Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors.

Abstract:

:A series of cyclic conformationally restricted penicillamine containing somatostatin octapeptide analogues have been prepared by standard solid phase synthetic techniques and tested for their ability to inhibit specific [125I]CGP 23,996 (des-Ala1-,Gly2-[desamino-Cys3Tyr11]-dicarba3, 14-somatostatin), [3H]naloxone or [3H]DPDPE ([D-Pen2-D-Pen5]enkephalin) binding in rat brain membrane preparations. We now report structure-activity relationship studies with the synthesis of our most potent and selective mu opioid receptor compound D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2, which we refer to as Cys2Tyr3Orn5Pen7-amide. While this octapeptide exhibited high affinity (IC50 = 2.80 nM) for an apparently single population of binding sites (nH = 0.89 +/- 0.1) and exceptional selectivity for mu opioid receptors with an IC50(DPDPE)/IC50 (naloxone) ratio of 4,829, it also displayed very low affinity for somatostatin receptors (IC50 = 22,700 nM). Thus, Cys2Tyr3Orn5Pen7-amide may be the ligand of choice for further characterization of mu opioid receptors and for examining the physiological role of this class of receptors.

journal_name

Life Sci

journal_title

Life sciences

authors

Gulya K,Pelton JT,Hruby VJ,Yamamura HI

doi

10.1016/0024-3205(86)90574-6

subject

Has Abstract

pub_date

1986-06-16 00:00:00

pages

2221-9

issue

24

eissn

0024-3205

issn

1879-0631

pii

0024-3205(86)90574-6

journal_volume

38

pub_type

杂志文章
  • The potential of asiaticoside for TGF-β1/Smad signaling inhibition in prevention and progression of hypoxia-induced pulmonary hypertension.

    abstract:AIMS:Asiaticoside (AS) is a saponin monomer extracted from the medicinal plant Centella asiatica, which has a variety of biological effects. We intended to investigate the effects of asiaticoside on a hypoxia-induced pulmonary hypertension (HPH) rat model and examine the possible effects of asiaticoside on TGF-β1/Smad ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2015.07.016

    authors: Wang XB,Wang W,Zhu XC,Ye WJ,Cai H,Wu PL,Huang XY,Wang LX

    更新日期:2015-09-15 00:00:00

  • Changes in the liver protein pattern of female Wistar rats treated with the hypoglycemic agent SDZ PGU 693.

    abstract::SDZ PGU 693 acts as a hypoglycemic agent by stimulating glucose utilisation in insulin-sensitive peripheral tissues, such as skeletal muscle and fat. In a 28 day toxicity study the compound was found to induce hepatocellular hypertrophy in Wistar rats treated with 300 mg/kg/day. To gain insights into the pathomechanis...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(98)00509-8

    authors: Arce A,Aicher L,Wahl D,Anderson NL,Meheus L,Raymackers J,Cordier A,Steiner S

    更新日期:1998-01-01 00:00:00

  • Effects of the cannabinoid receptor agonist CP 55,940 and the cannabinoid receptor antagonist SR 141716 on intracranial self-stimulation in Lewis rats.

    abstract::Lewis rats were trained to self-stimulate the medial forebrain bundle (MFB) using a rate-frequency paradigm. They were then tested for the effects of the cannabinoid receptor agonist CP 55,940, the selective cannabinoid receptor antagonist SR 141716 and the dopamine D1 receptor antagonist SCH 23390. CP 55,940 (0, 10, ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(01)01366-2

    authors: Arnold JC,Hunt GE,McGregor IS

    更新日期:2001-11-21 00:00:00

  • Effect of melatonin on bone metabolism in ovariectomized rats.

    abstract::To assess the effect of pharmacological dose of melatonin on bone metabolism in ovariectomized rats, urinary deoxypyridinoline (a marker of bone resorption) and calcium excretion, circulating levels of calcium, phosphorus and bone alkaline phosphatase activity (a marker of bone formation), and bone mineral density (BM...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(01)01431-x

    authors: Ladizesky MG,Cutrera RA,Boggio V,Somoza J,Centrella JM,Mautalen C,Cardinali DP

    更新日期:2001-12-21 00:00:00

  • Dysregulated ion channels and transporters activate endoplasmic reticulum stress in rat kidney of fetal growth restriction.

    abstract:AIMS:The mechanisms underlying the fetal origin of renal disease remains unknown. This study aimed to investigate the profiles of ion channel and transporter proteins in the fetal kidney in fetal growth restriction (FGR)rats, and to explore their association with the fetal origin of renal disease. MAIN METHODS:An FGR ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.118276

    authors: Guo Y,Lu Y,Wang J,Zhu L,Liu X

    更新日期:2020-10-15 00:00:00

  • Harmine inhibits the proliferation and migration of glioblastoma cells via the FAK/AKT pathway.

    abstract:AIMS:Glioblastoma is one of the most invasive tumors of the central nervous system, and has a high degree of malignancy and poor prognosis. Harmine, an active ingredient extracted from perennial herbs, has been reported to have obvious antitumor effects on various tumors. However, the effects of harmine on glioblastoma...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2021.119112

    authors: Zhu YG,Lv YX,Guo CY,Xiao ZM,Jiang QG,Kuang H,Zhang WH,Hu P

    更新日期:2021-01-26 00:00:00

  • Endocrine influences on the actions of morphine: IV. Effects of sex and strain.

    abstract::The antinociceptive and temperature responses to morphine were compared in male and female rats from two different strains. Males of both the Sprague-Dawley and Wistar-Furth strains were slightly more responsive to the acute actions of morphine than were females of the same strain. However, Wistar-Furth animals requir...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(84)90633-7

    authors: Kasson BG,George R

    更新日期:1984-04-23 00:00:00

  • Molecular process in acute liver injury and regeneration induced by carbon tetrachloride.

    abstract::Injection of carbon tetrachloride (CCl4) intraperitoneally into model animals induces acute liver injury mediated by reactive oxygen species (ROS) as normal metabolites in hepatocytes. In this study, the molecular process in this type of liver injury was analyzed from the aspect of liver function and regulatory factor...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2004.02.030

    authors: Taniguchi M,Takeuchi T,Nakatsuka R,Watanabe T,Sato K

    更新日期:2004-08-13 00:00:00

  • The response to analgesia testing is affected by gonadal steroids in the rat.

    abstract::The effect of gonadal steroids on the response to analgesia testing was determined in castrated male and female rats and castrated male and female rats treated with testosterone propionate (TP) and estradiol benzoate (EB), respectively. The time to respond to a noxious somatic stimulus in the form of heat was assessed...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(89)90631-0

    authors: Forman LJ,Tingle V,Estilow S,Cater J

    更新日期:1989-01-01 00:00:00

  • Polynitroxyl albumin plus tempol attenuates liver injury and inflammation after hepatic ischemia and reperfusion.

    abstract::PNA+Tempol, albumin containing conjugated (polynitroxyl albumin; PNA) and free (4-hydroxyl-2,2,6,6-tetramethyl-piperidinyl-1-oxyl; Tempol) nitroxide may protect against injury caused by reactive oxygen species. Therefore, the actions of PNA+Tempol on liver injury and inflammation induced by hepatic ischemia and reperf...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(00)00907-3

    authors: Blonder JM,McCalden TA,Hsia CJ,Billings RE

    更新日期:2000-11-17 00:00:00

  • A gene-based anti-angiogenesis therapy as a novel strategy for cancer treatment.

    abstract::Angiogenesis-targeted therapy of cancer is considered a promising strategy for therapeutic management of cancer progression. Over the last two decades, a few anti-angiogenesis monoclonal antibodies (mAbs) blocking VEGF signaling have been developed and approved by the FDA. The most widely used anti-angiogenesis drug i...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2019.117018

    authors: Fallah A,Heidari HR,Bradaran B,Sisakht MM,Zeinali S,Molavi O

    更新日期:2019-12-15 00:00:00

  • Augmented platelet calcium uptake in response to serotonin stimulation in patients with major depression measured using Mn2+ influx and 45Ca2+ uptake.

    abstract::There is an augmented platelet intracellular calcium response to serotonin stimulation in major depression. The role that calcium influx has in this process is not known. The objective of this study was to determine platelet calcium influx in response to serotonin by two methods, Mn2+ influx and 45Ca2+ uptake, in orde...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(99)00608-6

    authors: Plein H,Berk M,Eppel S,Butkow N

    更新日期:2000-01-01 00:00:00

  • Hepatoprotective effect of celecoxib against tamoxifen-induced liver injury via inhibiting ASK-1/JNK pathway in female rats.

    abstract::Hepatotoxicity is a common side effect encountered with tamoxifen (TAM) administration. Due to the great value of TAM in breast cancer treatment, hepato-protection is seriously recommended. AIMS:The present study investigated the hepato-protective effect of celecoxib (CX) against TAM-induced hepatotoxicity in rats. ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2019.116573

    authors: El-Kashef DH,El-Sheakh AR

    更新日期:2019-08-15 00:00:00

  • Therapeutic evaluation of solid lipid nanoparticle of quercetin in pentylenetetrazole induced cognitive impairment of zebrafish.

    abstract:BACKGROUND:Quercetin is a major flavonoid in various plants. It possesses the multiple pharmacological actions like vascular integrity and regulatory action of the blood-brain barrier. AIMS:The present study is focused on evaluating the role of solid lipid nanoparticle of quercetin in pentylenetetrazole (PTZ) induced ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2018.03.010

    authors: Rishitha N,Muthuraman A

    更新日期:2018-04-15 00:00:00

  • Protective effect of cepharanthin on cisplatin-induced renal toxicity through metallothionein expression.

    abstract:AIMS:Cisplatin (CDDP) is a potent anticancer agent, but severe renal toxicity can limit its use. We investigated the protective effect of cepharanthin (CE), a biscoclaurin alkaloid, on the renal toxicity of CDDP. MAIN METHODS:Mice were given CDDP along with CE. Effects of CE on CDDP toxicity were investigated by assay...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2013.01.031

    authors: Sogawa N,Hirai K,Sogawa C,Ohyama K,Miyazaki I,Tsukamoto G,Asanuma M,Sasaki A,Kitayama S

    更新日期:2013-04-09 00:00:00

  • Promoting effect of concanavalin A on transport of sodium cefoxitin and phenol red from rat rectal compartment.

    abstract::Concanavalin A enhanced the rat rectal absorption of phenol red and cefoxitin at pH 7.4 and the uptake of cefoxitin into brush border membrane vesicles prepared from rat rectal membrane. The enhancing action of concanavalin A demonstrated a sodium ion dependency and was inhibited by the presence of 4,4'-diisothiocyano...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(84)90496-x

    authors: Nishihata T,Higuchi T

    更新日期:1984-01-30 00:00:00

  • Motilin acts within the CNS to inhibit urinary bladder contractions.

    abstract::Although peripheral actions have been shown for the brain-gut peptide, motilin, its localization in the CNS of mammals suggests some physiological role at this site. In the present experiments intracerebroventricular or intrathecal, but not peripheral, administrations of motilin produced a dose-related and naloxone re...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(84)90043-2

    authors: Porreca F,Dray A

    更新日期:1984-06-25 00:00:00

  • Protein kinase C inhibitor chelerythrine attenuates the morphine-induced excitatory amino acid release and reduction of the antinociceptive effect of morphine in rats injected intrathecally with pertussis toxin.

    abstract::Neuropathic pain syndromes respond poorly to opioid treatment. In our previous studies, we found that intrathecal (i.t.) injection of pertussis toxin (PTX) produces thermal hyperalgesia, which is poorly responsive to morphine and is accompanied by an increase in cerebrospinal fluid (CSF) levels of excitatory amino aci...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2005.08.020

    authors: Wu GJ,Wen ZH,Chang YC,Yang SN,Tao PL,Wong CS

    更新日期:2006-03-13 00:00:00

  • Measurement of endogenous dopamine and norepinephrine release from superfused slices of rat prefrontal cortex in vitro: modulation by D2 and alpha-2 presynaptic receptors.

    abstract::Endogenous dopamine (DA) and norepinephrine (NE) in the superfusate from slices of rat medial prefrontal cortex were measured by high-performance liquid chromatography coupled to electrochemical detection (HPLC-ECD). Stimulation with high K+ or methamphetamine (MAP) evoked a dose-dependent elevation in the release of ...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(91)90356-g

    authors: Ohmori T,Koyama T,Yamashita I

    更新日期:1991-01-01 00:00:00

  • mCPP but not TFMPP is an antagonist at cardiac 5HT3 receptors.

    abstract::The prototypic arylpiperazines, meta-chlorophenylpiperazine (mCPP), meta-trifluoromethylphenylpiperazine (TFMPP) and quipazine are widely studied serotonergic ligands with nonselective effects at 5HT1 and 5HT2 receptor subtypes. The present study was designed to compare the affinities of these arylipiperazines at 5HT3...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(92)90372-v

    authors: Robertson DW,Bloomquist W,Wong DT,Cohen ML

    更新日期:1992-01-01 00:00:00

  • Mechanism underlying the block of human Cav3.2 T-type Ca2+ channels by benidipine, a dihydropyridine Ca2+ channel blocker.

    abstract:AIMS:Benidipine, a dihydropyridine Ca(2+) channel blocker, has been reported to block T-type Ca(2+) channels; however, the mechanism underlying this effect was unclear. In this study, we characterized the mechanism responsible for this blocking activity. Furthermore, the blocking activity was compared between two enant...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2011.03.019

    authors: Inayoshi A,Sugimoto Y,Funahashi J,Takahashi S,Matsubara M,Kusaka H

    更新日期:2011-05-09 00:00:00

  • Z-4 allele upstream of the aldose reductase gene is associated with proliferative retinopathy in Japanese patients with NIDDM, and elevated luciferase gene transcription in vitro.

    abstract::We determined by PCR the number of (A-C)n repeats in the 2. 1 kb upstream of the aldose reductase (AR2) gene in healthy control subjects and in patients with NIDDM in Japanese. Sixty-one patients were recruited based on the severity of retinopathy and subdivided into two groups with proliferative retinopathy and witho...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(99)00329-x

    authors: Ikegishi Y,Tawata M,Aida K,Onaya T

    更新日期:1999-01-01 00:00:00

  • Lack of both α2-antiplasmin and plasminogen activator inhibitor type-1 induces high IgE production.

    abstract:AIMS:We investigated the pathophysiological changes in mice lacking α2-antiplasmin (α2-AP) and plasminogen activator inhibitor type-1 (PAI-1) genes, and elucidated the involvement of these inhibitors for fibrinolysis in immune response. MAIN METHODS:The pathophysiological changes induced by a lack of both α2-AP and PA...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2013.05.023

    authors: Okada K,Ueshima S,Kawao N,Yano M,Tamura Y,Tanaka M,Sakamoto A,Hatano M,Arima M,Miyata S,Nagai N,Tokuhisa T,Matsuo O

    更新日期:2013-07-30 00:00:00

  • The emerging roles of KPNA2 in cancer.

    abstract::Karyopherin α2 (KPNA2, also known as importinα-1), a member of the nuclear transporter family, is involved in the nucleocytoplasmic transport pathway of a variety of tumor-associated proteins. Recent studies have found that KPNA2 is overexpressed in various cancers, which is associated with poor prognosis. In addition...

    journal_title:Life sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.lfs.2019.117140

    authors: Han Y,Wang X

    更新日期:2020-01-15 00:00:00

  • Time course study for antigen-induced airway hyperreactivity and the effect of soluble IL-5 receptor.

    abstract::To study the role of IL-5 in allergic airway hyperreactivity, the time course for the production of cytokines, the infiltration of inflammatory cells and the onset of airway hyperreactivity after three inhalations of antigens were studied in mice. The effect of the soluble alpha-chain of murine recombinant interleukin...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(94)90139-2

    authors: Yamaguchi S,Nagai H,Tanaka H,Tsujimoto M,Tsuruoka N

    更新日期:1994-01-01 00:00:00

  • NMDA and glycine regulate the affinity of the Mg2+-block site in NR1-1a/NR2A NMDA receptor channels expressed in Xenopus oocytes.

    abstract::NMDA receptors are glutamate-regulated ion channels of critical importance for many neurophysiological and neuropathological processes. Mg2+ blocks the NMDA receptor by binding to the channel pore with an apparent affinity that depends on the membrane potential. We have investigated the effect of NMDA and the required...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/s0024-3205(01)00975-4

    authors: Liu Y,Hill RH,Arhem P,von Euler G

    更新日期:2001-03-09 00:00:00

  • Mitochondrial characteristics contribute to proliferation and migration potency of MDA-MB-231 cancer cells and their response to cisplatin treatment.

    abstract:AIM:Despite recent advances in therapeutic strategies, cancer is still a leading cause of mortality worldwide. Mitochondrial dysfunction is implicated in cancer initiation and metastasis, and even in chemo- and radio-resistance. However, the precise role of mitochondria in cancer is crosstalk and controversial. This st...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.117339

    authors: Kheirandish-Rostami M,Roudkenar MH,Jahanian-Najafabadi A,Tomita K,Kuwahara Y,Sato T,Roushandeh AM

    更新日期:2020-03-01 00:00:00

  • Thiol group may be involved in the irreversible blockade of presynaptic alpha 2-adrenoreceptors by pyrextramine and benextramine in the isolated guinea pig ileum.

    abstract::This study, conducted on isolated guinea pig ileum, was designed to establish the mechanism of presynaptic alpha 2-adrenoreceptor blockade by the tetramine disulfides, benextramine and pyrextramine. At 1 microM these drugs irreversibly blocked norepinephrine (NE)-induced inhibition of the twitch response to electrical...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/0024-3205(86)90407-8

    authors: Brasili L,Cassinelli A,Angeli P,Melchiorre C

    更新日期:1986-05-05 00:00:00

  • Viscus fat area contributes to the Framingham 10-year general cardiovascular disease risk in patients with type 2 diabetes mellitus.

    abstract:OBJECTIVE:To explore the correlation of the viscus fat area (VFA) with the Framingham 10-year general cardiovascular disease risk in patients with type 2 diabetes mellitus (T2DM). METHODS:A total of 202 patients with T2DM were divided into two groups based on VFA (a VFA ≥ 100 cm2 group and a VFA < 100 cm2 group), or f...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2019.01.036

    authors: Xu L,Song P,Xu J,Zhang H,Yu C,Guan Q,Zhao M,Zhang X

    更新日期:2019-03-01 00:00:00

  • Advanced chronic kidney disease is associated with higher serum concentration of monocyte microparticles.

    abstract::Advanced chronic kidney disease is associated with high rates of cardiovascular disease. Considering the crucial role of capillaries in renal function, our study aimed to evaluate microparticles related to vascular physiology examining the link between stages of chronic kidney disease with circulating endothelial (EMP...

    journal_title:Life sciences

    pub_type: 杂志文章

    doi:10.1016/j.lfs.2020.118295

    authors: Fonseca F,Ballerini AP,Izar MC,Kato J,Ferreira CE,Fonzar W,do Amaral J,Rezende P,Machado-Santelli G,França C

    更新日期:2020-11-01 00:00:00