Further studies on the pharmacological features of the nociceptin/orphanin FQ receptor ligand ZP120.


:ZP120 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) ligand. In previous studies, the effects of ZP120 were found to be sensitive to J-113397 in mouse tissues while resistant to UFP-101 in rat tissues. The aim of this study was to further investigate the ZP120 pharmacological profile using mouse and rat preparations, J-113397 and UFP-101, as well as NOP receptor knockout (NOP(-/-)) mice. Electrically stimulated mouse and rat vas deferens were used to characterize the pharmacology of ZP120 in vitro. For in vivo studies the tail-withdrawal assay was performed in wild type (NOP(+/+)) and NOP knockout (NOP(-/-)) mice. In the mouse and rat vas deferens ZP120 mimicked the effects of N/OFQ showing higher potency but lower maximal effects. In both preparations, J-113397 antagonized N/OFQ and ZP120 effects showing similar pK(B) values ( approximately 7.8). UFP-101 antagonized the actions of N/OFQ (pK(B) values approximately 7.3) but did not modify the effects of ZP120. The inhibitory effects of N/OFQ and ZP120 were no longer evident in vas deferens tissues taken from NOP(-/-) mice. In NOP(+/+) mice subjected to the tail-withdrawal assay, ZP120 (1 nmol) mimicked the pronociceptive action of N/OFQ (10 nmol), producing longer lasting effects. The effects of both peptides were absent in NOP(-/-) animals. The NOP receptor ligand ZP120 is a high potency NOP selective partial agonist able to evoke long-lasting effects; its diverse antagonist sensitivity in comparison with N/OFQ may derive from different modality of binding to the NOP receptor.






Fischetti C,Rizzi A,Gavioli EC,Marzola G,Trapella C,Guerrini R,Petersen JS,Calo G




Has Abstract


2009-02-01 00:00:00
















  • Beta-amyloid peptides undergo regulated co-secretion with neuropeptide and catecholamine neurotransmitters.

    abstract::Beta-amyloid (Aβ) peptides are secreted from neurons, resulting in extracellular accumulation of Aβ and neurodegeneration of Alzheimer's disease. Because neuronal secretion is fundamental for the release of neurotransmitters, this study assessed the hypothesis that Aβ undergoes co-release with neurotransmitters. Model...


    pub_type: 杂志文章


    authors: Toneff T,Funkelstein L,Mosier C,Abagyan A,Ziegler M,Hook V

    更新日期:2013-08-01 00:00:00

  • Change in substance P in a firearm wound and its significance.

    abstract::The present study was designed to detect the change of substance P (SP) in firearm wounds and its relationship with wound healing. Twenty two rabbits were randomly divided into two groups, one with firearm wounds created by steel balls shooting rabbits' thighs and another with stab wounds created by knife. The experim...


    pub_type: 杂志文章


    authors: Xinan L,Suguang L,Liangchao Z,Lei C

    更新日期:1998-01-01 00:00:00

  • Investigation of gastrin-releasing peptide as a mediator for 5'-guanidinonaltrindole-induced compulsive scratching in mice.

    abstract::Gastrin-releasing peptide (GRP) has been implicated in the itch-scratch cycle. We investigated if this gut-brain-skin peptide plays a role in the compulsive, hindleg scratching of the neck of mice by 5'-guanidinonaltrindole (GNTI), the kappa opioid receptor antagonist, and in the antipruritic activity of nalfurafine, ...


    pub_type: 杂志文章


    authors: Inan S,Dun NJ,Cowan A

    更新日期:2011-02-01 00:00:00

  • Molecular cloning, over expression, and activity studies of a peptidic HIV-1 protease inhibitor: designed synthetic gene to functional recombinant peptide.

    abstract::The aspartic protease inhibitor (ATBI) purified from a Bacillus sp. is a potent inhibitor of several proteases including recombinant HIV-1 protease, pepsin, and fungal aspartic protease. In this study, we report the cloning, and over expression of a synthetic gene coding for ATBI in Escherichia coli and establish a pu...


    pub_type: 杂志文章


    authors: Vathipadiekal V,Umasankar PK,Patole MS,Rao M

    更新日期:2010-01-01 00:00:00

  • Differential distribution of chicken-I and chicken-II GnRH in the turtle brain.

    abstract::Chicken-I and chicken-II gonadotropin-releasing hormone (cI-GnRH and cII-GnRH) were shown to be differentially distributed in the brain of a turtle, Trachemys scripta, by HPLC and specific radioimmunoassays. The cI-GnRH was most concentrated in the median eminence (ME), while cII-GnRH was most concentrated in the caud...


    pub_type: 杂志文章


    authors: Tsai PS,Licht P

    更新日期:1993-03-01 00:00:00

  • Migrating motor complex recorded spontaneously and induced by motilin and erythromycin in an ex vivo rabbit intestinal preparation.

    abstract::We investigated basal motility and the motor effects of motilin, erythromycin, and prostigmine on segments of rabbit gastrointestinal tract removed from extrinsic neural and vascular pathway and immersed in an oxygenated organ bath. Motility was recorded by means of four strain gauges sutured on the serosal surface of...


    pub_type: 杂志文章


    authors: Marzio L,Grossi L,Martelli L,Falcucci M,Lapenna D

    更新日期:1994-01-01 00:00:00

  • Upregulation of ANP and NPR-C mRNA in the kidney and heart of eNOS knockout mice.

    abstract:OBJECTIVES:The aim of the present studywas to examine the question of whether the atrial natriuretic peptide (ANP) system is altered by endothelial nitric-oxide synthase (eNOS). METHODS:Male eNOS-deficient mice (eNOS-/-) and wild type control mice (eNOS+/+, C57B1/6J) were used. Blood pressure was measured in anestheti...


    pub_type: 杂志文章


    authors: Yuan K,Kim SY,Oh YB,Yu J,Shah A,Park BH,Kim SH

    更新日期:2010-07-01 00:00:00

  • Plasma levels and diagnostic value of catestatin in patients with heart failure.

    abstract::Catestatin (CST) is an endogenous neuropeptide with multiple cardiovascular activities. The study is to investigate circulating CST levels in heart failure (HF) patients and to evaluate the role of CST as a biomarker for HF. Plasma CST concentrations were measured by enzyme-linked immunosorbent assay in 228 HF patient...


    pub_type: 杂志文章


    authors: Liu L,Ding W,Li R,Ye X,Zhao J,Jiang J,Meng L,Wang J,Chu S,Han X,Peng F

    更新日期:2013-08-01 00:00:00

  • Exploiting endogenous opioids: Lessons learned from endomorphin 2 in the female rat.

    abstract::Effective management of chronic pain is demanded by ethical as well as medical considerations. Although opioid analgesics remain among the most effective pharmacotherapies for ameliorating many types of pain, their use is clouded by concerns regarding their addictive properties, underscored by the current epidemic of ...


    pub_type: 杂志文章,评审


    authors: Gintzler AR,Liu NJ,Storman EM,Wessendorf MW

    更新日期:2019-02-01 00:00:00

  • Significance of the N- and C-terminal regions of CAP-1, a cuticle calcification-associated peptide from the exoskeleton of the crayfish, for calcification.

    abstract::Calcification-associated peptide (CAP)-1 is considered to play an important role in calcification of the exoskeleton of the crayfish, Procambarus clarkii. In this study, in order to clarify the molecular mechanism of calcification, we constructed expression systems of recombinant molecules of CAP-1 and its related pep...


    pub_type: 杂志文章


    authors: Inoue H,Ohira T,Nagasawa H

    更新日期:2007-03-01 00:00:00

  • Urocortin and corticotropin-releasing factor receptor expression in the human colonic mucosa.

    abstract::Urocortin is a newly identified member of the CRF neuropeptide family. Urocortin has been found to bind with high affinity to CRF receptors. The present study investigated urocortin and CRF receptor expression in human colonic mucosa. Non-pathologic sections of adult colorectal tissues were obtained from patients with...


    pub_type: 杂志文章


    authors: Muramatsu Y,Fukushima K,Iino K,Totsune K,Takahashi K,Suzuki T,Hirasawa G,Takeyama J,Ito M,Nose M,Tashiro A,Hongo M,Oki Y,Nagura H,Sasano H

    更新日期:2000-12-01 00:00:00

  • Comparative analysis of kisspeptin-immunoreactivity reveals genuine differences in the hypothalamic Kiss1 systems between rats and mice.

    abstract::Kiss1 mRNA and its corresponding peptide products, kisspeptins, are expressed in two restricted brain areas of rodents, the anteroventral periventricular nucleus (AVPV) and the arcuate nucleus (ARC). The concentration of mature kisspeptins may not directly correlate with Kiss1 mRNA levels, because mRNA translation and...


    pub_type: 杂志文章


    authors: Overgaard A,Tena-Sempere M,Franceschini I,Desroziers E,Simonneaux V,Mikkelsen JD

    更新日期:2013-07-01 00:00:00

  • Characterization of growth hormone-releasing hormone (GHRH) binding to cloned porcine GHRH receptor.

    abstract::To study structure-activity relationships of growth hormone-releasing hormone (GHRH), a competitive binding assay was developed using cloned porcine adenopituitary GHRH receptors expressed in human kidney 293 cells. Specific binding of [His1, 125I-Tyr10,Nle27]hGHRH(1-32)-NH2 increased linearly with protein concentrati...


    pub_type: 杂志文章


    authors: Hassan HA,Hsiung HM,Zhang XY,Smith DP,Smiley DL,Heiman ML

    更新日期:1995-01-01 00:00:00

  • The synthesis of an analogue of the locust CRF-like diuretic peptide, and the biological activities of this and some C-terminal fragments.

    abstract::The synthesis is described of an analogue of the locust CRF-like diuretic peptide in which methionine in positions 1,3, and 13 is replaced by isosteric methyl-homoserine residues. This analogue has been tested for biological activity on Malpighian tubules in vitro, and feeding behavior in vivo. It is highly active in ...


    pub_type: 杂志文章


    authors: Goldsworthy GJ,Chung JS,Simmonds MS,Tatari M,Varouni S,Poulos CP

    更新日期:2003-10-01 00:00:00

  • Differential antagonism of endomorphin-1 and endomorphin-2 supraspinal antinociception by naloxonazine and 3-methylnaltrexone.

    abstract::To determine if different subtypes of mu-opioid receptors were involved in antinociception induced by endomorphin-1 and endomorphin-2, the effect of pretreatment with various mu-opioid receptor antagonists beta-funaltrexamine, naloxonazine and 3-methylnaltrexone on the inhibition of the paw-withdrawal induced by endom...


    pub_type: 杂志文章


    authors: Sakurada S,Hayashi T,Yuhki M,Fujimura T,Murayama K,Yonezawa A,Sakurada C,Takeshita M,Sato T,Zadina JE,Kastin AJ,Sakurada T

    更新日期:2002-05-01 00:00:00

  • Effects of estradiol, progesterone, and norethisterone on regional concentrations of galanin in the rat brain.

    abstract::Concentrations of immunoreactive galanin were compared in eight gross brain regions of ovariectomized female rats treated with either estradiol, estradiol + progesterone, estradiol + norethisterone, or placebo. Higher concentrations with estradiol treatment compared with placebo were found in the pituitary (357%), fro...


    pub_type: 杂志文章


    authors: Rugarn O,Theodorsson A,Hammar M,Theodorsson E

    更新日期:1999-01-01 00:00:00

  • The female reproductive system of the kissing bug, Rhodnius prolixus: arrangements of muscles, distribution and myoactivity of two endogenous FMRFamide-like peptides.

    abstract::Phalloidin staining F-actin was used to image muscle fiber arrangements present in the reproductive system of the adult female Rhodnius prolixus. A mesh of muscle fibers encircles the ovaries whereas a criss-cross pattern of finer muscle fibers covers each ovariole. Two layers of muscle fibers (arranged longitudinally...


    pub_type: 杂志文章


    authors: Sedra L,Lange AB

    更新日期:2014-03-01 00:00:00

  • Neuropeptides interact with glycolipid receptors: a surface plasmon resonance study.

    abstract::Using Surface Plasmon Resonance (SPR) we investigated the interaction of seven neuropeptides with different characteristics and beta-amyloid (Abeta42) peptide, with membranes containing gangliosides. A wide range of affinities characterized the bindings (K(D) = 10(-3)- 10(-7) M), following the scheme: for GM1, Abeta42...


    pub_type: 杂志文章


    authors: Valdes-Gonzalez T,Inagawa J,Ido T

    更新日期:2001-07-01 00:00:00

  • Synthetic peptides related to the dermorphins. II. Synthesis and biological activities of new analogues.

    abstract::A new series of analogues of the potent opiate-like peptides dermorphins (mainly tetra- and pentapeptides) were synthesized in order to better evaluate the structure-activity relationships. Relative potencies were referred to dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2), the prototype of this class of frog skin pe...


    pub_type: 杂志文章


    authors: Melchiorri P,Erspamer GF,Erspamer V,Guglietta A,De Castiglione R,Faoro F,Perseo G,Piani S,Santangelo F

    更新日期:1982-09-01 00:00:00

  • Immunoreactive peptides related to dynorphin B (= rimorphin) in the rat brain.

    abstract::We have developed a radioimmunoassay for synthetic dynorphin B, a novel opioid tridecapeptide, which shares a common precursor molecule with dynorphin1-17 (= dynorphin A) and the neo-endorphins. The levels of immunoreactivity towards this peptide in rat brain and pituitary show a pattern quantitatively and qualitative...


    pub_type: 杂志文章


    authors: Zhu YX,Höllt V,Loh H

    更新日期:1983-11-01 00:00:00

  • Endorphin and MSH in concert form the corticotropic principle released by tilapia (Oreochromis mossambicus; Teleostei) melanotropes.

    abstract::HPLC characterization of tilapia pituitary endorphins using an antibody specific for N-terminally acetylated endorphins yielded three major peaks in the neurointermediate lobe, but none in the pars distalis. The melanotropes secreted two of the immunoreactive products in vitro, one of which coeluted with Xenopus laevi...


    pub_type: 杂志文章


    authors: Balm PH,Hovens ML,Wendelaar Bonga SE

    更新日期:1995-01-01 00:00:00

  • Cholinergic and VIPergic effects on thyroid hormone secretion in the mouse.

    abstract::The thyroid gland is known to harbor cholinergic and VIPergic nerves. In the present study, the influences of cholinergic stimulation by carbachol, cholinergic blockade by methylatropine and stimulation with various VIP sequences on basal, TSH-induced and VIP-induced thyroid hormone section were investigated in vivo i...


    pub_type: 杂志文章


    authors: Ahrén B

    更新日期:1985-07-01 00:00:00

  • Sympathetic nervous system-targeted neuropeptide Y overexpression in mice enhances neointimal formation in response to vascular injury.

    abstract::Sympathetic neurotransmitter neuropeptide Y (NPY) is associated with vascular remodelling, neointimal hyperplasia and atherosclerosis in experimental animal models and clinical studies. In order to study the role of sympathetic nerve-produced NPY in vascular diseases, transgenic mouse model overexpressing NPY in centr...


    pub_type: 杂志文章


    authors: Ruohonen ST,Abe K,Kero M,Toukola L,Ruohonen S,Röyttä M,Koulu M,Pesonen U,Zukowska Z,Savontaus E

    更新日期:2009-04-01 00:00:00

  • Neuropeptides associated with the frontal ganglion of larval Lepidoptera.

    abstract::The occurrence of neuropeptides in the frontal ganglia of larvae of the tobacco hawkmoth, Manduca sexta, the tomato moth, Lacanobia oleracea and the cotton leafworm, Spodoptera littoralis was investigated using reversed-phase high performance liquid chromatography (RP-HPLC), matrix-assisted laser desorption time of fl...


    pub_type: 杂志文章


    authors: Audsley N,Matthews J,Weaver RJ

    更新日期:2005-01-01 00:00:00

  • Regulation of ghrelin secretion during pregnancy and lactation in the rat: possible involvement of hypothalamus.

    abstract::We investigated the plasma concentration of ghrelin peptide during pregnancy and lactation in rats. Plasma ghrelin levels on days 10 and 15 of pregnancy were significantly lower than those of the non-pregnant rats. Thereafter, the plasma ghrelin levels on day 20 of pregnancy sharply increased to levels comparable with...


    pub_type: 杂志文章


    authors: Shibata K,Hosoda H,Kojima M,Kangawa K,Makino Y,Makino I,Kawarabayashi T,Futagami K,Gomita Y

    更新日期:2004-02-01 00:00:00

  • Osmotic stimulation affects neurohypophysial corticotropin releasing factor-41 content: effect of dexamethasone.

    abstract::In this study we examined the effects of 2% saline loading (S), partial restriction of water consumption (R) or a combination of S or R with dexamethasone (DEX) treatment for 14 days on corticotropin releasing factor (CRF)-41 content of the neurointermediate lobe (NIL) and supraoptic nuclei (SON) of male Wistar rats. ...


    pub_type: 杂志文章


    authors: Dohanics J,Linton EA,Lowry PJ,Makara GB

    更新日期:1990-01-01 00:00:00

  • Combined effects of vasoactive intestinal peptide and dopamine on adenylate cyclase in prolactin-secreting cells.

    abstract::VIP stimulates adenylate cyclase activity of male and female rat anterior pituitaries and human prolactinomas, while dopamine inhibits the enzyme activity of female rat pituitaries and prolactinomas. A dopamine inhibited cyclase can be detected also in male rats provided the enzyme activity is increased by VIP. The an...


    pub_type: 杂志文章


    authors: Oliva D,Vallar L,Giannattasio G,Spada A,Nicosia S

    更新日期:1984-11-01 00:00:00

  • Isolation of a gastrin releasing peptide receptor from normal rat pancreas.

    abstract::The presence of a putative GRP receptor on rat pancreatic particulate membranes was demonstrated by covalent cross-linking to 125I-gastrin releasing peptide (GRP), which revealed a radioactive band with Mr = 80-90 kDa on reduced SDS-PAGE. Fresh rat pancreatic membranes contained a GRP receptor which was solubilized wi...


    pub_type: 杂志文章


    authors: Kane MA,Kelley K,Ross SE,Portanova LB

    更新日期:1991-03-01 00:00:00

  • Immunohistochemical and chromatographic studies of peptides with tachykinin-like immunoreactivity in the central nervous system of the lamprey.

    abstract::The distribution and chemical properties of compounds with tachykinin-like immunoreactivity (TK-LI) in the spinal cord and brain of lampreys (Lampetra fluviatilis and Ichthyomyzon unicuspis) were investigated by means of immunohistochemistry and various chromatographic methods combined with radioimmunoassay. The distr...


    pub_type: 杂志文章


    authors: Van Dongen PA,Theodorsson-Norheim E,Brodin E,Hökfelt T,Grillner S,Peters A,Cuello AC,Forssmann WG,Reinecke M,Singer EA

    更新日期:1986-03-01 00:00:00

  • Synthesis, conformational studies and biological activities of VIP and related fragments.

    abstract::VIP and related fragments were prepared by the solid-phase method. The peptides were assembled on a benzhydrylamine resin and couplings of the Boc-amino acids were carried out by the symmetrical anhydride method. Cleavage was achieved by treatment with liquid HF and purification was accomplished by successive steps of...


    pub_type: 杂志文章


    authors: Fournier A,Saunders JK,St-Pierre S

    更新日期:1984-03-01 00:00:00