Antagonists with inhibition. Medical search. Frequent questions

2002). It's been demonstrated the fact that vertebral opioid receptor antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) blocks 10 and100 Hz EA-produced anti-hyperalgesia within a comprehensive Freunds adjuvant (CFA)-induced inflammatory discomfort rat model, as the receptor antagonist nor-binaltorphimine (Nor-BNI) will not (Zhang et al. (gasyblog.com)
Such effect was completely reversed both by the opioid receptor antagonist naloxone and by the unselective muscarinic receptor antagonist atropine. (researchgate.net)
LDN is a competitive opioid receptor antagonist. (ldnresearchtrust.org)

N,N'-Alkane-diyl-bis-3-picoliniums as nicotinic receptor antagonists: inhibition of nicotine-evoked dopamine release and hyperactivity. (uams.edu)
It's been reported that intracerebroventricular shot of the receptor antagonist blocked 2 however, not 100 Hz electroacupuncture (EA)-produced analgesia within an uninjured pet model. (gasyblog.com)
On the supraspinal level, intracerebroventricular shot of CTOP, a receptor antagonist, obstructed 2 however, not 100 Hz EA-produced analgesia within an uninjured pet model (Huang et al. (gasyblog.com)
In this study, we have investigated whether treatment with a selective C5aR antagonist prevents Inhibition of inflammation and fibrosis by a complement C5a receptor antagonist in DOCA-salt hypertensive rats in deoxycorticosterone acetate (DOCA)-salt hypertensive rats. (edu.au)
Adenylate cyclase in guinea pig hippocampal and cortical homogenates was confirmed as an H2-receptor, and shown by measurement of pA2 values of H2-antagonists (imidazolylpropyl methylthiourea, NQ-guanylhistamine, imidazolylpropylguanidine, thiaburimamide, metiamide and cimetidine). (erowid.org)
Inactive as either antagonists or agonists on the H2-receptor were psilocin, bufotenine, mescaline, different classes of anticonvulsant drugs, barbiturates and narcotic agonists and antagonists, as well as lithium chloride, chlordiazepc, ice, THC and procaine. (erowid.org)
The development of newer, more-selective nonsteroidal mineralocorticoid receptor antagonists has yielded new opportunities for dual RAAS inhibition. (medpagetoday.com)
Now, however, the question of whether dual RAAS blockade is safe or effective is again at the fore, with the introduction of SGLT2 inhibitors, incretin-based agents such as GLP-1 RAs and dipeptidyl peptidase 4 (DPP-4) inhibitors, and nonsteroidal mineralocorticoid receptor antagonists (MRAs). (medpagetoday.com)
We investigated, whether GPVI-Fc added in vitro on top of acetylsalicylic acid (ASA), the P2Y 12 antagonist ticagrelor, and the fibrinogen receptor antagonist abciximab alone or in combination would increase inhibition of platelet activation by atherosclerotic plaque. (thieme-connect.com)
Also antagonist at the vascular 5-HT 2 receptor (K i = 11 nM). (rndsystems.com)
Small molecule antagonists of relaxin receptor" (NCI, 1U01CA177711, PI: AI Agoulnik). (fiu.edu)
Amiloride acted primarily as a competitive antagonist, reducing the sensitivity of the receptor to GABA without affecting the maximal current amplitude. (aspetjournals.org)
Inhibition of the IAPP receptor with the antagonist AC187 only reverted IAPP effects partially. (lu.se)
Potent, competitive AMPA / kainate receptor antagonist. (abcam.com)
Also antagonist at NMDA receptor glycine site. (abcam.com)
Both Ketanserin, (10 mg/kg, i.p.) a 5-HT2-receptor antagonist, and Cetirizin, a H1-blocker, (30 mg/kg, i.p.) administered 1 hr after TMA challenge inhibited the subsequent LAR. (cdc.gov)
Montelukast (10 mg/kg, i.p.), a leukotriene receptor antagonist, inhibited EAR, but not LAR, when administered either before or 1 hr after challenge. (cdc.gov)
Strippoli Giovanni FM, Bonifati Carmen, Craig Maria E, Navaneethan Sankar D, Craig Jonathan C. Angiotensin converting enzyme inhibitors and angiotensin II receptor antagonists for preventing the progression of diabetic kidney disease. (bvs.br)

Importantly, however, guidelines recommend against using ACEis and ARBs in combination with each other-a strategy known as dual RAAS inhibition or dual RAAS blockade-because combinations of RAAS inhibitors have not proven to be renal protective over the long term. (medpagetoday.com)
In contrast, the strong inhibition of platelet adhesion by GPVI-Fc in combination with GPIIb/IIIa inhibitors could be harmful. (thieme-connect.com)

Mimic dopamine action of inhibition of prolactin release. (medscape.com)

CPZ-induced calcium transients in human TRPA1-expressing HEK293t cells were blocked by the selective TRPA1 antagonists HC 030031 and A967079 and involved three cysteine residues in the N-terminal domain. (nature.com)
Selective pharmacological inhibition of mediators demonstrates different pathophysiological mechanisms of EAR and LAR for the asthma-like responses in the BNR TMA model. (cdc.gov)

Under static conditions, GPVI-Fc inhibited plaque-induced platelet aggregation by 53%, and increased platelet inhibition by ASA (51%) and ticagrelor (64%) to 66% and 80%, respectively. (thieme-connect.com)
Under arterial flow, GPVI-Fc inhibited plaque-induced platelet aggregation by 57%, and significantly increased platelet inhibition by ASA (28%) and ticagrelor (47%) to about 81% each. (thieme-connect.com)
Yet despite the consensus that platelet inhibition with aspirin and/or clopidogrel improves outcomes, recurrence remains common and there is a growing awareness that inappropriate dosing of antiplatelets contributes to poor outcomes. (sbir.gov)

Attenuation of experimental colitis by capsazepine (CPZ) has long been attributed to its antagonistic action on TRPV1 and associated inhibition of neurogenic inflammation. (nature.com)
Described herein are methods and compositions relating to inhibition of mechanically-induced TRPV4 activation, e.g., for the treatment of pulmonary edema, edema, inflammation, hypertension, and/or hyperalgesia. (google.com)

Our binding assays show indeed that nutlins, the newly discovered, potent antagonists of the Mdm2-p53 interaction, are not capable to efficiently disrupt the Mdmx-p53 interaction. (rcsb.org)

Studies in healthful human beings demonstrate that naloxone, a particular opiate antagonist, reverses acupuncture analgesia (Jiang et al. (gasyblog.com)

Effects of DA D 1 antagonists SCH23390 and SK&F83566 on locomotor activities in rats. (rndsystems.com)
The adenosine antagonist, aminophylline (30 mg/kg, i.p.) also inhibited LAR in some, but not all treated/challenged rats. (cdc.gov)

We conclude that GPVI-Fc added on top of single or dual antiplatelet therapy with ASA and/or a P2Y 12 antagonist is likely to improve anti-atherothrombotic protection without increasing bleeding risk. (thieme-connect.com)
This dual phosphorylation system is extremely sensitive to inhibition by antiplatelet agents and is well-suited for formatting to monitor antiplatelet therapy. (sbir.gov)

In summary, intraocular NO inhibits myopia dose-dependently and is obligatory for inhibition of myopia by atropine. (nih.gov)

The negative feedback promotes epileptic oscillations whereas the striatal feedforward inhibition suppresses the positive feedback provided by the cortico-striato-nigral pathway. (jneurosci.org)
We have shown that the inhibition of relaxin hormone signaling suppresses prostate cancer progression. (fiu.edu)

iGluR competitive antagonists 6-Cyano-7-nitroquinoxaline-2,3-dione (CNQX) or 6,7-dinitroquinoxaline-2,3-dione acted (DNQX) acts as a negative regulator of primary root and lateral root density. (intechopen.com)

Proximal cortical feedback inputs can relieve the tonic Mg block of NMDA receptors (NMDARs) at distal synapses and gate dendrodendritic inhibition onto mitral cells. (jneurosci.org)

Prepulse inhibition (PPI) is a neurological phenomenon in which a weaker prestimulus (prepulse) inhibits the reaction of an organism to a subsequent strong reflex-eliciting stimulus (pulse), often using the startle reflex. (wikipedia.org)
This gets rid of the tonic inhibition of GABA on serotonergic neurons in the RVM, and activation of the serotonergic neurons inhibits discomfort. (gasyblog.com)

SCH 23390 and SK&F 83566 are antagonists at vascular DA and serotonin receptors. (rndsystems.com)
It is a pure antagonist at various opioid receptors, Delta Kappa, Mu, and Opioid Growth Factor (OGF) receptors. (ldnresearchtrust.org)
LDN is an antagonist at the OGF receptors and there are OGF receptors on a wide range of cells in the body. (ldnresearchtrust.org)

In this study we show that TRPA1 agonism, rather than TRPV1 inhibition, in colonic sensory neurons is the key initial step in colitis protection by CPZ enemas. (nature.com)
Here we demonstrate that similar activity amplification occurs in mice, and that this is related to suppressed inhibition to PB neurons from the central nucleus of the amygdala (CeA) in animals of either sex. (iasp-pain.org)
We describe a novel pathway, consisting of inhibition by dynorphin, somatostatin and corticotropin-releasing hormone expressing neurons in the central nucleus of the amygdala that project to the parabrachial nucleus (PB). (iasp-pain.org)

We show that these maintained oscillations result from an interplay between the negative feedback through the cortico-subthalamo-nigral pathway and the striatal feedforward inhibition. (jneurosci.org)

These agents cause increased hypothalamic secretion of GnRH owing to blockage of estrogen inhibition. (medscape.com)

20%) adhesion inhibition at 1 mg/ml, dextrans increasingly substituted with carboxylic and benzylamide groups (CMBD) exhibited increasing anti-adhesive activities. (unige.ch)
Three CMBD derivatives showing an increasing proportion (5-14%) of benzylamide groups showed inhibition of bacterial adhesion increasing from 33 to 51% at 1 mg/ml. (unige.ch)
Another category of substituted dextrans having a variable proportion (2-26%) of sulfonated benzylamide groups (CMBDS) produced active inhibition of S. aureus adhesion. (unige.ch)
In comparison to these heparin-like dextran derivatives, native heparin produced inhibition values of S. aureus adhesion which were intermediate between those of CMBD and CMBDS compounds. (unige.ch)

These findings raise the possibility that the pattern of interneuronal activation, and thus lateral inhibition onto principal cells, is not regulated predominately by dendrodendritic synaptic inputs but instead may reflect the temporal coincidence of several types of synaptic inputs to granule cells. (jneurosci.org)
These results suggest that the proximal excitatory inputs to granule cells may play an important role in gating recurrent and lateral dendrodendritic inhibition (DDI) in the olfactory bulb. (jneurosci.org)

It demonstrates that abnormally strong striatal feedforward inhibition promotes synchronous oscillatory activity in the BG-thalamo-cortical network and relate this property to the observed strong suppression of the striatal output during seizures. (jneurosci.org)

Antagonistic effects of zinc and aluminum on lead inhibition of *-aminolevulinic acid dehydratase. (cdc.gov)

A new systematic review and meta-analysis assessed the impact of dual renin-angiotensin-aldosterone system inhibition on risk of acute kidney injury and hyperkalemia in patients diagnosed with diabetic kidney disease. (medpagetoday.com)
This means that inhibition of the RAAS, in susceptible individuals and settings in which RAAS activation is critical, is associated with an increased risk of acute kidney injury, hypotension, and hyperkalemia. (medpagetoday.com)

At one time, dual RAAS blockade was expected to provide more-complete inhibition of RAAS among patients with DKD. (medpagetoday.com)
It's possible that dual RAAS blockade with some combination of ACEi, ARB, MRA, or direct renin inhibitor can achieve more-complete inhibition of RAAS, and thereby confer greater CV and kidney protection versus any single agent. (medpagetoday.com)

We demonstrate that abnormally strong striatal feedforward inhibition can promote synchronous oscillatory activity that persists in the network over several tens of seconds as observed during seizures. (jneurosci.org)

These results indicate that a relationship exists between the pentasaccharide induced inhibition of experimental venous stasis thrombosis and the inhibition of thrombin generation. (nih.gov)

1994. Inhibition of Na+-glucose cotransport in kidney cortical cells by cadmium and copper: Protection by zinc. (cdc.gov)

Pentasaccharide added to human and rabbit plasmas in vitro from 0 to 5.0 micrograms/ml produced a concentration dependent effect up to a 35 to 50% inhibition of generated thrombin. (nih.gov)
Analysis of plasma obtained from animals in which a complete antithrombotic effect was observed in vivo demonstrated an approximate 45 to 55% inhibition of thrombin generation. (nih.gov)
1976. The in vitro effect of zinc on the inhibition of human *-aminolevulinic acid dehydratase by lead. (cdc.gov)
GTP and 5'-guanylyl imidophosphate, a poorly hydrolyzable GTP analog, decreased the affinity of the agonist 5-HT for the binding sites but had little effect on the affinity of the antagonist 2bromo-LSD. (erowid.org)
Lewis EJ, Hunsicker LG, Bain RP, Rohde RD. The effect of angiotensin-converting-enzyme inhibition on diabetic nephropathy. (bvs.br)

In the mouse xenograft model of colon cancer, we were able to observe a reduced tumor growth in response to CysLT1R antagonist treatment. (lu.se)

Inhibition generated by granule cells, the most common GABAergic cell type in the olfactory bulb, plays a critical role in shaping the output of the olfactory bulb. (jneurosci.org)

When prepulse inhibition is high, the corresponding one-time startle response is reduced. (wikipedia.org)
A second site (Drp1-Ser637) is phosphorylated in response to platelet antagonists. (sbir.gov)

Continuous growth on antagonist also leads to impairment of root meristem size, which suggests that iGluR-like channels may play a role in meristem maintenance. (intechopen.com)

Here we used an aptamer displacement screen to identify SecinH3, a small molecule antagonist of cytohesins. (nature.com)

Pulse-alone results are compared to prepulse-plus-pulse, and the percentage of the reduction in the startle reflex represents prepulse inhibition. (wikipedia.org)

3 Hl-antagonists (including cyproheptadine) blocked the H2 receptor (as shown by inhibition of dimaprit). (erowid.org)

The inhibition of the tumor growth was accompanied with changes in proliferation and apoptosis as determined by reduced Ki-67 expression, increased expression of p21WAF/Cip1, cleaved caspase 3 and caspase-cleaved keratin 18. (lu.se)

In ex vivo studies similar concentration dependent inhibition of thrombin generation was observed. (nih.gov)

Anatomy8

Organisms8

Diseases1

Chemicals and Drugs208

Analytical, Diagnostic and Therapeutic Techniques and Equipment10

Psychiatry and Psychology2

Phenomena and Processes17

Disciplines and Occupations1

Information Science2

Health Care1

Opioid receptor antagonist3

Receptor18

Inhibitors2

Dopamine1

Selective2

Platelet inhibition3

Inflammation2

Potent1

Opiate1

Rats2

Antiplatelet2

Atropine1

Suppresses2

CNQX1

NMDA1

Inhibits2

Receptors3

Neurons3

Pathway1

Estrogen1

Adhesion4

Lateral2

Demonstrates1

Antagonistic1

Acute2

Blockade2

Demonstrate1

Experimental1

Kidney1

Effect5

Treatment1

Cells1

Response2

Leads1

Small1

Results1

Shown1

Growth1

Studies1