نتایج جستجو برای: neighbor on path nop

تعداد نتایج: 8466328  

Journal: :Journal of medicinal chemistry 2011
Gerta Cami-Kobeci Willma E Polgar Taline V Khroyan Lawrence Toll Stephen M Husbands

The unique pharmacological profile of buprenorphine has led to its considerable success as an analgesic and as a treatment agent for drug abuse. Activation of nociceptin/orphanin FQ peptide (NOP) receptors has been postulated to account for certain aspects of buprenorphine's behavioral profile. In order to investigate the role of NOP activation further, a series of buprenorphine analogues has b...

Journal: :The Journal of pharmacology and experimental therapeutics 2016
Michael A Statnick Yanyun Chen Michael Ansonoff Jeffrey M Witkin Linda Rorick-Kehn Todd M Suter Min Song Charlie Hu Celia Lafuente Alma Jiménez Ana Benito Nuria Diaz Maria Angeles Martínez-Grau Miguel A Toledo John E Pintar

Nociceptin/orphanin FQ (N/OFQ), a 17 amino acid peptide, is the endogenous ligand of the ORL1/nociceptin-opioid-peptide (NOP) receptor. N/OFQ appears to regulate a variety of physiologic functions including stimulating feeding behavior. Recently, a new class of thienospiro-piperidine-based NOP antagonists was described. One of these molecules, LY2940094 has been identified as a potent and selec...

Journal: :The Journal of pharmacology and experimental therapeutics 2011
Taline V Khroyan Willma E Polgar Juan Orduna Jose Montenegro Faming Jiang Nurulain T Zaveri Lawrence Toll

1-(1-Cyclooctylpiperidin-4-yl)-indolin-2-one (SR14150) and 1-(1-(2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl)piperidinl-4-yl)-indolin-2-one (SR16835) are moderately selective nociceptin/orphanin FQ (NOP) receptor agonists. In the [(35)S]guanosine 5'-O-(3-thiotriphosphate) assay in vitro, SR14150 is a partial agonist at both the NOP and μ-opioid receptors, whereas SR16835 is a full agonist at the NO...

2018
Francesca Felicia Caputi Elio Acquas Sanjay Kasture Stefania Ruiu Sanzio Candeletti Patrizia Romualdi

BACKGROUND Behavioral studies demonstrated that the administration of Withania somnifera Dunal roots extract (WSE), prolongs morphine-elicited analgesia and reduces the development of tolerance to the morphine's analgesic effect; however, little is known about the underpinning molecular mechanism(s). In order to shed light on this issue in the present paper we explored whether WSE promotes alte...

Journal: :Molecular pharmacology 2013
Courtney L Donica Hibah O Awwad Deepak R Thakker Kelly M Standifer

The nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor is the fourth and most recently discovered member of the opioid receptor superfamily that also includes μ, δ, and κ opioid receptor subtypes (MOR, DOR, and KOR, respectively). The widespread anatomic distribution of the NOP receptor enables the modulation of several physiologic processes by its endogenous agonist, N/OFQ. Accordingly, the...

2016
Mark F. Bird Maria Camilla Cerlesi Mark Brown Davide Malfacini Vanessa Vezzi Paola Molinari Laura Micheli Lorenzo Di Cesare Mannelli Carla Ghelardini Remo Guerrini Girolamo Calò David G. Lambert

INTRODUCTION Opioid receptors are currently classified as Mu (μ), Delta (δ), Kappa (κ) plus the opioid related nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP). Despite compelling evidence for interactions and benefits of targeting more than one receptor type in producing analgesia, clinical ligands are Mu agonists. In this study we have designed a Mu-NOP agonist named DeNo. The Mu agonist...

Journal: :The Journal of pharmacology and experimental therapeutics 2008
Melissa A Burmeister Michael A Ansonoff John E Pintar Daniel R Kapusta

Intracerebroventricular administration of the opioid-like peptide nociceptin/orphanin FQ (N/OFQ) produces bradycardia, hypotension, and diuresis in mice. We hypothesized that these responses are solely caused by selective activation of central N/OFQ peptide (NOP) receptors. To test this premise, we first examined whether i.c.v. N/OFQ produced dose-dependent diuretic and cardiovascular depressor...

2017
Federica Ferrari Davide Malfacini Blair V Journigan Mark F Bird Claudio Trapella Remo Guerrini David G Lambert Girolamo Calo' Nurulain T Zaveri

Nociceptin/orphanin FQ (N/OFQ) regulates several biological functions via selective activation of the N/OFQ receptor (NOP), a member of the opioid receptor family. We recently identified a new high affinity and highly selective NOP agonist AT-403. In this study, we characterized the functional profile of AT-403 and compared it to other known nonpeptide NOP agonists Ro 65-6570, Ro 2q, SCH-221510...

Journal: :Journal of Medicinal Chemistry 2021

The nociceptin/orphanin FQ (N/OFQ)/N/OFQ receptor (NOP) system controls different biological functions including pain and cough reflex. Mixed NOP/opioid agonists elicit similar effects to strong opioids but with reduced side effects. In this work, 31 peptides the general sequence [Tyr/Dmt1,Xaa5]N/OFQ(1-13)-NH2 were synthesized pharmacologically characterized for their action at human recombinan...

Journal: :Revista de Informática Teórica e Aplicada 2021

The parallelism allowed by FPGAs has attracted attention for knowing applications that need processing power. However, the specific and very technical development language not stimulate its broad use. As an alternative, there are High-level Synthesis Languages (HSL), which allow less complicated FPGA they do tend to take full advantage of technology. Therefore, another alternative was developed...

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