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neuropeptide S receptor

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https://www.readbyqxmd.com/read/28317098/cgrp-receptor-activity-in-mice-with-global-expression-of-human-receptor-activity-modifying-protein-1
#1
Keegan J Bohn, Baolin Li, Xiaofang Huang, Bianca N Mason, Anne-Sophie Wattiez, Adisa Kuburas, Christopher S Walker, Peiyi Yang, Jianliang Yu, Beverly A Heinz, Kirk W Johnson, Andrew F Russo
BACKGROUND AND PURPOSE: CGRP is a potent vasodilator and nociceptive neuropeptide linked to migraine. CGRP receptors are heterodimers of receptor activity-modifying protein-1 (RAMP1) and either calcitonin receptor-like receptor (CLR), which forms the canonical CGRP receptor, or calcitonin receptor (CTR), which forms the amylin-1 (AMY1 ) receptor. The goal of this study was to test whether transgenic mice globally expressing human RAMP1 (hRAMP1) have increased CGRP receptor activity and whether the receptors are sensitive to the human selective antagonist telcagepant...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28315588/neuromedin-an-insight-into-its-types-receptors-and-therapeutic-opportunities
#2
REVIEW
Saumitra Gajjar, Bhoomika M Patel
Neuropeptides are small protein used by neurons in signal communications. Neuromedin U was the first neuropeptide discovered from the porcine spinal and showed its potent constricting activities on uterus hence was entitled with neuromedin U. Following neuromedin U another of its isoform was discovered neuromedin S which was observed in suprachiasmatic nucleus hence was entitled neuromedin S. Neuromedin K and neuromedin L are of kanassin class which belong to tachykinin family. Bombesin family consists of neuromedin B and neuromedin C...
January 22, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28302146/relationship-of-acute-axonal-damage-wallerian-degeneration-and-clinical-disability-in-multiple-sclerosis
#3
Shailender Singh, Tobias Dallenga, Anne Winkler, Shanu Roemer, Brigitte Maruschak, Heike Siebert, Wolfgang Brück, Christine Stadelmann
BACKGROUND: Axonal damage and loss substantially contribute to the incremental accumulation of clinical disability in progressive multiple sclerosis. Here, we assessed the amount of Wallerian degeneration in brain tissue of multiple sclerosis patients in relation to demyelinating lesion activity and asked whether a transient blockade of Wallerian degeneration decreases axonal loss and clinical disability in a mouse model of inflammatory demyelination. METHODS: Wallerian degeneration and acute axonal damage were determined immunohistochemically in the periplaque white matter of multiple sclerosis patients with early actively demyelinating lesions, chronic active lesions, and inactive lesions...
March 17, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28300612/characterization-of-melanin-concentrating-hormone-mch-and-its-receptor-in-chickens-tissue-expression-functional-analysis-and-fasting-induced-up-regulation-of-hypothalamic-mch-expression
#4
Lin Cui, Chan Lv, Jiannan Zhang, Chunheng Mo, Dongliang Lin, Juan Li, Yajun Wang
Melanin-concentrating hormone (MCH) is a neuropeptide expressed in the brain and exerts its actions through interaction with the two known G protein-coupled receptors, namely melanin-concentrating hormone receptor 1 and 2 (MCHR1 and MCHR2) in mammals. However, the information regarding the expression and functionality of MCH and MCHR(s) remains largely unknown in birds. In this study, using RT-PCR and RACE PCR, we amplified and cloned a MCHR1-like receptor, which is named cMCHR4 according to its evolutionary origin, and a MCHR2 from chicken brain...
March 11, 2017: Gene
https://www.readbyqxmd.com/read/28296145/synthesis-and-opioid-activity-of-tyr1-z-cf-ch-gly2-and-tyr1-s-r-cf3ch-nh-gly2-leu-enkephalin-fluorinated-pep-tidomimetics
#5
Somnath N Karad, Mohan Pal, Thomas E Prisinzano, Rachel Saylor Crowley, Ryan A Altman
We describe the design, synthesis, and opioid activity of fluoroalkene (Tyr1-ψ[(Z)CF=CH]-Gly2) and trifluoroethylamine (Tyr1-ψ[(S)/(R)-CF3CH-NH]-Gly2) analogs of the endogenous opioid neuropeptide, Leu-enkephalin. The fluoroalkene peptidomimetic exihibited low nanomolar functional activity (5.0 ± 2 nM and 60 ± 15 nM for δ- and μ-opioid receptors, respectively) with a μ/δ-selectivity ratio that mimicked the natural peptide. However, the trifluoroethyl-amine peptidomimetics, irrespective of stereochemistry, did not activate the opioid receptors, which suggest that bulky CF3 substitu-ents are not tolerated at this position...
March 14, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28295755/evidence-for-a-functional-vasoconstrictor-role-for-atp-in-the-human-cutaneous-microvasculature
#6
James A Lang, Alex C Krajek, Kevin A Smaller
Noradrenaline is responsible for eliciting ∼60% of the reflex cutaneous vasoconstriction (VC) response in young adults, whereas the remainder is due to one or more unidentified coreleased sympathetic adrenergic neurotransmitter(s). Inconsistent evidence has placed neuropeptide Y in this role; however, other putative cotransmitters have yet to be tested. We hypothesize that ATP contributes to the reflex cutaneous VC response. Two protocols were conducted in young adults (n = 10); both involved the placement of three microdialysis (MD) probes in forearm skin and whole-body cooling (Tsk  = 30...
March 10, 2017: Experimental Physiology
https://www.readbyqxmd.com/read/28284882/current-findings-on-the-role-of-oxytocin-in-the-regulation-of-food-intake
#7
REVIEW
Maartje S Spetter, Manfred Hallschmid
In the face of the alarming prevalence of obesity and its associated metabolic impairments, it is of high basic and clinical interest to reach a complete understanding of the central nervous pathways that establish metabolic control. In recent years, the hypothalamic neuropeptide oxytocin, which is primarily known for its involvement in psychosocial processes and reproductive behavior, has received increasing attention as a modulator of metabolic function. Oxytocin administration to the brain of normal-weight animals, but also animals with diet-induced or genetically engineered obesity reduces food intake and body weight, and can also increase energy expenditure...
March 8, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28267583/identification-of-the-first-biased-nps-receptor-agonist-that-retains-anxiolytic-and-memory-promoting-effects-with-reduced-levels-of-locomotor-stimulation
#8
Stewart D Clark, Terrence P Kenakin, Steven Gertz, Carla Hassler, Elaine A Gay, Tiffany L Langston, Rainer K Reinscheid, Scott P Runyon
The neuropeptide S system has been implicated in a number of centrally mediated behaviors including memory consolidation, anxiolysis, and increased locomotor activity. Characterization of these behaviors has been primarily accomplished using the endogenous 20AA peptide (NPS) that demonstrates relatively equal potency for the calcium mobilization and cAMP second messenger pathways at human and rodent NPS receptors. This study is the first to demonstrate that truncations of the NPS peptide provides small fragments that retain significant potency only at one of two single polymorphism variants known to alter NPSR function (NPSR-107I), yet demonstrate a strong level of bias for the calcium mobilization pathway over the cAMP pathway...
March 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28228241/neuropeptide-s-reduces-propofol-or-ketamine-induced-slow-wave-states-through-activation-of-cognate-receptors-in-the-rat
#9
Xiang-Pan Kong, Can Wang, Jun-Fan Xie, Peng Zhao, Li-Rong Dai, Yu-Feng Shao, Jian-Sheng Lin, Yi-Ping Hou
Intracerebroventricular injection of NPS reduces the duration of the ketamine- or thiopental-induced loss of the righting reflex in rats. But the specific EEG activities are unknown. We therefore sought to examine the effects of the NPS-NPSR system on anesthetic-induced characteristics of EEG power spectra and sleep-wake profiles. NPS alone or together with an NPSR antagonist was injected intracerebroventricularly, whereas the propofol (50mg/kg) or ketamine (100mg/kg) was administrated intraperitoneally. NPS (1 or 2nmol) significantly reduced the amount of propofol-induced EEG delta activity and slow wave states (SWS)...
February 14, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28194370/peptide-agonists-of-vasopressin-v2-receptor-reduce-expression-of-neuroendocrine-markers-and-tumor-growth-in-human-lung-and-prostate-tumor-cells
#10
Marina Pifano, Juan Garona, Carla S Capobianco, Nazareno Gonzalez, Daniel F Alonso, Giselle V Ripoll
Neuroendocrine tumors (NETs) comprise a heterogeneous group of malignancies that express neuropeptides as synaptophysin, chromogranin A (CgA), and specific neuronal enolase (NSE), among others. Vasopressin (AVP) is a neuropeptide with an endocrine, paracrine, and autocrine effect in normal and pathological tissues. AVP receptors are present in human lung, breast, pancreatic, colorectal, and gastrointestinal tumors. While AVP V1 receptors are associated with stimulation of cellular proliferation, AVP V2 receptor (V2r) is related to antiproliferative effects...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28192258/binding-and-functional-pharmacological-characteristics-of-gepant-type-antagonists-in-rat-brain-and-mesenteric-arteries
#11
Majid Sheykhzade, Nilofar Amandi, Monica Vidal Pla, Bahareh Abdolalizadeh, Anette Sams, Karin Warfvinge, Lars Edvinsson, Darryl S Pickering
AIM: The neuropeptide calcitonin gene-related peptide (CGRP) is found in afferent sensory nerve fibers innervating the resistance arteries and plays a pivotal role in a number of neurovascular diseases such as migraine and subarachnoid bleedings. The present study investigates the binding and antagonistic characteristics of small non-peptide CGRP receptor antagonists (i.e. gepants) in isolated rat brain and mesenteric resistance arteries. METHODS: The antagonistic behavior of gepants was investigated in isolated rat mesenteric arteries using a wire myograph setup while binding of gepants to CGRP receptors was investigated in rat brain membranes using a radioligand competitive binding assay...
March 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28166374/a-potential-role-for-the-secretogranin-ii-derived-peptide-em66-in-the-hypothalamic-regulation-of-feeding-behavior
#12
F Trebak, I Dubuc, A Arabo, A Alaoui, L Boukhzar, J Maucotel, M Picot, S Cherifi, C Duparc, J Leprince, G Prévost, Y Anouar, R Magoul, N Chartrel
EM66 is a conserved 66-amino acid peptide derived from secretogranin II (SgII), a member of the granin protein family. EM66 is widely distributed in secretory granules of endocrine and neuroendocrine cells as well as in hypothalamic neurons. Although EM66 is abundant in the hypothalamus, its physiological function remains to be elucidated. The aim of the present study was to investigate a possible involvement of EM66 in the hypothalamic regulation of feeding behavior. We show that ICV administration of EM66 induces a drastic dose-dependent inhibition of food intake in mice deprived of food for 18 h, which is associated with an increase of hypothalamic POMC and MC3R mRNA levels and c-Fos immunoreactivity in the POMC neurons of the arcuate nucleus...
February 6, 2017: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28165287/cgrp-receptor-antagonist-activity-of-olcegepant-depends-on-the-signalling-pathway-measured
#13
Christopher S Walker, Ann C Raddant, Michael J Woolley, Andrew F Russo, Debbie L Hay
Background Calcitonin gene-related peptide (CGRP) is a neuropeptide that acts in the trigeminovascular system and is believed to play an important role in migraine. CGRP activates two receptors that are both present in the trigeminovascular system; the CGRP receptor and the amylin 1 (AMY1) receptor. CGRP receptor antagonists, including olcegepant (BIBN4096BS) and telcagepant (MK-0974), can treat migraine. This study aimed to determine the effectiveness of these antagonists at blocking CGRP receptor signalling in trigeminal ganglia (TG) neurons and transfected CGRP and AMY1 receptors in Cos7 cells, to better understand their mechanism of action...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28150369/bidirectional-relationship-between-alcohol-intake-and-sensitivity-to-social-defeat-association-with-tacr1-and-avp-expression
#14
Britta S Nelson, Michelle K Sequeira, Jesse R Schank
While epidemiological studies show that alcohol abuse is often co-morbid with affective disorders, the causal direction of this association is unclear. We examined this relationship using mouse models including social defeat stress (SDS), social interaction (SI) and voluntary alcohol consumption. C57BL6/J mice exposed to SDS segregate into two subpopulations, those that express depressive-like phenotypes ('susceptible') and those that do not ('resilient'). First, we stratified SDS-exposed mice and measured their voluntary alcohol consumption...
February 1, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28119086/two-types-of-albino-mutants-in-desert-and-migratory-locusts-are-caused-by-gene-defects-in-the-same-signaling-pathway
#15
Ryohei Sugahara, Seiji Tanaka, Akiya Jouraku, Takahiro Shiotsuki
Albinism is caused by mutations in the genes involved in melanin production. Albino nymphs of Locusta migratoria and Schistocerca gregaria reared under crowded conditions are uniformly creamy-white in color. However, nothing is known about the molecular mechanisms underlying this phenomenon in locusts. The albino strain of L. migratoria is known to lack the dark-color-inducing neuropeptide corazonin (Crz). In this study, we report that this albino strain has a 10-base-pair deletion in the gene LmCRZ, which encodes Crz...
April 15, 2017: Gene
https://www.readbyqxmd.com/read/28093335/intracoerulear-microinjection-of-orexin-a-induces-morphine-withdrawal-like-signs-in-rats
#16
Masoumeh Ghaemi-Jandabi, Hossein Azizi, S Mohammad Ahmadi-Soleimani, Saeed Semnanian
Orexin (hypocretin) neuropeptides play a pivotal role in expression of opioid withdrawal signs. Hypothalamic orexinergic neurons provide dense afferents for the nucleus locus coeruleus (LC). Somatic signs of opioid withdrawal are associated with the enhanced activity of LC neurons. In addition, intra-LC administration of orexin-A leads to the hyperactivity of LC neurons. The present study was an attempt to investigate whether intra-LC microinjection of orexin-A induces morphine withdrawal-like signs in both morphine dependent and control rats...
January 16, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28089664/neurotensin-nts1-and-nts2-receptor-agonists-produce-anxiolytic-like-effects-in-the-22-khz-ultrasonic-vocalization-model-in-rats
#17
Floyd F Steele, Shannon C Whitehouse, Jacob S Aday, Adam J Prus
Neurotensin is a neuropeptide neurotransmitter that interacts with multiple neurotransmitter systems, including those regulating amygdalar function, via NTS1 and NTS2 receptors. Both receptors are expressed in the amygdala and agonists for NTS1 or NTS2 receptors have exhibited anxiolytic effects in animal models. Systemic adminstration of NTS1 receptor agonist PD149163 was recently shown to reduce footshock conditioned 22-kHz ultrasonic vocalizations in rats, suggesting that PD149163 produced an anxiolytic effect...
January 12, 2017: Brain Research
https://www.readbyqxmd.com/read/28058675/neuropeptide-cycloprolylglycine-is-an-endogenous-positive-modulator-of-ampa-receptors
#18
T A Gudasheva, V V Grigoriev, K N Koliasnikova, V L Zamoyski, S B Seredenin
We have previously shown that neuropeptide cycloprolylglycine (CPG) increases the content of brain-derived neurotrophic factor (BDNF) in the culture of neuronal cells under normal conditions and in pathology. This is the first study to show that CPG at a physiological concentration of 10(-6) M significantly enhances the transmembrane AMPA currents in rat cerebellar Purkinje cells. Thus, CPG is a positive endogenous modulator of AMPA receptors. It was assumed that the neuropsychotropic effects of CPG are implemented as a result of BDNF accumulation after the activation of AMPA receptors by this neuropeptide...
November 2016: Doklady. Biochemistry and Biophysics
https://www.readbyqxmd.com/read/28053042/induction-of-migraine-like-photophobic-behavior-in-mice-by-both-peripheral-and-central-cgrp-mechanisms
#19
Bianca N Mason, Eric A Kaiser, Adisa Kuburas, Maria-Cristina M Loomis, John A Latham, Leon F Garcia-Martinez, Andrew F Russo
The neuropeptide calcitonin gene-related peptide (CGRP) is a key player in migraine. Although migraine can be treated using CGRP antagonists that act peripherally, the relevant sites of CGRP action remain unknown. To address the role of CGRP both within and outside the CNS, we used CGRP-induced light-aversive behavior in mice as a measure of migraine-associated photophobia. Peripheral (intraperitoneal) injection of CGRP resulted in light-aversive behavior in wild-type CD1 mice similar to aversion seen previously after central (intracerebroventricular) injection...
January 4, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28043969/the-role-of-nfkb-in-drug-addiction-beyond-inflammation
#20
REVIEW
S E Nennig, J R Schank
AIMS: Nuclear factor kappa light chain enhancer of activated B cells (NFkB) is a ubiquitous transcription factor well known for its role in the innate immune response. As such, NFkB is a transcriptional activator of inflammatory mediators such as cytokines. It has recently been demonstrated that alcohol and other drugs of abuse can induce NFkB activity and cytokine expression in the brain. A number of reviews have been published highlighting this effect of alcohol, and have linked increased NFkB function to neuroimmune-stimulated toxicity...
January 1, 2017: Alcohol and Alcoholism: International Journal of the Medical Council on Alcoholism
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