Cyclic lactam analogues of ovine pituitary adenylate cyclase activating polypeptide (PACAP): discovery of potent type II receptor antagonists.

abstract：:Trefoil factors (TFFs) 1, 2 and 3 are small polypeptides that are co-secreted with mucin throughout the body. They are up-regulated in cancer and inflammatory processes in the gastrointestinal system, where they are proposed to be involved in tissue regeneration, proliferation and protection. Our aim was to explore th...

journal_title：Peptides

authors： Viby NE,Nexø E,Kissow H,Andreassen H,Clementsen P,Thim L,Poulsen SS

更新日期：2015-01-01 00:00:00

abstract：:Bombyxin-IV, a molecular species of bombyxin, which is a member of insulin-like heterodimeric peptides of the silkworm Bombyx mori with prothoracicotropic hormone activity, was synthesized. The A- and B-chains of bombyxin-IV containing four and two Cys residues, respectively, were first synthesized separately by solid...

journal_title：Peptides

authors： Maruyama K,Nagasawa H,Isogai A,Tamura S,Ishizaki H,Suzuki A

更新日期：1990-01-01 00:00:00

abstract：:The anorectic effect of IP injection of amylin (1 microgram/kg) was abolished by simultaneous IP injection of the amylin receptor antagonist calcitonin gene-related peptide-(8-37) [CGRP(8-37), 10 micrograms/kg]. The IP injection of pancreatic glucagon (400 micrograms/kg) at dark onset also reduced food intake in 24-h ...

journal_title：Peptides

authors： Lutz TA,Del Prete E,Szabady MM,Scharrer E

更新日期：1996-01-01 00:00:00

abstract：:Intracerebroventricular injections of rat hypothalamic growth hormone-releasing factor (rhGRF) were examined for effects on food intake in free-feeding rats. It was found that, in picomole doses, rhGRF had a stimulatory effect on food intake. Examination of higher doses of rhGRF revealed a decrease in the facilitatory...

journal_title：Peptides

authors： Vaccarino FJ,Feifel D,Rivier J,Vale W,Koob GF

更新日期：1988-01-01 00:00:00

abstract：:We sought to establish Endothelin (ET-3) role in the central regulation of bile secretion in the rat. The intracerebroventricular (icv) injection of ET-3 evoked a cholestatic or a choleretic effect depending on the administered dose. Lower doses increased bile flow and bicarbonate excretion, whereas higher doses decre...

journal_title：Peptides

authors： Rodríguez MR,Sabbatini ME,Santella G,Dabas P,Villagra A,Vatta MS,Bianciotti LG

更新日期：2005-07-01 00:00:00

abstract：:Modification to the structure of glucagon has provided a number of glucagon receptor antagonists with possible therapeutic application for diabetes. These novel peptide analogs include desHis(1)Pro(4)Glu(9)-glucagon and desHis(1)Pro(4)Glu(9)(Lys(30)PAL)-glucagon. This study has evaluated the metabolic benefits of once...

journal_title：Peptides

authors： McShane LM,Franklin ZJ,O'Harte FP,Irwin N

更新日期：2014-10-01 00:00:00

abstract：:Effects of spantide ([D-Arg1,D-Trp7,9,Leu11]substance P) on coronary resistance vessels were studied in isolated guinea pig hearts perfused at constant rate with isotonic buffer containing 20 or 40 mM KCl. Spantide (1 microM) caused a 20-fold rightward shift of the substance P (SP) dose-response curve for vasodilation...

journal_title：Peptides

authors： Hoover DB

更新日期：1991-09-01 00:00:00

abstract：:Obestatin is a second peptide derived from the preproghrelin polypeptide. It was originally thought to have anorexigenic effects, thereby functioning as an antagonist of ghrelin. However, this has been a subject of debate ever since. Since acylated ghrelin strongly induces insulin resistance, it could be hypothesized ...

journal_title：Peptides

authors： Kiewiet RM,Gauna C,van Aken MO,van de Zande B,van der Lely AJ

更新日期：2008-12-01 00:00:00

abstract：:Rhesus monkey MCH-R1 and MCH-R2 receptors were cloned. Amino acid homology is 98.8% between monkey and human MCH-R1, while monkey and human MCH-R2 are 98% homologous. Binding and intracellular signaling characteristics of the monkey receptors were compared with the human homologues. The results demonstrate that MCH bi...

journal_title：Peptides

authors： Fried S,O'Neill K,Hawes BE

更新日期：2002-08-01 00:00:00

abstract：:The 41-residue corticotropin releasing factor (CRF) was synthesized by the solid phase method. The synthetic CRF and arginine vasopressin (AVP) were examined for ACTH releasing activity and effects on the release of 5 other pituitary hormones in vivo and in vitro. Injection of the CRF into pharmacologically blocked ra...

journal_title：Peptides

authors： Turkelson CM,Arimura A,Culler MD,Fishback JB,Groot K,Kanda M,Luciano M,Thomas CR,Chang D,Chang JK,Shimizu M

更新日期：1981-01-01 00:00:00

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...

journal_title：Peptides

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

更新日期：2001-07-01 00:00:00

abstract：:The hypophysiotrophic hormone corticotropin releasing factor (CRF) stimulates the anterior pituitary corticotroph to export stress hormones such as adrenocorticotrophic hormone (ACTH). In rat anterior pituitary cells, CRF-induced elevation of cyclic AMP was profoundly potentiated (by an order of magnitude) by stimulat...

journal_title：Peptides

authors： Cronin MJ,Zysk JR,Baertschi AJ

更新日期：1986-09-01 00:00:00

abstract：:A new, p -carborane containing analog of tyrosine, 3-[1-hydroxy-1,12-dicarba-closo-dodecaboran (12)-12-yl]alanine, was prepared from protected 3-[1-hydroxy-1,12-dicarba-closo-dodecaboran (12)-12-yl]propionic acid in five steps using Oppolzer's sultam methodology for asymmetric hydroxyamination as the key step. The tyr...

journal_title：Peptides

authors： Ujváry I,Nachman RJ

更新日期：2002-04-01 00:00:00

abstract：:This paper reviews aspects of NPY research that were emerging in 1985, shortly after the isolation and characterization of the peptide. NPY had become known for its widespread distribution especially in the central and peripheral nervous systems, but also in the gastro-intestinal and respiratory tracts and in fibers i...

journal_title：Peptides

authors： Chronwall BM,Zukowska Z

更新日期：2004-03-01 00:00:00

abstract：:Food deprivation and adrenalectomy are associated with low concentrations of leptin in blood and the absence of obesity. Because leptin is known to cross the blood-brain barrier (BBB) by a saturable transport system, we examined whether fasting and adrenalectomy (ADX) also act at the BBB. Multiple-time regression anal...

journal_title：Peptides

authors： Kastin AJ,Akerstrom V

更新日期：2000-05-01 00:00:00

abstract：:Cholecystokinin induces a reduction in exploratory behaviors which could reflect an underlying behavioral state of either satiety or malaise. To investigate these alternative hypotheses, the effects of CCK were compared to the effects of (a) consumption of an extra quantity of palatable food, of (b) bombesin at doses ...

journal_title：Peptides

authors： Crawley JN

更新日期：1983-07-01 00:00:00

abstract：:Instability and proteolytic degradation limit the delivery options and in vivo efficacy of many therapeutic peptides. We previously generated a thioether stabilized angiotensin-(1-7) analog, cAng-(1-7), which is resistant against proteolytic degradation in the circulation. We here investigated oral and pulmonary deliv...

journal_title：Peptides

authors： de Vries L,Reitzema-Klein CE,Meter-Arkema A,van Dam A,Rink R,Moll GN,Akanbi MH

更新日期：2010-05-01 00:00:00

abstract：:Prolactin (PRL) is known to exert neuroprotective effects against excitotoxic damage in the hippocampus of female rats, both in vitro and in vivo. It is still unknown whether this effect can be seen in the male hippocampus and intracellular signaling mediating such action. To assess this, adult male CD-1 mice were sub...

journal_title：Peptides

authors： Anagnostou I,Muñoz-Mayorga D,Morales T

更新日期：2021-01-01 00:00:00

abstract：:Irisin was first identified in skeletal muscle cells, but its precise location has not yet been demonstrated, and there is limited information about irisin protein in other human and rat tissues. The present immunohistochemical study was undertaken to screen skeletal muscle and other tissues for irisin immunoreactivit...

journal_title：Peptides

authors： Aydin S,Kuloglu T,Aydin S,Kalayci M,Yilmaz M,Cakmak T,Albayrak S,Gungor S,Colakoglu N,Ozercan IH

更新日期：2014-11-01 00:00:00

abstract：:Two molecular forms of gonadotropin-releasing hormone (GnRH) were identified in the extracts of various brain areas, spinal cord and pituitary in female and male goldfish and had chromatographic and immunological properties similar to [His5, Trp7, Tyr8]-GnRH (cGnRH-II) and [Trp7,Leu8]-GnRH (sGnRH). Radioimmunoassay us...

journal_title：Peptides

authors： Yu KL,Sherwood NM,Peter RE

更新日期：1988-05-01 00:00:00

abstract：:Endothelial neutral endopeptidase (EC 3.4.24.11, NEP) contributes to the inactivation of vasoactive and inflammatory peptides such as f-Met-Leu-Phe, substance P, atrial natriuretic peptide, and bradykinin. The aim of the present study was to investigate the cellular regulation of NEP expression in human endothelial ce...

journal_title：Peptides

authors： Graf K,Kunkel K,Zhang M,Gräfe M,Schultz K,Schudt C,Biroc S,Fleck E,Kunkel G

更新日期：1995-01-01 00:00:00

abstract：:Four potent angiotensin converting enzyme (ACE) inhibitory peptides, IY, RIY, VW and VWIS, were isolated from subtilisin digest of rapeseed protein. Among them RIY and VWIS are new peptides with IC(50) 28 and 30 microM, respectively. All isolated peptides lowered blood pressure of spontaneously hypertensive rats (SHR)...

journal_title：Peptides

authors： Marczak ED,Usui H,Fujita H,Yang Y,Yokoo M,Lipkowski AW,Yoshikawa M

更新日期：2003-06-01 00:00:00

abstract：:The actions of a behaviorally active luteinizing hormone-releasing hormone fragment, Ac-LHRH(5-10), on CA1 pyramidal cells were studied utilizing conventional intracellular recordings from the in vitro rat hippocampal slice preparation. The behaviorally active fragment (10(-7) M) and the natural decapeptide [LHRH(1-10...

journal_title：Peptides

authors： Chen Y,Wong M,Moss RL

更新日期：1993-09-01 00:00:00

abstract：:In the conscious dog migrating and nonmigrating colonic motor complexes (CMC) were recorded by means of chronically implanted strain gauge force transducers. Intravenous injection of a synthetic enkephalin analogue immediately induced a premature CMC at all three recording sites of the colon. Naloxone inhibited the en...

journal_title：Peptides

authors： Bickel M,Belz U

更新日期：1988-05-01 00:00:00

abstract：:The distribution of somatostatin (SRIF) was examined in normal human forebrain, using thick vibratome cut sections. The unlabeled antibody enzyme method of immunocytochemistry revealed a widespread distribution of SRIF immunoreactive neurons and fibers throughout the septum, diencephalon and corpus striatum. Within th...

journal_title：Peptides

authors： Bennett-Clarke CA,Joseph SA

更新日期：1986-09-01 00:00:00

abstract：:The proteolytic conversion of oxytocin and vasopressin by purified rat brain synaptic membranes was studied at 37 degrees C and physiological pH 7.4. The formed peptide fragments were isolated by high performance liquid chromatography and characterized by amino acid analysis. When oxytocin was incubated with synaptic ...

journal_title：Peptides

authors： Stancampiano R,Melis MR,Argiolas A

更新日期：1991-09-01 00:00:00

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...

journal_title：Peptides

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

abstract：:Opioid receptor analyses of deltorphin A (H-Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2) analogues indicated the following: (a) increased negativity differentially affected affinities (Ki) and selectivity (Ki mu/Ki delta); (b) shifted sequence heptapeptides, [Asp5,Leu6,Met-NH2(7)] and [Asp4,His5,Leu6,Met-NH2(7)], reversed selec...

journal_title：Peptides

authors： Lazarus LH,Salvadori S,Attila M,Grieco P,Bundy DM,Wilson WE,Tomatis R

更新日期：1993-01-01 00:00:00

abstract：:Arginine vasopressin (AVP), which is synthesized and secreted in the hypothalamic paraventricular nucleus (PVN), is the most important bioactive substance in the pain modulation. Our pervious study had shown that AVP plays an important role in pain modulation in caudate nucleus (CdN). The experiment was designed to in...

journal_title：Peptides

authors： Yang J,Li P,Zhang XY,Zhang J,Hao F,Pan YJ,Lu GZ,Lu L,Wang DX,Wang G,Yan FL

更新日期：2011-01-01 00:00:00

abstract：:We tested the endogenous tripeptide TRH (thyrotropin releasing hormone) ability to bind to MC (melanocortin) receptor subtypes. We discovered that TRH binds to the human MCI receptor expressed in COS cells and to murine B16 melanoma cells with 5790+/-1010 nM and 6370+/-1260 nM Ki's, respectively. TRH did not bind to t...

journal_title：Peptides

authors： Schiöth HB,Prusis P,Muceniece R,Mutulis F,Mutule I,Wikberg JE

更新日期：1999-01-01 00:00:00