Receptors adrenergic alpha. Medical search. Frequent questions

Although clonidine is considered an agonist in some tissues, we found that this compound was a mixed agonist-antagonist for alpha -adrenergic responses in platelets. (aspetjournals.org)
These studies demonstrate that [ 3 H]clonidine, a mixed agonist-antagonist, can be used to identify high-affinity alpha 2 -adrenergic receptors on human platelets. (aspetjournals.org)
Because [ 3 H]clonidine sites are regulated by Mg 2+ and GTP, these alpha 2 -adrenergic receptors are likely to be the sites mediating alpha -adrenergic agonist responses in platelets. (aspetjournals.org)
In contrast, an agonist and antagonist for alpha(2)-receptors acted only on capacitated spermatozoa. (kcl.ac.uk)
Emerphed ( ephedrine sulfate) is an alpha- and beta- adrenergic agonist and a norepinephrine-releasing agent used to treat clinically important low blood pressure ( hypotension ) occurring in the setting of anesthesia . (rxlist.com)
Adrenaclick contains epinephrine, a non-selective alpha and beta-adrenergic receptor agonist, indicated in the emergency treatment of allergic reactions (Type I) including anaphylaxis. (drugs.com)
EpiPen and EpiPen Jr are non-selective alpha and beta-adrenergic receptor agonist indicated in the emergency treatment of allergic reactions (Type I) including anaphylaxis. (nih.gov)
Studies of alpha1-adrenergic receptor subtype expression and receptor density by saturation binding with 125I-HEAT showed that GSNO decreased alpha1-adrenergic receptor density but did not alter affinity for antagonist or agonist. (duke.edu)
cAMP stimulates transcription of the beta 2-adrenergic receptor gene in response to short-term agonist exposure. (duke.edu)

Postural hypotension is particularly common after the initial dose of the alpha-1 adrenergic antagonist. (nih.gov)
A radioactively labeled alpha-adrenergic antagonist, [3H]dihydroergocryptine, binds specifically to a site on rabbit uterine membranes. (duke.edu)
alpha-Adrenergic antagonists, such as phentolamine and phenoxybenzamine, potently compete for the binding sites while the beta-adrenergic antagonist propranolol does not. (duke.edu)
Seven hours later, subjects were intrathecally infused with vehicle, 15, 30, 60, or 120 micrograms of prazosin (an alpha 1-adrenergic antagonist). (nih.gov)
The positive inotropic effect and the hydrolysis of phosphoinositide induced by endothelin-3 in rabbit ventricular myocardium: inhibition by a selective antagonist of ET(A) receptors, FR139317. (aspetjournals.org)
LY353433, a potent, orally effective, long-acting 5-HT(4) receptor antagonist: comparison to cisapride and RS23597-190. (aspetjournals.org)

There is no longer a subtype α1C receptor. (wikipedia.org)
At one time, there was a subtype known as α1C, but it was found to be identical to the previously discovered α1A receptor subtype. (wikipedia.org)
The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. (aspetjournals.org)
To determine which alpha 1-adrenergic receptor subtype mediates the contractile response of the human prostate, we first studied the pharmacological properties of three cloned human alpha 1 subtypes (alpha 1a/d, alpha 1b, and alpha 1c). (aspetjournals.org)
SK&F104856 was found to be 6-fold more potent at the alpha 1a/d receptor subtype than at alpha 1b- or alpha 1c-adrenergic receptors. (aspetjournals.org)
The potencies of indoramin, 5-methylurapidil, and SK&F104856 to inhibit the contractile response and to displace [3H]prazosin from the cloned human alpha 1c subtype were similar. (aspetjournals.org)
Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype. (duke.edu)
An alpha 2-adrenergic receptor subtype has been cloned from a human kidney cDNA library using the gene for the human platelet alpha 2-adrenergic receptor as a probe. (duke.edu)

Dibenzyline-induced alpha -adrenergic blockade leaves beta -adrenergic receptors unopposed. (nih.gov)
Their use in therapy of hypertension is based on the inhibition of vascular resistance in arterioles from alpha-adrenergic blockade, which results in an increase in venous capacitance and lowering of blood pressure. (nih.gov)
Blockade of only spinal alpha 1 adrenoceptors is insufficient to attenuate DDT-induced alterations in motor function. (nih.gov)
To evaluate changes in venous alpha 1-adrenoceptor responsiveness during chronic alpha 1-adrenoceptor blockade, dose-response curves to phenylephrine and angiotensin II were constructed in 10 healthy subjects before, during, and after administration of terazosin 1 mg orally for 28 d. (jci.org)

To avoid confusion, the naming convention was continued with the letter D. There are 3 alpha-1 adrenergic receptor subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins. (wikipedia.org)
Molecular cloning studies have revealed the existence of three subtypes of alpha 1-adrenergic receptors. (aspetjournals.org)
In an effort to bridge the gap between molecular biology and pathophysiology, we have chosen a model smooth muscle system, the human prostate, and investigated the role of alpha 1 subtypes in this tissue. (aspetjournals.org)
Indoramin and (+)-niguldipine were selective for the alpha 1c-adrenergic receptor, with at least 10-fold lower affinity at either alpha 1a/d or alpha 1b subtypes. (aspetjournals.org)
METHODS: Antibodies specific for different receptor subtypes were used for Western blotting of mouse and human sperm lysates and for immunocytochemical evaluation of whole mouse and human spermatozoa. (kcl.ac.uk)
A dosage regimen of lysergic acid diethylamide (LSD) that reliably produces behavioral tolerance in rats was evaluated for effects on neurotransmitter receptor binding in rat brain using a variety of radioligands selective for amine receptor subtypes. (erowid.org)

Binding is rapid, reaching equilibrium in less than 17 minutes at 25 degrees C. Adrenergic agonists compete for this binding site with an order of affinities identical to the pharmacological potency order of these agents as alpha-adrenergic agonists (epinephrine greater than norepinephrine greater than isoprotereonl). (duke.edu)
The only known mechanism of neural inhibition of inflammation in the spleen relies on the production of norepinephrine by splenic catecholaminergic fibers which binds to β2-adrenergic receptors (β 2-ARs) of CD4 + T cells. (nih.gov)

Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. (cusabio.com)

It is concluded that activation of alpha2A-adrenergic signal in chondrocytes promotes temporomandibular joint degenerative remodelling by chondrocyte-mediated pro-catabolic activities. (cusabio.com)
Study showed that alpha2A adrenergic receptors are highly expressed in the cell bodies and axons of mesoprefrontal dopaminergic neurons provides a morphological basis to the vast functional evidence that somatodendritic and nerve-terminal alpha2A adrenergic receptors control dopaminergic activity and dopamine release in the prefrontal cortex. (cusabio.com)

The majority of alpha-1 receptors are directed toward the function of epinephrine, a hormone that has to do with the fight-or-flight response. (wikipedia.org)
Dibenzyline (phenoxybenzamine hydrochloride) may interact with compounds that stimulate both alpha- and beta- adrenergic receptors (i.e., epinephrine) to produce an exaggerated hypotensive response and tachycardia. (nih.gov)
Pharmacological studies of human platelets indicate that epinephrine initiates platelet aggregation and secretion by interacting with alpha -adrenergic receptors on the platelet surface. (aspetjournals.org)
Beta-adrenergic blocking drugs: antagonize cardiostimulating and bronchodilating effects of epinephrine. (drugs.com)
Alpha-adrenergic blocking drugs: antagonize vasoconstricting and hypertensive effects of epinephrine. (drugs.com)

We also identify a role for sympathetic nervous system regulation of the inhibitory adrenergic receptor (ADRA2A) in regulating leptin production. (elifesciences.org)

By binding to specific receptor-sites these agents appear to potentiate the effects of gamma-aminobutyric acid (GABA) and facilitate inhibitory GABA neurotransmission and other inhibitory transmitters. (medscape.com)
These agents stimulate alpha-adrenoreceptors in brain stem, activating an inhibitory neuron, which in turn results in reduced sympathetic outflow. (medscape.com)

These agents are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells where they inhibit acid secretion. (medscape.com)
The alpha-1 adrenergic receptor antagonists (also called alpha-blockers) are a family of agents that bind to and inhibit type 1 alpha-adrenergic receptors and thus inhibit smooth muscle contraction. (nih.gov)
indeed at least one study has shown an increase in heart failure, stroke and cardiovascular disease with long term therapy with alpha-blockers. (nih.gov)
Recently, selective alpha-1a adrenergic receptors blockers have been developed for use in benign prostatic hypertrophy that are claimed to have less effect on blood pressure. (nih.gov)
Atropine and blockers of nicotinic or alpha- or beta-adrenergic receptors had no effect. (erowid.org)
Adrenergic blockers include alpha-blockers, beta-blockers, alpha-beta blockers, and peripherally acting adrenergic blockers. (msdmanuals.com)

Because catecholamines, like 5-HT, constrict lung vessels via a GPCR coupled to G(q), we hypothesized that S-nitrosothiols modify the alpha1-adrenergic GPCR system to inhibit pulmonary vasoconstriction by receptor agonists, e.g., phenylephrine (PE). (duke.edu)

Behavioral and biochemical characterization of benzodiazepine receptor partial agonists in pigeons. (aspetjournals.org)

CONCLUSION: These experiments provide the first good evidence that mammalian spermatozoa have both beta-adrenergic receptors, known to stimulate cAMP production by membrane-associated adenylyl cyclases (mACs), and alpha(2)-adrenergic receptors, known to inhibit cAMP production by mACs. (kcl.ac.uk)

Alpha -adrenergic agonists and antagonists competed for [ 3 H]clonidine binding sites with a rank order of potency typical for interaction at an alpha 2 -adrenergic receptor. (aspetjournals.org)
Uncapacitated and capacitated mouse spermatozoa were incubated with specific agonists and antagonists for alpha(2)-, beta(1)-, beta(2)- and beta(3)-adrenergic receptors for similar to 35 min and then assessed using chlortetracycline (CTC) fluorescence. (kcl.ac.uk)

Thus, we sought to examine the interaction of the alpha 2 -selective compound, clonidine, with human platelets in both pharmacological and radioligand binding studies. (aspetjournals.org)
Data show that the central alpha2 receptor agonists clonidine and dexmedetomidine are effective to attenuate local and systemic injury in experimental severe necrotizing pancreatitis (SNP) and should be evaluated in the clinical setting. (cusabio.com)

Thyroid gene expression analyses using Affymetrix U34A GeneChips, a regularized t -test, and Gene Map Annotator and Pathway Profiler demonstrated significant changes in rhodopsin-like G-protein-coupled receptor transcripts from all chemicals tested. (nih.gov)
We have reported that S-nitrosoglutathione (GSNO) inhibits 5-hydroxytryptamine (5-HT)-mediated pulmonary vasoconstriction via a cGMP-independent mechanism likely involving S-nitrosylation of its G protein-coupled receptor (GPCR) system. (duke.edu)
In CSNO-treated lung protein, the alpha1-adrenergic receptor was shown to undergo S-nitrosylation in vitro using a biotin switch assay. (duke.edu)
cDNA for the human beta 2-adrenergic receptor: a protein with multiple membrane-spanning domains and encoded by a gene whose chromosomal location is shared with that of the receptor for platelet-derived growth factor. (duke.edu)

The Na+/H+ exchanger regulatory factor (NHERF) binds to the tail of the beta2-adrenergic receptor and plays a role in adrenergic regulation of Na+/H+ exchange. (duke.edu)

Moreover, direct binding experiments using nonselective antagonists, such as [ 3 H]dihydroergocryptine, indicate a single class of platelet alpha -adrenergic receptors. (aspetjournals.org)

Compounds that stimulate both types of receptors may, therefore, produce an exaggerated hypotensive response and tachycardia. (nih.gov)
This class of drugs stimulate a specific set of receptors (clinically referred as alpha-adrenergic genre of receptors). (internationaldrugmart.com)

Dopamine-elicited outward current in subcoeruleus nucleus neurons are mediated by adrenergic alpha2 receptors. (cusabio.com)
A prevalent model predicts that leptin's actions are mediated through pro-opiomelanocortin (POMC) neurons that express leptin receptors (LEPRs). (elifesciences.org)

The alpha-1A adrenergic receptor (α1A adrenoreceptor), also known as ADRA1A, formerly known also as the alpha-1C adrenergic receptor, is an alpha-1 adrenergic receptor, and also denotes the human gene encoding it. (wikipedia.org)

This initiative is intended to facilitate the development of: 1) PET and SPECT probes for molecular targets (e.g., receptors, intracellular messengers, disease-related proteins) that are of broad interest to the neuroscience research community, and 2) new technologies for radiotracer development. (nih.gov)
The NIH institutes listed in this FOA are specifically interested in the development of radioligands for molecular targets (e.g., receptors, cell adhesion molecules, intracellular messengers, and disease related proteins) that are of broad interest to the scientific community. (nih.gov)

These CD4 + T cells trigger the release of acetylcholine that inhibits the secretion of inflammatory cytokines by macrophages through α7 nicotinic acetylcholine receptor (α7nAchRs) signaling. (nih.gov)

Propranolol is a nonselective beta-adrenergic receptor blocking agent. (medscape.com)
Because the nonselective alpha-1 adrenergic antagonists cause a relaxation of smooth muscle both in arterioles (alpha-1b receptors) and in the bladder neck and prostate (alpha-1a receptors), they are also useful in the therapy of symptoms of urinary obstruction due to benign prostatic hypertrophy. (nih.gov)

Nanoparticle inhalation modulates arteriolar sympathetic constriction: role of nitric oxide, prostanoids, and alpha-adrenergic receptors. (cdc.gov)

This observation and the recent finding that alpha 2-adrenergic agonists potentiate N6,2'-O-dibutyryl-cAMP or isobutylmethylxanthine stimulation of arylalkylamine N-acetyltransferase in the rat pineal gland establish that alpha 2D-like adrenergic receptors are located on pinealocytes. (nih.gov)

In addition to conveying cellular responses to an effector molecule, receptors are often themselves regulated by their effectors. (duke.edu)

The findings of the present study suggest that selective alpha 1c-adrenergic receptor antagonists may be clinically more efficacious and better tolerated agents for the treatment of symptomatic benign prostatic hyperplasia. (aspetjournals.org)

Scholars@Duke publication: Alpha-adrenergic receptor identification by (3H)dihydroergocryptine binding. (duke.edu)
Scholars@Duke publication: S-nitrosoglutathione inhibits alpha1-adrenergic receptor-mediated vasoconstriction and ligand binding in pulmonary artery. (duke.edu)

We recently observed interaction between alpha-2 adrenergic receptors and those for NPY at the presynaptic level. (unicatt.it)

Co-director of proposal to evaluate PET imaging of the peripheral benzodiazepine receptor as a cellular marker of inflammation in Alzheimer's disease and atherosclerosis. (nih.gov)

A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance regulator determines binding to the Na+/H+ exchanger regulatory factor family of PDZ proteins. (duke.edu)
However, uropod-localized receptors and ezrin/radixin/moesin proteins still cluster in nocodazole-treated cells, indicating that MTs are required specifically for uropod stability. (exeter.ac.uk)

Nitrergic and alpha2-adrenergic modulation of gastric sensory and motor function were assessed in this study. (nih.gov)

At present, however, the alpha-1 adrenergic antagonists are recommended only as adjunctive therapy of hypertension and not as monotherapy. (nih.gov)

This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy. (jci.org)

This gene encodes the alpha-1A-adrenergic receptor. (wikipedia.org)

Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. (jci.org)

Structural analogs of catecholamines that are devoid of alpha-adrenergic physiological activity do not compete for [3H]dihydroergocryptine binding sites. (duke.edu)

These data suggest that alpha-adrenergic receptors can be directly identified and studied by [3H]dihydroergocryptine binding. (duke.edu)

Summary of the ASPET-sponsored Colloquium: Alpha-2 adrenergic receptors: structure, function, and therapeutic implications, October 25-27, 1995. (aspetjournals.org)

We have isolated and sequenced a cDNA encoding the human beta 2-adrenergic receptor. (duke.edu)

Description: A sandwich ELISA kit for detection of Adrenergic Receptor Alpha 2C from Rat in samples from blood, serum, plasma, cell culture fluid and other biological fluids. (tuberculosisdrugresearch.org)
Description: A sandwich quantitative ELISA assay kit for detection of Human Adrenergic Receptor Alpha 2C (ADRa2C) in samples from tissue homogenates or other biological fluids. (tuberculosisdrugresearch.org)
Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Adrenergic Receptor Alpha 2C (ADRa2C) in Tissue homogenates and other biological fluids. (tuberculosisdrugresearch.org)

Rat pineal alpha 2-adrenergic receptors were unaltered after nerve endings degenerated. (nih.gov)
5-HT Acts on smooth muscle receptors which are blocked by LSD, bromolysergic acid or methysergide and on enteric nerve receptors which are blocked by biguanides-and quaternary derivatives of 5-HT but not by morphine. (erowid.org)

Chronic administration of alpha 1-receptor antagonists is associated with loss of clinical efficacy, especially in congestive heart failure, although the mechanism is uncertain. (jci.org)

Anatomy1

Organisms1

Diseases2

Chemicals and Drugs18

Anthropology, Education, Sociology and Social Phenomena1

Information Science2

Health Care1

Agonist9

Antagonist6

Subtype8

Blockade4

Subtypes6

Norepinephrine2

Adenylate Cyclase1

Alpha2A adrenergic2

Epinephrine5

Adra2a1

Inhibitory2

Blockers6

Phenylephrine1

Characterization1

Inhibit1

Agonists and antagonists2

Clonidine2

Protein4

Regulation1

Platelet1

Stimulate2

Neurons2

Adrenoreceptor1

Intracellular messengers2

Nicotinic1

Nonselective2

Nitric Oxide1

Potentiate1

Responses1

Clinically1

Scholars@Duke2

Presynaptic1

Peripheral1

Proteins2

Gastric1

Hypertension1

Adrenoceptor1

Gene1

Humans1

Catecholamines1

Dihydroergocryptine1

Therapeutic1

CDNA1

Biological3

Nerve2

Mechanism1