Antagonist neuropeptides. Medical search. Frequent questions

An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one or both of the orexin receptors, OX1 and OX2. (wikipedia.org)
Orexin receptor antagonists are not currently used as first-line treatments for insomnia due to cost and concerns about possible misuse liability. (wikipedia.org)
Rates of somnolence or fatigue with orexin receptor antagonists in clinical trials were 7% (vs. 3% with placebo) for suvorexant 15 to 20 mg, 7 to 10% (vs. 1.3% for placebo) for lemborexant 5 to 10 mg, and 5 to 6% (vs. 4% with placebo) for daridorexant 25 to 50 mg. (wikipedia.org)
The elimination half-lives of clinically used orexin receptor antagonists are 12 hours for suvorexant, about 17 to 19 hours ("effective" half-life) or 55 hours (terminal elimination half-life) for lemborexant, and 6 to 10 hours for daridorexant. (wikipedia.org)
The elimination half-lives of investigational orexin receptor antagonists are 2 to 3 hours for seltorexant and about 1.5 to 3 hours for vornorexant. (wikipedia.org)
Lemborexant, an orexin receptor antagonist sedative-hypnotic: Is it useful for insomnia in psychiatric disorders? (wikipedia.org)
BIIE0246, a newly synthesized non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, could contend with high affinity (8 to 15?nM) for particular [125I]PYY3C36 binding sites in HEK293 cells transfected using the rat Con2 receptor cDNA, and in rat human brain and individual frontal cortex membrane homogenates. (phytid.org)
Used together, these outcomes show that BIIE0246 is certainly an extremely potent, high affinity antagonist selective for the Y2 receptor subtype. (phytid.org)
Our data obviously show that BIIE0246 may be the 1st powerful and extremely selective Y2 receptor antagonist to become developed. (phytid.org)
On the other hand, BIIE0246 acted like a powerful antagonist in the rat vas deferens and doggie saphenous vein, two prototypical Y2 bioassays (Pheng bioassays, we've also proven that BIIE0246 can stop the activation from the Y2 receptor 22338-71-2 supplier subtype without impacting the actions of NPY or its homologues in the Y1 and Y4 receptors. (phytid.org)
Neuropeptide S (NPS) regulates various biological functions by selectively activating the NPS receptor (NPSR). (unife.it)
This effect was blocked by coinjection of 1 μg (hr)IL-1β receptor antagonist or 0.1 ng of 3-((+)-2-carboxypiperazin-4-yl)-propyl-1-phosphonate, selective antagonists of IL-1β and NMDA receptors, respectively. (jneurosci.org)
Characterization of the brain penetrant neuropeptide Y Y 2 receptor antagonist SF-11. (rndsystems.com)
Neuropeptide Y (NPY) receptors belong to the G-protein-coupled receptor superfamily and have important roles in food intake, anxiety and cancer biology(1,2). (uni-regensburg.de)
Daridorexant is a dual orexin receptor antagonist for the treatment of insomnia. (springer.com)
The ibogaine-induced increases in NTLI in striatum, nucleus accumbens and substantia nigra were blocked by coadministration of the selective D1 receptor antagonist, SCH 23390. (erowid.org)
The D2 receptor antagonist, eticlopride, blocked the ibogaine-induced increase in nigral NTLI, but not in striatum and nucleus accumbens. (erowid.org)
Finally, a mixture of a V1 AVP and the α-helical corticotropin-releasing hormone (CRH) receptor antagonists administered via inverse microdialysis into the PVN caused a significant increase in the plasma adrenocorticotropic hormone (ACTH) concentration compared with vehicle-treated controls both under basal conditions and during social defeat, indicating inhibitory effects of intra-PVN-released AVP and/or CRH on HPA system activity. (jneurosci.org)
Eisai Co., Ltd. (Headquarters: Tokyo, CEO: Haruo Naito, "Eisai") announced today that its Hong Kong subsidiary Eisai (Hong Kong) Co., Ltd. has obtained approval for the in-house-discovered and developed orexin receptor antagonist DAYVIGO ® (generic name: lemborexant) for the treatment of adults with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance. (eisai.com)
DAYVIGO is a dual orexin receptor antagonist that inhibits orexin neurotransmission regulating sleep-wake rhythm by binding competitively to the two subtypes of orexin receptors (OX1R and OX2R). (eisai.com)
Delivery is accompanied by increases in anxiety levels that are significantly related to an activation of the inflammatory response system (IRS), as indicated by increases in the serum concentrations of interleukin-6 and the interleukin-1 receptor antagonist (IL-1RA) and increases in the activity of prolyl endopeptidase (PEP), a cytosolic endopeptidase that cleaves peptide bonds on the carboxyl side of proline in behaviorally active neuropeptides involved in anxiety. (psychiatrist.com)
Daridorexant is a dual orexin receptor antagonist that blocks the binding of the wake-promoting orexin neuropeptides, and is thought to turn down overactive wakefulness, as opposed to treatments that generally sedate the brain. (fhea.com)
The NMDA-induced phase delay was antagonized by an NMDA-receptor antagonist MK-801. (eurekamag.com)
In addition, both the advances and delays in phase caused by NMDA were potentiated by cotreatment with neuropeptide Y, whereas AMPA-induced phase delay was not potentiated by neuropeptide Y. This points to a functional link between NMDA and neuropeptide Y receptor-mediated mechanisms in the SCN. (eurekamag.com)
In addition to these serotoninergic medications, a new treatment that is a combination of fluoxetine with an NMDA receptor antagonist was also reported to be effective for canine refractory compulsive disorders. (vin.com)
Other agents include amylin, melanocortin-4 receptor agonists, neuropeptide Y antagonists, beta(3) adrenergic agonists and glucagon-like peptide-1 agonists. (drugbank.com)
The peptide is an antagonist of the muscular nicotinic acetylcholine membrane's receptor (mnAChR). (platinumskincare.com)
Methods: The expression of neuropeptides involved in homeostasis regulation will be assessed in vitro after treatment with the agonist and the antagonist of the ±7nAChR receptor and with leptin. (fapesp.br)
Some of the animals will undergo intracerebroventricular injection of ±7nAChR receptor agonist, antagonist and siRNA and will also be treated with leptin. (fapesp.br)
Our previous results have shown that ±7nAChR receptor modulates food intake by enhancing the expression of anorexigenic neuropeptides and suppressing the expression of orexigenic neuropeptides. (fapesp.br)

Neuropeptide W/B receptors are a family of G protein-coupled receptors (GPCRs) that bind the endogenous ligands neuropeptides B and W. The two receptors in the family are NPBW1 and NPBW2. (multispaninc.com)
DAYVIGO binds to orexin receptors OX1R and OX2R and acts as a competitive antagonist with stronger inhibition effect on OX2R, which suppresses both REM and non-REM sleep drive, such that DAYVIGO may provide faster sleep onset and better sleep maintenance to patients. (eisai.com)
DAYVIGO is Eisai's in-house discovered and developed small molecule that binds to orexin receptors, OX1R and OX2R, and acts as a competitive antagonist (IC 50 values of 6.1 nM and 2.6 nM, respectively). (eisai.com)
Blocking the binding of wake-promoting neuropeptides orexin to receptors OX1R and OX2R is thought to suppress wake drive (Ki values of 8.1 nM and 0.48 nM, respectively). (eisai.com)
Agouti-related Protein (AgRP), also known as the protein product of the Agouti-related Transcript (ART), is a neuropeptide and a functional antagonist of alpha-MSH on Melanocortin (MC)-3 and MC-4 receptors, both of which are implicated in obesity. (novusbio.com)
Neuropeptides bind to specific receptors on other neurons, altering their physiological properties and thereby influencing neural circuit function. (neurosciencenews.com)

Currently, there are no known human NPBW1 or NPBW2 agonists and antagonists. (multispaninc.com)

Neuropeptides substance P, calcitonin gene-related peptide and proteases trypsin stimulated GPCR endocytosis and evoked sustained signals and hyperexcitability in pain-sensing neurons. (dtic.mil)
The calcitonin gene-related peptide (CGRP) is a neuropeptide widely distributed throughout the human body. (bvsalud.org)

PACAP (6-38) is a potent antagonist of PACAP-38. (eurogentec.com)

Here we report crystal structures of the human Y1R bound to the two selective antagonists UR-MK299 and BMS-193885 at 2.7 and 3.0 angstrom resolution, respectively. (uni-regensburg.de)

Orexins (or hypocretins) are hypothalamic neuropeptides with a multitude of physiological functions. (researchgate.net)
Metabolic parameters will be measured by a indirect calorimetry and the expression of hypothalamic neuropeptides will be analyzed using Real-Time PCR. (fapesp.br)

A number of peptides and small-molecule compounds have been characterized as Y1R antagonists and have shown clinical potential in the treatment of obesity(4), tumour(1) and bone loss(5). (uni-regensburg.de)

In capsaicin-sensitive sensory neurons, CGRP co-localizes with substance P and other neuropeptides, in the motor endplate with acetylcholine. (bachem.com)
While primarily recognized as a nociceptive mediator, CGRP antagonists are currently utilized for migraine treatment. (bvsalud.org)
In summary, CGRP represents a neuropeptide with a complex systemic impact, extending well beyond nociception, thus offering new perspectives in medical research and therapeutics. (bvsalud.org)

Sensory neurons of nociceptive character, which encode chemical, thermal and mechanical stimuli and release neuropeptides, pervade the whole mammalian body. (nature.com)
Aim 2 determines whether endosomally-targeted antagonists inhibit channel activity, gene expression and hyperexcitability of neurons. (dtic.mil)
Tachykinin is a neuropeptide, a short protein molecule that is released from certain neurons when they are activated. (neurosciencenews.com)

Thus, the measurement of dynamic changes in the concentration of extracellular AVP in distinct brain areas under defined experimental conditions would provide a missing link for the physiological involvement of the endogenous neuropeptide in the regulation of autonomic, endocrine, and behavioral parameters. (jneurosci.org)

Substance P antagonists occupy a central role in this area of intensive scientific activity. (biopsychiatry.com)
They determined that when corneal nerves are severed during surgery, substance P (a neuropeptide) is secreted in both eyes, thus disabling the regulatory T cells that are required for graft survival. (aao.org)
However, the researchers were able to restore immune privilege and promote graft survival by administering a substance P antagonist. (aao.org)

The PP-fold family comprises neuropeptide Y (NPY), peptide YY (PYY), and pancreatic polypeptide (PP). They are composed of a chain of 36 amino acids residue and share amino acid homology, amidated C-terminal ends. (hindawi.com)

Therapies include dynamin and clathrin inhibitors lipid-conjugated antagonists that accumulate in endosomes antagonists encapsulated into nanoparticles that disassemble in acidic endosomes. (dtic.mil)

PACAP-27 is a neuropeptide originally isolated from bovine hypothalamus but is also found in humans and rats. (eurogentec.com)

Comparative Pharmacology of the 3 Marketed Dual Orexin Antagonists-Daridorexant, Lemborexant, and Suvorexant-Part 2. (wikipedia.org)

These antagonists effectively reversed nociception in preclinical models of visceral pain, migraine pain, and nerve injury pain. (dtic.mil)

Aim 3 evaluates the therapeutic potential of endosomally-targeted GPCR antagonists in trauma- and stress-induced pain relevant to military personnel. (dtic.mil)

Recently, the NPSR ligand [tBu-d-Gly5]NPS was generated and in vitro characterized as a pure antagonist at the mouse NPSR. (unife.it)
Collectively, the present results demonstrated that [tBu-d-Gly5]NPS behaves both in vitro and in vivo as a pure and potent NPSR antagonist. (unife.it)

The orexin neuropeptide signaling system plays a role in wakefulness. (eisai.com)

They were more effective than conventional antagonists of plasma membrane GPCRs. (dtic.mil)

The structures combined with mutagenesis studies reveal the binding modes of Y1R to several structurally diverse antagonists and the determinants of ligand selectivity. (uni-regensburg.de)

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)
Many neuropeptides are also hormones released by non-neuronal cells. (bvsalud.org)

So, being able to precisely and locally modify a neuropeptide like Tac2 is a promising approach to mental health treatments. (neurosciencenews.com)

It is well-established that the neuropeptide arginine vasopressin (Avp) is important to the neural modulation of mammalian behavior. (frontiersin.org)
In the cardiovascular system, it functions as a potent vasodilator, yet its antagonists do not induce arterial hypertension, suggesting concurrent modulation by other molecules. (bvsalud.org)

The rich data set generated by these experiments revealed how this neuropeptide acts globally across the brain to coordinate diverse behavioral responses to social isolation stress. (neurosciencenews.com)

7 More recently biological evidence including genetic association, brain structural abnormalities in Doberman pinschers 8,9 , and elevated neuropeptides in Bull terriers 10 suggests a link between canine compulsive disorder and human psychiatric disorders. (vin.com)

The antagonists failed to affect anxiety-related behavior of the animals as assessed with the elevated plus-maze. (jneurosci.org)

However, central effects of AVP have been revealed mainly by pharmacological approaches, which presuppose the intracerebral release of the neuropeptide. (jneurosci.org)
So far, however, little information is available about the intrahypothalamic release of these neuropeptides under physiological rather than pharmacological conditions. (jneurosci.org)

Anatomy21

Organisms14

Diseases3

Chemicals and Drugs177

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Psychiatry and Psychology4

Phenomena and Processes21

Disciplines and Occupations2

Information Science2

Health Care1

Receptor30

Receptors6

Agonists1

Calcitonin gene-re2

Potent antagonist1

Selective antagonists1

Hypothalamic neuropeptides2

Peptides1

CGRP3

Neurons3

Endogenous1

Substance3

PANCREATIC-POLYPEPTIDE1

Inhibitors1

Humans1

Lemborexant1

Nociception1

Therapeutic potential1

Vitro2

Wakefulness1

GPCRs1

Selectivity1

Cells2

Approach1

Modulation2

Behavioral1

Structural1

Animals1

Release2