.com)

this agent is a non-selective receptor blockers. (pharmacology2000.com)
An example of an 'irreversible' non-selective α-receptor blocker is phenoxybenzamine (Dibenzyline). (pharmacology2000.com)
Yohimbine is classified as a selective α 2 -adrenergic receptor antagonist. (pharmacology2000.com)
The lysophospholipid ligands of these receptors are structurally similar, however recognition of these lipids by these receptors is highly selective. (biomedcentral.com)

In June of that year, Raymond Ahlquist, Professor of Pharmacology at Medical College of Georgia, published a paper concerning adrenergic nervous transmission. (wikipedia.org)
In 1954, he was able to incorporate his findings in a textbook, Drill's Pharmacology in Medicine, and thereby promulgate the role played by α and β receptor sites in the adrenaline/noradrenaline cellular mechanism. (wikipedia.org)

Adrenaline or noradrenaline are receptor ligands to either α1, α2 or β-adrenoreceptors. (wikipedia.org)
Sphingosine-1-phosphate and lysophosphatidic acid (LPA) are ligands for two related families of G protein-coupled receptors, the S1P and LPA receptors, respectively. (biomedcentral.com)
Computational modelling of the interactions between these ligands and both wild type and mutant S1P 4 receptors showed excellent agreement with experimental data, therefore confirming the fundamental role of this residue in ligand recognition by S1P receptors. (biomedcentral.com)
of orthosteric ligands, (ii) the discussion surface area that recruits G protein and arrestins, (iii) the discussion sites of extra protein (GIPs, GPCR interacting protein that control G proteins signaling or bring about G protein-independent indicators). (biotechpatents.org)
This will become illustrated by concentrating on the ligand-based medication style of oxytocin (OT) and vasopressin (AVP) receptor ligands using organic peptide qualified prospects as starting factors. (biotechpatents.org)
They recognize extracellular signaling substances (ligands) of varied nature (as well as the canonical signaling pathway, the G-protein activation/inactivation routine. (biotechpatents.org)
Chances are that a assortment of brand-new ligands will emerge because high-throughput assays have already been developed to display screen for peptides that bind selectively to different conformations of G proteins subunits [50] or focus on the user interface with a particular subset of RGS protein [51]. (biotechpatents.org)

This section focuses on disease management using pharmacological interventions, namely -receptor antagonists. (pharmacology2000.com)

Turnock-Jones JJ, Jennings CA, Robbins MJ, Cluderay JE, Cilia J, Reid JL, Taylor A , Jones DN, Emson PC , Southam E. Increased expression of the NR2A NMDA receptor subunit in the prefrontal cortex of rats reared in isolation. (neurotree.org)

Parafollicular (PF) cells secrete 5-HT in response to stimulation of a G-protein-coupled Ca 2+ receptor (CaR) by increased extracellular Ca 2+ (↑[Ca 2+ ] e ). (jneurosci.org)
Amino acid residues that are responsible for the binding of SP and its antagonists are present in the extracellular loops and transmembrane regions of NK-1. (wikidoc.org)
One mechanism is the binding of an extracellular ligand to a transmembrane G-protein-coupled receptor (GPCR). (pancreapedia.org)
The receptor protein has seven transmembrane α-helices connected by alternating cytosolic and extracellular loops. (pancreapedia.org)
The ligand-binding site is in the extracellular domain and the cytosolic domain has a heterotrimeric G protein-binding site (127). (pancreapedia.org)
The receptors contain seven transmembrane-spanning Chelices, with an extracellular N-terminus, an intracellular C-terminus and 3 interhelical loops about each family member part from the membrane [1C3]. (biotechpatents.org)

PGC-1α is a transcriptional coactivator that binds to and activates transcription factors that regulate the genes involved in energy metabolism. (mrsupps.com)
These homologies, coupled with observed differences in the structure of S1P and LPA receptor genes, suggest that these receptor families evolved from distinct ancestral genes. (biomedcentral.com)
Using DNA microarray analysis, we identified several genes that are regulated by Wnt-5a and Rfz-2 as well as by Wnt-1. (biomedcentral.com)
We then focused on two genes previously linked to various cancers, mesothelin and stromelysin-1, which are respectively up-regulated by Wnt-1 and Wnt-5a in C57mg cells. (biomedcentral.com)

Whereas the above two example drugs show α-adrenergic receptor selectivity (α 1 vs. α 2 ), oxymetazoline activates both α 1 and α 2 adrenergic receptors. (pharmacology2000.com)
We tested whether mutation of this "ligand selectivity" residue to glutamine could confer LPA-responsiveness to the related S1P receptor, S1P 4 . (biomedcentral.com)
Glutamic acid in the third transmembrane domain of the S1P receptors is a general selectivity switch regulating response to S1P over the closely related phospholipids, LPA. (biomedcentral.com)
The Edg receptor family is classified into two clusters based on ligand selectivity: S1P 1/2/3/4/5 (formerly Edg1/5/3/6/8) specifically respond to S1P whilst LPA 1/2/3 (formerly Edg2/4/7) respond to LPA [ 5 ]. (biomedcentral.com)
In the present study, the role of this residue in determining ligand selectivity for the S1P 4 receptor was examined. (biomedcentral.com)

In hypothalamic neurons, modulators such as neuropeptide Y (NPY) and adenosine depress glutamatergic transmission by either a pertussis toxin (PTx)-sensitive G-protein-coupled pathway or by inhibition of voltage-activated calcium channels (VACCs). (jneurosci.org)
Chakraborti S, Roy S, Chowdhury A, Mandal A, Chakraborti T. Role of PKCα-p38 MAPK-Giα axis in peroxynitrite-mediated inhibition of β-adrenergic response in pulmonary artery smooth muscle cells. (cardiologymedjournal.com)

The α-adrenergic receptor is described by seven α-helical transmembrane (TM) domains which form a 'crevice' for ligand binding. (pharmacology2000.com)

In particular we are studying the role of eicosanoids in normal pregnancy and preeclampsia, the contribution of a purinergic receptor to the release of the cytokine interleukin-1beta in pregnancy as well as investigation of the inflammasome in coordinating inflammatory pathways coupled to cytokine release. (nottingham.ac.uk)
Because these regions are related to complexed signal transduction pathways mediated by cytokines , it has been proposed that cytokines and neurotropic factors can induce NK-1. (wikidoc.org)
We found members of the two DA receptor families (D 1 - and D 2 -like) associated with different signaling pathways in human GCs, namely D 1 (as expected) and D 5 (both are Gs coupled and linked to cAMP increase) and D 2 , D 4 (Gi/Gq coupled and linked to IP3/DAG). (biomedcentral.com)
Ovarian DA can act thus via D 1,2,4,5 , which are co-expressed by endocrine cells of the follicle and the corpus luteum and are linked to different signaling pathways. (biomedcentral.com)
Vertebrate Wnts signal through frizzled receptors that in some experimental contexts (e.g., without co-expressing LRP5/6) preferentially activate the Wnt/beta-catenin or Wnt/Ca 2+ pathways [ 5 ]. (biomedcentral.com)
Neuroendocrine system and autonomic nervous system are the two pathways that connect the central nervous system to the peripheral immune system [1]. (brainimmune.com)

By analyzing specific amino acid mutations of the α 2A - receptor with respect to changes in PB binding, certain sites were identified that may serve as the molecular target for phenoxybenzamine-mediated receptor blockade. (pharmacology2000.com)
This cysteine (at position 117) appears important in the association of phenoxybenzamine with receptor with PB likely covalently coupled to this amino acid. (pharmacology2000.com)
[1,2] Therefore, the amino acid may also help with adenosine triphosphate (ATP) production. (priceplow.com)
The central theme of this methodology is the formation of alpha -aminoalkyl radicals from existing amino acid and alpha -amino alcohol derivatives by 1,5-hydrogen atom transfer and the subsequent trapping of these radicals with appropriate radicalphiles, thus generating quaternary centres with high efficiency and excellent stereocontrol. (exeter.ac.uk)
Tryptophan (TRP) is an essential dietary amino acid that, unless otherwise committed to protein synthesis, undergoes metabolism via the Tryptophan-Kynurenine (TRP-KYN) pathway in vertebrate organisms. (mdpi.com)

After a ligand binds to the GPCR, it activates a heterotrimeric G-protein, which is composed of three subunits: a guanine nucleotide binding α-subunit, and a βγ-heterodimer (98). (pancreapedia.org)
Depending on which family the G protein is, it goes on to activate (G αs protein subunit) or inhibit (G αi protein subunit) the membrane-bound cyclase. (pancreapedia.org)

This interaction precludes the recruitment of G protein and network marketing leads to desensitization of G protein-dependent signaling [31] thus. (biotechpatents.org)

Activation of this receptor type centrally reduces sympathetic outflow, which is the proposed mechanism that accounts for antihypertensive actions noted following clonidine administration. (pharmacology2000.com)
Some of the receptors are cation channels, which can directly depolarize the nociceptor upon activation, while other receptors activate second messenger systems to change neuronal excitability by changing expression of, or modifying the function of, other cation channels. (frontiersin.org)
These results indicate a length restriction for activation of this receptor and demonstrate the utility of using LPA-responsive S1P receptor mutants to probe binding pocket length using readily available LPA species. (biomedcentral.com)
Some of these responses reflect activation of G protein-coupled receptors of the endothelial differentiation gene (Edg) family. (biomedcentral.com)

The results of the 20 years studies of the presence in blood serum and other body fluids of endogenous modulators of adrenergic and M-cholinergic impact as a component of humoral link of autonomic nervous system. (cardiologymedjournal.com)

adrenergic receptor antagonists i.e. typically propranolol (Inderal) are used in management of hypertrophic obstructive cardiomyopathy. (pharmacology2000.com)

These data suggest that glutamate, acting at several metabotropic receptors expressed by astrocytes, could modulate glial activity evoked by neurotransmitters and thereby influence the ongoing modulation of neurons by astrocytes. (jneurosci.org)

Wnts in this functional class activate the canonical Wnt/beta-catenin pathway (Wnt-1, -3A, and -8). (biomedcentral.com)

Interestingly, Wnt-5a may couple to either pathway depending on which frizzled receptor is present. (biomedcentral.com)

This cyclic conformation allows cyclic nucleotides to bind to proteins to which other nucleotides cannot. (pancreapedia.org)
Identification of convert motifs generally just involves interactions from the spatially-orientated aspect chain residues from the ligand using the receptor plus they can as a result be looked at as scaffolds, that could theoretically end up being substituted by choice rigid (+)-Camphor non-peptidic scaffolds that keep up with the useful aspect chains in the proper conformation. (biotechpatents.org)

glutamate receptor, ionotropic, NMDA1. (wikigenes.org)

The effectiveness of adrenergic antagonists in this setting is likely due to reduced outflow tract pressure gradients. (pharmacology2000.com)

While the latter conclusion was subsequently shown to be incorrect (it is now known to be noradrenaline), his receptor nomenclature and concept of two different types of detector mechanisms for a single neurotransmitter, remains. (wikipedia.org)
However, the mechanisms underlying these differential changes in 5-HT1A receptor expression remain unclear. (biomedcentral.com)

Phenylephrine and methoxamine are examples of drugs that selectively activate α 1 -adrenergic receptors (adrenomimetic). (pharmacology2000.com)

Pertussis toxin B-pentamer mediates intercellular transfer of membrane proteins and lipids. (uc.edu)
Mechanosensitive membrane proteins: Usual and unusual suspects in mediating mechanotransduction. (stanford.edu)
This Viewpoint, which accompanies a Special Issue focusing on membrane mechanosensors, discusses unifying and unique features of both established and emerging mechanosensitive (MS) membrane proteins, their distribution across protein families and phyla, and current and future challenges in the study of these important proteins and their partners. (stanford.edu)
MS membrane proteins are essential for tissue development, cellular motion, osmotic homeostasis, and sensing external and self-generated mechanical cues like those responsible for touch and proprioception. (stanford.edu)
As the field continues to grow, so too will the list of proteins suspected to function as mechanosensors and the diversity of known MS membrane proteins. (stanford.edu)

Liver monocyte chemoattractant protein 1 (a proinflammatory protein associated with metabolic syndrome) gene expression was also significantly elevated in peri-SCN area dopaminergic lesioned rats. (biomedcentral.com)
[1] [2] Substance P and its closely related neurokinin A (NKA) are produced from a polyprotein precursor after differential splicing of the preprotachykinin A gene . (wikidoc.org)
To test the hypothesis that a specific cell line can respond to distinct Wnts with different patterns of gene expression, we over-expressed Wnt-5a and Rfz-2 in C57mg mammary epithelial cells and compared this cell line to C57mg cells over-expressing Wnt-1. (biomedcentral.com)
Beta-catenin then accumulates in the nucleus where it interacts with its transcriptional co-activators, members of the Lymphoid Enhancer Factor/T Cell Factor (LEF/TCF) family of high mobility group DNA binding proteins to regulate gene expression [ 1 ]. (biomedcentral.com)
Studies that use loss-of-function strategies (e.g., targeted gene deletion, receptor blockade, enzyme inhibitors, etc.) are perhaps most useful in this regard, but the interpretation of such data is often confounded by associated changes of food intake and body weight, by off-target effects ( 11 ), or by compensatory adaptations triggered by the experimental intervention. (silverchair.com)

Experimental characterisation confirmed that replacement of glutamic acid with glutamine in S1P 1 changed ligand specificity from S1P to LPA, and the reciprocal mutation in LPA 1 resulted in recognition of both LPA and S1P [ 7 ]. (biomedcentral.com)

The α1 couples to Gq, which results in increased intracellular Ca2+ and subsequent smooth muscle contraction. (wikipedia.org)
The β receptor couples to Gs and increases intracellular cAMP activity, resulting in e.g. heart muscle contraction, smooth muscle relaxation and glycogenolysis. (wikipedia.org)

These lipids elicit diverse responses from a wide range of cell types, including enhanced cell survival, cell proliferation, induction of cytoskeletal changes and chemotaxis (reviewed in [ 1 - 4 ]. (biomedcentral.com)

Phosphorylation sets off recruitment of arrestins, which associate using the phosphorylated receptor. (biotechpatents.org)

replacement of the naturally occurring glutamic acid with glutamine (present at this position in the LPA receptors) has previously been shown to be sufficient to change the specificity of S1P 1 from S1P to 18:1 LPA. (biomedcentral.com)

This review examines the evidence that alterations in transcriptional regulation of the 5-HT1A receptor could underlie its dys-regulation in mental illness. (biomedcentral.com)

Although metabotropic glutamate receptor (mGluR) modulation has been studied extensively in neurons, it has not been investigated in astrocytes. (jneurosci.org)

The role of the β-adrenergic receptor-inhibitory mechanism in the regulating the contracitile activity of the human uterus. (cardiologymedjournal.com)
Binding of SP to NK-1 results in internalization by the clathrin -dependent mechanism to the acidified endosomes where the complex disassociates. (wikidoc.org)

1] Patients may present with a history of relapsing urinary tract infections (UTIs), which may be episodic or persistent. (medscape.com)

Reversible blockade suggests that the inhibitor dissociates from the receptor relatively easily. (pharmacology2000.com)

While conventional drugs such as the α1-adrenergic receptor antagonists and 5α-reductase inhibitors have been found to be useful in the treatment of BPH, the adverse side effects associated with their usage, have led to increased search for alternative means of managing this disease. (frontiersin.org)
Nonsteroidal anti-inflammatory drugs (NSAIDs) and alpha blockers help with symptom relief. (medscape.com)

this is flanked by a series of upstream repressor elements for REST, Freud-1/CC2D1A and Freud-2/CC2D1B factors that not only restrict its expression to neurons, but may also regulate the level of expression of 5-HT1A receptors in various subsets of neurons, including serotonergic neurons. (biomedcentral.com)

Dobutamine is an example of a drug that selectively stimulates the heart via β 1 receptors, although dobutamine also has activity at α adrenergic receptors as well. (pharmacology2000.com)
Taken together, these results highlight an integrated regulation of 5-HT1A autoreceptors that differs in several aspects from regulation of post-synaptic 5-HT1A receptors, and could be selectively targeted to enhance serotonergic neurotransmission. (biomedcentral.com)

The purinergic P2X 7 receptor: regulation of uterine function in labour and preterm labour. (nottingham.ac.uk)

Clonidine activates another type of adrenergic receptor, designated α 2 . (pharmacology2000.com)

Desk 2 G Protein-Coupled Receptors for Protein and Peptides molecular modeling. (biotechpatents.org)

Many cells have these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system (SNS). (wikipedia.org)
In it, he explicitly named the different responses as due to what he called α receptors and β receptors, and that the only sympathetic transmitter was adrenaline. (wikipedia.org)
Here we address the question as to whether the low frequency variability (approximately 0.1 Hz) of the heart period may depend on a baroreflex-mediated response to blood pressure oscillations, induced by the alpha-sympathetic drive on the peripheral resistance. (researchgate.net)
We inhibited the vascular response to the sympathetic vasomotor activity with a peripheral alpha-blocker (urapidil) and maintained mean blood pressure at control levels with angiotensin II. (researchgate.net)
The prostate is innervated by sympathetic nerves from T-10 to L-1. (medscape.com)

Approximately half of the members of the human GPCR superfamily are chemosensory receptors, including odorant receptors (ORs), trace amine-associated receptors (TAARs), bitter taste receptors (TAS2Rs), sweet and umami taste receptors (TAS1Rs). (mdpi.com)

Unfortunately, modern Western diet and lifestyle habits (consisting of excessive caloric intake typically coupled with insufficient physical activity) can cause an excessive accumulation of both subcutaneous and visceral white adipose tissue (WAT) that can have numerous adverse effects on health and health markers. (mrsupps.com)

Substance P and the NK1 receptor are widely distributed in the brain and are found in brain regions that are specific to regulating emotion ( hypothalamus , amygdala , and the periaqueductal gray ). (wikidoc.org)
The serotonin-1A (5-HT1A) receptor is among the most abundant and widely distributed 5-HT receptors in the brain, but is also expressed on serotonin neurons as an autoreceptor where it plays a critical role in regulating the activity of the entire serotonin system. (biomedcentral.com)

that is, of the 182 amino acids defining the TM domains of the human α 2A -adrenergic receptors, about 40% are identical with the human β 2 -adrenergic receptors. (pharmacology2000.com)
Human cytomegalovirus G protein-coupled receptor US28 promotes latency by attenuating c-fos. (uc.edu)
Antioxidant enzyme expression, lipid peroxidation, and protein oxidation in human myometrium with parturition Reproductive Sciences. (nottingham.ac.uk)
High resolution crystal structure of human β 2 -adrenergic G protein-coupled receptor. (guidetoimmunopharmacology.org)
High levels of dopamine (DA) were described in human ovary and recently evidence for DA receptors in granulosa and luteal cells has been provided, as well. (biomedcentral.com)
Human granulosa cells (GCs) derived from women undergoing in vitro fertilization (IVF) are an adequate model for endocrine cells of the follicle and the corpus luteum and were therefore employed in an attempt to decipher their DA receptor repertoire and functionality. (biomedcentral.com)
Among the DA receptors found in human GCs, D 2 expression was marked both at mRNA and protein levels and it was therefore further studied. (biomedcentral.com)
A previous study showed D 2 in human GCs, which are linked to cAMP, and the present study reveals the full spectrum of DA receptors present in these endocrine cells, which also includes D 2 -like receptors, linked to calcium. (biomedcentral.com)

Its receptor - the neurokinin type 1 - is distributed over cytoplasmic membranes of many cell types (neurons, glia, endothelia of capillaries and lymphatics, fibroblasts, stem cells, white blood cells) in many tissues and organs. (wikidoc.org)
Elevated 5-HT1A autoreceptor expression would tend to reduce the activity of 5-HT neurons, while reduced post-synaptic 5-HT1A receptors would result in a blunted behavioral response to 5-HT. (biomedcentral.com)

Approximately 1 in 30 Ashkenazi Jews is presumed to be a carrier, which results in a potential disease incidence of 1 in 3600 live births to this population. (medscape.com)
and neurocardiac syndromes, such as Friedreich disease [ 1 ]. (springeropen.com)
One in 30 Ashkenazi Jews is presumed to be a carrier, which results in a potential disease incidence of 1 in 3600 live births to this population. (medscape.com)

Supporting differences in Wnt signaling, gain of function of Wnt-1 in C57mg mouse mammary epithelial cells leads to their morphological transformation while loss of function of Wnt-5a leads to the same transformation. (biomedcentral.com)

Since all reactions are, by definition, reversible, those reactions in which the inhibitor and receptor complex is so stable that dissociation is unlikely are described as 'irreversible. (pharmacology2000.com)

We therefore decided to investigate whether replacement of this residue (E 3.29(122) ) with glutamine conferred LPA-responsiveness to the S1P 4 receptor and hence determine the role of this residue in this lower-affinity S1P receptor. (biomedcentral.com)

Anatomy8

Organisms9

Diseases1

Chemicals and Drugs202

Analytical, Diagnostic and Therapeutic Techniques and Equipment13

Psychiatry and Psychology2

Phenomena and Processes19

Disciplines and Occupations2

Information Science3

Health Care1

Agonists3

Agonist5

Subtypes3

GPCRs3

Kinase6

Beta-adrenergic1

Selective4

Pharmacology2

Ligands7

Pharmacological1

Prefrontal Cortex of Rats1

Extracellular6

Genes4

Selectivity5

Inhibition2

Transmembrane1

Pathways6

Amino acid5

Subunit2

Interaction1

Activation4

Modulators1

Propranolol1

Neurotransmitters1

Functional1

Pathway1

Conformation2

Ionotropic1

Outflow1

Mechanisms2

Activate1

Membrane proteins5

Gene5

Characterisation1

Intracellular2

Lipids1

Phosphorylation1

Specificity1

Transcriptional1

Glutamate1

Mechanism2

Tract1

Blockade1

Drugs2

Regulate1

Selectively2

Regulation1

Activates1

Molecular1

Sympathetic5

GPCR1

Tissue1

Widely distributed2

Human8

Neurons2

Disease3

Epithelial1

Inhibitor1

Affinity1