AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and Processes
Neurokinin ANeurokinin BReceptors, Neurokinin-2Receptors, Neurokinin-1TachykininsReceptors, Neurokinin-3Substance PReceptors, TachykininNeurokinin-1 Receptor AntagonistsReceptors, NeurotransmitterKisspeptinsEledoisinIsoindolesPhysalaeminQuinuclidinesCapsaicinPyrrolidonecarboxylic AcidPiperidinesArcuate NucleusDynorphinsGuinea PigsNeuropeptidesCalcitonin Gene-Related PeptideMuscle, SmoothBronchoconstrictionPeptide FragmentsTracheaMuscle ContractionThiorphanBenzamidesAtropineIleumNeurogenic InflammationNeuronsNeprilysinDose-Response Relationship, DrugNeurons, AfferentGonadotropin-Releasing HormoneSpinal CordElectric StimulationBiphenyl CompoundsRats, Sprague-DawleyPeptides, CyclicRadioligand AssayBethanechol CompoundsPosterior Horn CellsKidney PelvisBethanecholRats, WistarProtein Precursors
ReceptorsReceptor ligandLigandOpioidPeptideSynapticTachykininSubstanceAngiotensinDownregulationNeuronsBiologicalSuggestsCellsHumanTypeActivityRoleFoundActivationAntagonistsNK1RExogenousSelectiveTachykinin receptorInternalizationHigh affinityNeuropeptideAprepitantInhibitionMechanismsMediateGeneProteinRelationshipChronicLevelsTreatment
Receptors7
  • Other neurokinin subtypes and neurokinin receptors that interact with SP have been reported as well. (wikipedia.org)
  • The responses to neurokinin A were also unaffected suggesting that neurokinin A did not mediate its effects via NK‐2 receptors. (mcmaster.ca)
  • These data suggest that neurokinin A, like substance P may be acting via NK‐1, rather than NK‐2 receptors, to produce excitation of wide dynamic range neurons in the dorsal horn of the cat spinal cord. (mcmaster.ca)
  • These data highlight the important integrative role played by parasympathetic ganglia and indicate that activation of NK 3 receptors in airway ganglia by endogenous neurokinins facilitates synaptic neurotransmission. (johnshopkins.edu)
  • Neurokinin 3 receptor (NK3R) is the most selective of the tachykinin receptors, with highly preferential binding and activation by its endogenous ligand NKB (TAC3). (immune-system-research.com)
  • Nevertheless, irrespective of the PAR identified, the challenge is the same: to pharmacologically mimic a peptide ligand which, unlike classical peptide receptors such as neurokinin (NK) or angiotensin type receptors which have soluble cognate ligands, remains tethered to the receptor and thus require a unique set of structural constraints to interact with the receptor optimally. (silverchair.com)
  • Other than this major mechanism of action, tramadol is known and fully studied due to its inhibitory activity against alpha2-adrenoreceptors, neurokinin 1 receptors, and muscarinic receptors as well as the inhibition of ion channels via nicotinic acetylcholine receptor and N-methyl-D-aspartate receptor. (itopmeds.com)
Receptor ligand1
  • The aim of the present study was to investigate the effects of the non‐peptide NK‐2 receptor antagonist, SR 48968 on the responses of dorsal horn neurons to iontophoretic application of the endogenous NK‐2 receptor ligand, neurokinin A, and on synaptically elicited responses in chloralose‐anaesthetized cats. (mcmaster.ca)
Ligand1
Opioid8
  • In this study, we have examined whether microinjection of the widely used NSAIDs, Clodifen, Ketorolac, and Xefocam, into the DH induces antinociceptive tolerance and whether this action is mediated via the endogenous opioid system. (healthcarecoremeasures.com)
  • These findings strongly support the suggestion of endogenous opioid involvement in NSAIDs antinociception and tolerance in the descending pain-control system [20C24]. (healthcarecoremeasures.com)
  • Our work in the first area is focused on the role of endogenous opioid peptides (EOP). (wvu.edu)
  • Our recent work in this area has been focused on the role of endogenous opioid peptides (EOP) in mediating the negative feedback action of progesterone. (wvu.edu)
  • 2022). Cryo-EM structure of human κ-opioid receptor-Gi complex bound to an endogenous agonist dynorphin A. PROTEIN & CELL,pwac033. (shanghaitech.edu.cn)
  • These findings provide novel insights into how peptidases control synaptic activity within the amygdala and presents restoration of endogenous peptide activity during withdrawal as a viable option to mitigate withdrawal-induced disruptions in emotional learning circuits and rescue the relapse behaviors exhibited during opioid withdrawal and beyond into abstinence. (jneurosci.org)
  • This suggests that changes to endogenous opioid activity in the BLA during withdrawal may underlie the disruptions to emotional learning processes that support and escalate drug use. (jneurosci.org)
  • Whether BLA endogenous opioid actions are changed by opioid withdrawal is unknown. (jneurosci.org)
Peptide2
  • Introduction from Drug peptide supply about:β-Ala8-Neurokinin A: 4-10 English name β-Ala8-Neurokinin A: 4-10 Chinese name CAS NO 122063-01-8 Peptide sequence Asp-Ser-Phe-Val-beta-Ala-Leu-Met-NH2 Molecular formula C35H56N8O10S1 Molecular weight 780.9 storage temperature 2-8℃ purity ≥98% Package 1mg;5mg;10mg;50mg;100mg,1g or according to customer's detail requirement. (remetide.com)
  • How to buy β-Ala8-Neurokinin A: 4-10 in the U. S. Peptide supplier remetide specializes in the production and sales of It in the USA. (remetide.com)
Synaptic1
  • Under normal physiological conditions, synaptic transmission between the basolateral amygdala (BLA) and the neighboring main island (Im) of GABAergic intercalated cells (ITCs) is strongly inhibited by endogenous opioids. (jneurosci.org)
Tachykinin1
  • Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. (csnpharm.com)
Substance4
  • Substance P and the closely related neurokinin A (NKA) are produced from a polyprotein precursor after alternative splicing of the preprotachykinin A gene. (wikipedia.org)
  • In 1983, Neurokinin A (previously known as substance K or neuromedin L) was isolated from porcine spinal cord and was also found to stimulate intestinal contraction. (wikipedia.org)
  • The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). (wikipedia.org)
  • Thiele, EA, Strittmatter, SM & Snyder, SH 1985, ' Substance K and substance P as possible endogenous substrates of angiotensin converting enzyme in the brain ', Biochemical and Biophysical Research Communications , vol. 128, no. 1, pp. 317-324. (johnshopkins.edu)
Angiotensin1
  • In the brain angiotensin converting enzyme is highly localized to a striatonigral pathway, which contains no endogenous angiotensin. (johnshopkins.edu)
Downregulation1
  • Downregulation of endogenous TRAIL and its effect on the human cancer cell line KELLY. (uni-muenchen.de)
Neurons7
  • 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. (wikipedia.org)
  • The effect of iontophoretic application of neurokinin A was tested on 51 dorsal horn neurons. (mcmaster.ca)
  • Neurokinin A induced a slow, prolonged excitation of 25 of the wide dynamic range neurons. (mcmaster.ca)
  • SR 48968 (50 pg to 1.0 mg/kg, i.v.) did not affect the on‐going basal activity ( n = 8) or the slow excitation induced by neurokinin A in any of the nine wide dynamic range neurons tested. (mcmaster.ca)
  • To eliminate the possibility that systemically administered SR 48968 may not be reaching central sites, SR 48968 was also applied iontophoretically (70-120 nA) to five neurons and tested against excitatory responses to iontophoretically applied neurokinin A. The on‐going activity of these cells were unaffected by SR 48968. (mcmaster.ca)
  • However, responses of wide dynamic range neurons to neurokinin A were totally blocked by i.v. administration (0.5 mg/kg) of the NK‐1 receptor antagonists CP‐96,345 ( n = 7) and CP‐99,994 ( n = 5) but not by CP‐96,344 ( n = 4), the inactive enantiomer of CP‐96,345. (mcmaster.ca)
  • Reproductive neural populations upstream of gonadotropin-releasing hormone (GnRH) neurons, such as kisspeptin, neurokinin B and RFRP-3 (GnIH) neurons, are possible targets for psychosocial stress to inhibit LH pulses, but this has not been well examined, especially in mice in which prior technical limitations prevented assessment of in vivo LH pulse secretion dynamics. (escholarship.org)
Biological1
  • Product English synonyms Biological activity of β-Ala8-Neurokinin A: 4-10. (remetide.com)
Suggests1
  • This possibly suggests an internalization of neurokinin-1 (NK1). (wikipedia.org)
Cells2
  • Presence of endogenous Rab28 in addition to an antigen of 31 kDa corresponding to TbRab28HA (29 kDa) was detected in recombinant Rab28 cells. (estme.org)
  • F) Representative image of endogenous Rab28 in BSF cells. (estme.org)
Human1
  • The association between human endogenous retroviruses and multiple sclerosis: A systematic review and meta-analysis. (nottingham.ac.uk)
Type2
  • The neurokinin type 3 (NK 3 ) receptor antagonists SB-223412 and SR-142801 inhibited vagally mediated cholinergic contractions of bronchi in vitro at stimulation voltages threshold for preganglionic nerve activation but had no effect on vagally mediated contractions evoked at optimal voltage or field stimulation-induced contractions. (johnshopkins.edu)
  • The neurokinin type 3 (NK3) receptor antagonists SB-223412 and SR-142801 inhibited vagally mediated cholinergic contractions of bronchi in vitro at stimulation voltages threshold for preganglionic nerve activation but had no effect on vagally mediated contractions evoked at optimal voltage or field stimulation-induced contractions. (johnshopkins.edu)
Activity1
  • At the same time, it presents local anesthetic properties by blocking potassium channels and its secondary mechanisms of action are thought to increase the activity of endogenous inhibitory control and decrease pain transmission which would explain the central analgesic effects of tramadol. (itopmeds.com)
Role1
  • This work has also expanded to examination of the role of two additional peptides: neurokinin B (NKB) and orphanin FQ (OFQ). (wvu.edu)
Found1
  • We found that endogenous LH pulses in castrated male mice are robustly and rapidly suppressed by one-time, acute restraint stress, with suppression observed as quickly as 12-18 min. (escholarship.org)
Activation1
  • Three other PARs were identified (PARs 2-4) all with a similar mechanism of activation and the reader is referred to a number of excellent reviews which report the ligands for each receptor, endogenous proteases and physiological functions in more comprehensive detail [ 2-4 ]. (silverchair.com)
Antagonists5
  • The invention generally relates to the field of neurokinin antagonists, and more particularly to new substituted aminopyrimidine compounds which are neurokinin antagonists and use of these compounds and their use in treatment and prevention of neurokinin conditions. (justia.com)
  • Considerable pre-clinical findings suggest the use of neurokinin receptor antagonists for the treatment of a wide range of biological diseases including migraine (Goadsby, P. J. (justia.com)
  • However, to date, a detailed understanding of the physiological role of these compounds has been severely hampered by a lack of selective, high affinity, metabolically stable neurokinin receptor antagonists that possess both good bioavailability and CNS penetration. (justia.com)
  • Although several tachykinin receptor antagonists have been described, most have been developed through modifying and/or deleting one or more of the amino acids that comprise the endogenous mammalian tachykinins such that the resulting molecules are still peptides that possess poor pharmacokinetic properties and limited in vivo activities. (justia.com)
  • The most recent new classification of anti-emetic agents are the neurokinin NK 1 antagonists. (vin.com)
NK1R1
Exogenous2
  • 9. Effect of peptidases on the ability of exogenous and endogenous neurokinins to produce neurokinin 1 receptor internalization in the rat spinal cord. (nih.gov)
  • These membrane proteins have evolved to sense a wide range of molecules that can be of either exogenous or endogenous origin. (wur.nl)
Selective9
  • Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 ( NK1 ) receptor antagonist with a K i of 0.66 nM. (medchemexpress.com)
  • L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC 50 of 2.3 nM. (medchemexpress.com)
  • Maropitant is a selective and orally active neurokinin ( NK1 ) receptor antagonist. (medchemexpress.com)
  • Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 ( NK1 ) receptor antagonist. (medchemexpress.com)
  • Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1( NK1 ) receptor antagonist, inhibits [ 3 H]SP binding to the NK1 receptor with pK i values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent. (medchemexpress.com)
  • Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pK i of 10.2 for human neurokinin-1 receptor . (medchemexpress.com)
  • Hemokinin 1, human is a selective tachykinin neurokinin 1 ( NK1 ) receptor full agonist. (medchemexpress.com)
  • GR 64349 is a selective and potent NK2 agonist (EC50 = 3.7 nM in rat colon) with activity comparable to that of neurokinin A (NKA). (creative-peptides.com)
  • Conformationally constrained tachykinin analogs: potent and highly selective neurokinin NK-2 receptor agonists. (creative-peptides.com)
Tachykinin receptor1
Internalization1
  • This possibly suggests an internalization of neurokinin-1 (NK1). (wikipedia.org)
High affinity1
  • 6. Point mutation increases a form of the NK1 receptor with high affinity for neurokinin A and B and septide. (nih.gov)
Neuropeptide1
  • The Tac2 gene encodes the neuropeptide Neurokinin B (NkB) that binds to the Neurokinin 3 receptor (Nk3R) (Fig. 1a ). (nature.com)
Aprepitant2
  • Aprepitant is a neurokinin-1 receptor antagonist. (medscape.com)
  • 17. Hepatoblastoma cells express truncated neurokinin-1 receptor and can be growth inhibited by aprepitant in vitro and in vivo. (nih.gov)
Inhibition1
  • Inhibition of endogenous GRK6 (G-protein-coupled receptor kinase) activity, by the introduction of catalytically inactive K215R GRK6, partially reversed the attenuation of agonist-induced responsiveness, whereas overexpression of wild-type GRK6 increased receptor desensitization. (jneurosci.org)
Mechanisms2
  • Pneumoniae has developed a list of potential reduced aspiration risk or cardiac mr can detect areas of the colon can overwhelm the endogenous scavenger mechanisms. (easternpropane.com)
  • Only by controlling for nonspecific effects can evidence of deficient DNIC become attributed to dysregulation in endogenous analgesic mechanisms. (ap26113.com)
Mediate1
  • 8. Differences in the length of the carboxyl terminus mediate functional properties of neurokinin-1 receptor. (nih.gov)
Gene3
  • The response of the Neurokinin 1-receptor in relation to its gene dose in reverse transfection was studied, as well as response reproducibility during repeated activations. (wur.nl)
  • Kisspeptins (Kp-10, -13, and -14), endogenous agonists for the G-protein-coupled receptor (GPR54), are encoded by the KiSS-1 gene. (momnewsdaily.com)
  • In order to avoid phenotypes from inadvertent disruption of the endogenous gene after integration from the transgene, we studied mice using the transgene in only 1 allele initially. (cancer-ecosystem.com)
Protein2
  • These cells expressed a combination of the Neurokinin 1-receptor and Cameleon YC3.6 protein as calcium indicator. (wur.nl)
  • Manipulation of endogenous GRK2 activity through introduction of either wild-type or catalytically inactive GRK2 ( K220R GRK2) almost completely inhibited agonist-stimulated IP 3 production, implying a phosphorylation-independent regulation of M 1 mACh receptor signaling, most probably mediated by a GRK2 N-terminal RGS-like (regulator of G-protein signaling) domain interaction with GTP-bound Gα q/11 . (jneurosci.org)
Relationship1
  • 3,14,15 Therefore, this suggests that there is a relationship between PCS and endogenous estrogen levels because estrogen is known to weaken vein walls. (phlebolymphology.org)
Chronic1
  • Neurologic patterns of use of quinolones however, overall adverse events o low molecular weight of premature chd or stroke, switching to a chronic sensory neuropathies in which the esophageal mucosa mucosal biopsy is o en result in earlier enzymatic steps of resuscitation should also have additional clinically silenthens. (easternpropane.com)
Levels1
  • DSP4 reduced endogenous NA levels in all central nervous system (CNS) regions analyzed. (researchgate.net)
Treatment1
  • An investigational endogenous opioid being studied for the treatment of COVID-19. (drugbank.com)