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acth chemical properties

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https://www.readbyqxmd.com/read/27586814/influence-of-the-n-terminus-acetylation-of-semax-a-synthetic-analog-of-acth-4-10-on-copper-ii-and-zinc-ii-coordination-and-biological-properties
#1
Antonio Magrì, Giovanni Tabbì, Alessandro Giuffrida, Giuseppe Pappalardo, Cristina Satriano, Irina Naletova, Vincenzo G Nicoletti, Francesco Attanasio
Semax is a heptapeptide (Met-Glu-His-Phe-Pro-Gly-Pro) that encompasses the sequence 4-7 of N-terminal domain of the adrenocorticotropic hormone and a C-terminal Pro-Gly-Pro tripeptide. N-terminal amino group acetylation (Ac-Semax) modulates the chemical and biological properties of parental peptide, modifying the ability of Semax to form complex species with Cu(II) ion. At physiological pH, the main complex species formed by Ac-Semax, [CuLH-2](2-), consists in a distorted CuN3O chromophore with a weak apical interaction of the methionine sulphur...
August 27, 2016: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/26789203/characterization-of-multisubstituted-corticotropin-releasing-factor-crf-peptide-antagonists-astressins
#2
Judit Erchegyi, Lixin Wang, Jozsef Gulyas, Manoj Samant, Marilyn H Perrin, Kathy Lewis, Charleen Miller, Joan Vaughan, Cynthia Donaldson, Wolfgang Fischer, William Low, Seiichi Yakabi, Hiroshi Karasawa, Yvette Taché, Catherine Rivier, Jean Rivier
CRF mediates numerous stress-related endocrine, autonomic, metabolic, and behavioral responses. We present the synthesis and chemical and biological properties of astressin B analogues {cyclo(30-33)[D-Phe(12),Nle(21,38),C(α)MeLeu(27,40),Glu(30),Lys(33)]-acetyl-h/r-CRF(9-41)}. Out of 37 novel peptides, 17 (2, 4, 6-8, 10, 11, 16, 17, 27, 29, 30, 32-36) and 16 (3, 5, 9, 12-15, 18, 19, 22-26, 28, 31) had k(i) to CRF receptors in the high picomolar and low nanomole ranges, respectively. Peptides 1, 2, and 11 inhibited h/rCRF and urocortin 1-induced cAMP release from AtT20 and A7r5 cells...
February 11, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26299832/-naming-and-classification-of-steroids-and-human-stress-ulcers-articles-of-historic-significance-published-by-hans-selye-70-years-ago
#3
REVIEW
Sándor Szabó, Klára Gyires
The name of Hans Selye is mostly known worldwide as the discoverer of stress reaction. Yet, he made numerous other seminal and clinically relevant discoveries. Namely, since he had a focused research on steroid hormones originating from the adrenal cortex that play a crucial role in stress response, he was the first who introduced about 70 years ago the first classification of steroids that is still valid nowadays. This is based on three objective facts: (a) the names of steroid groups are identical with their organ of origin (e...
August 30, 2015: Orvosi Hetilap
https://www.readbyqxmd.com/read/22336046/experimental-ft-ir-ft-raman-nmr-and-theoretical-spectroscopic-properties-of-intermolecular-hydrogen-bonded-1-acetyl-2-thiohydantoin-polymorphs
#4
Anamika Sharma, Vineet Gupta, Poonam Tandon, Poonam Rawat, Shiro Maeda, Ko-Ki Kunimoto
In this work, use of FT-Raman, FT-IR and (13)C NMR spectroscopies have been made for the full characterization of 1-acetyl-2-thiohydantoin (ACTH). A detailed interpretation of the vibrational spectra was carried out with the aid of normal coordinate analysis using single scaling factor. Our results support the hydrogen bonding pattern proposed in the reported crystalline structure. Good reproduction of experimental values is obtained and % error is small in majority of the cases. Isotropic chemical shifts were calculated using gauge-invariant atomic orbital (GIAO) along with several thermodynamic parameters...
May 2012: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/22045543/influence-of-amino-acid-composition-and-phosphorylation-on-the-ion-yields-of-peptides-in-maldi-ms
#5
Daiki Asakawa, Shohey Moriguchi, Mitsuo Takayama
The influence of arginine (Arg), lysine (Lys), and phenylalanine (Phe) residues and phosphorylation on the molecular ion yields of model peptides have been quantitatively studied using matrix-assisted laser desorption/ionization (MALDI) mass spectrometry in both positive- and negative-ion mode. The results obtained from these experiments have been interpreted from the standpoint of two different components, namely, desorption and ionization, on the basis of the physicochemical properties of constituent amino acids of the model peptides...
January 2012: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/21074436/discovery-of-nbi-77860-gsk561679-a-potent-corticotropin-releasing-factor-crf1-receptor-antagonist-with-improved-pharmacokinetic-properties
#6
John E Tellew, Marion Lanier, Manisha Moorjani, Emily Lin, Zhiyong Luo, Deborah H Slee, Xiaohu Zhang, Sam R J Hoare, Dimitri E Grigoriadis, Yves St Denis, Romano Di Fabio, Enza Di Modugno, John Saunders, John P Williams
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to identify antagonists with improved physico-chemical properties a new series of CRF(1) antagonists were designed to substitute the propyl groups at the C7 position of the pyrazolo[1,5-a]pyrimidine core of 1 with heterocycles. Compound (S)-8d was identified as a high affinity ligand with a pK(i) value of 8.2 and a functional CRF(1) antagonist with pIC(50) value of 7...
December 15, 2010: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/18669209/-neurohypophyseal-neuropeptides-and-unipolar-depression-which-future
#7
G Scantamburlo, W Pitchot, M Ansseau, J J Legros
Vasopressin (AVP) and oxytocin (OT) are two chemically similar neurohypophyseal neuropeptides which could be involved in mood disorders. Those two sister neuropeptides might be considered as ago-antagonist hormones. They act as neuromodulators of the stress response. AVP is known as an ACTH stimulating factor synergistic to CRH while OT could act as an antagonist of AVP on ACTH secretion. AVP seems to play an important role in the pathophysiology of major depression. Evidence suggests a role for OT as an endogenous antidepressant/anxiolytic hormone...
May 2008: Revue Médicale de Liège
https://www.readbyqxmd.com/read/18057828/diluted-isoflurane-as-a-suitable-alternative-for-diethyl-ether-for-rat-anaesthesia-in-regular-toxicology-studies
#8
Toshiaki Nagate, Tomonobu Chino, Chizuru Nishiyama, Daisuke Okuhara, Toru Tahara, Yoshimasa Maruyama, Hiroko Kasahara, Kayoko Takashima, Sayaka Kobayashi, Yoshiyuki Motokawa, Shin-ichi Muto, Junji Kuroda
Despite its explosive properties and toxicity to both animals and humans, diethyl ether is an agent long used in Japan in the anaesthesia jar method of rat anaesthetises. However, in response to a recent report from the Science Council of Japan condemning diethyl ether as acceptable practice, we searched for an alternative rat anaesthesia method that provided data continuous with pre-existing regular toxicology studies already conducted under diethyl ether anaesthesia. For this, we examined two candidates; 30% isoflurane diluted with propylene glycol and pentobarbitone...
November 2007: Journal of Veterinary Medical Science
https://www.readbyqxmd.com/read/15769796/distinct-functional-properties-of-native-somatostatin-receptor-subtype-5-compared-with-subtype-2-in-the-regulation-of-acth-release-by-corticotroph-tumor-cells
#9
COMPARATIVE STUDY
Joost van der Hoek, Marlijn Waaijers, Peter M van Koetsveld, Diana Sprij-Mooij, Richard A Feelders, Herbert A Schmid, Philippe Schoeffter, Daniel Hoyer, Davide Cervia, John E Taylor, Michael D Culler, Steven W J Lamberts, Leo J Hofland
In a series of human corticotroph adenomas, we recently found predominant mRNA expression of somatostatin (SS) receptor subtype 5 (sst5). After 72 h, the multiligand SS analog SOM230, which has a very high sst5 binding affinity, but not Octreotide (OCT), significantly inhibited basal ACTH release. To further explore the role of sst5 in the regulation of ACTH release, we conducted additional studies with mouse AtT-20 cells. SOM230 showed a 7-fold higher ligand binding affinity and a 19-fold higher potency in stimulating guanosine 5'-O-(3-thiotriphosphate) binding in AtT-20 cell membranes compared with OCT...
August 2005: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/15678666/-an-experimental-substantiation-for-using-the-semax-neuroprotector-in-the-treatment-of-optic-nerve-diseases
#10
N L Sheremet, G S Polunin, A N Ovchinnikov, A A Kamenskiĭ, N G Levitskaia, L A Andreeva, L Iu Alfeeva, I Iu Nagaev
In order to substantiate the feasibility of using the "Semax" neuroprotector in the treatment of optic-nerve diseases its pharmacokinetics in the intranasal administration was studied in experiments with rats; besides, the physical-and-chemical properties of "Semax" were investigated to define the preparation's stability and mobility in the electric field. A series of experiments, involving a tritium-marked "Semax", showed that the peptide actively penetrates into the brain and eyes of experimental animals after its intranasal administration...
November 2004: Vestnik Oftalmologii
https://www.readbyqxmd.com/read/15001661/targeting-melanocortin-receptors-as-a-novel-strategy-to-control-inflammation
#11
REVIEW
Anna Catania, Stefano Gatti, Gualtiero Colombo, James M Lipton
Adrenocorticotropic hormone and alpha-, beta-, and gamma-melanocyte-stimulating hormones, collectively called melanocortin peptides, exert multiple effects upon the host. These effects range from modulation of fever and inflammation to control of food intake, autonomic functions, and exocrine secretions. Recognition and cloning of five melanocortin receptors (MCRs) has greatly improved understanding of peptide-target cell interactions. Preclinical investigations indicate that activation of certain MCR subtypes, primarily MC1R and MC3R, could be a novel strategy to control inflammatory disorders...
March 2004: Pharmacological Reviews
https://www.readbyqxmd.com/read/14486383/some-aspects-of-the-relationship-between-chemical-structure-and-melanocyte-stimulating-properties-of-several-peptides-related-to-adrenocorticotropin
#12
B T PICKERING, C H LI
No abstract text is available yet for this article.
August 27, 1962: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/14165903/some-biological-and-chemical-properties-of-a-lysine-vasopressin-dimer
#13
A V SCHALLY, R GUILLEMIN
No abstract text is available yet for this article.
April 1964: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/14142029/a-synthetic-polypeptide-ciba-30-920-ba-with-adrenocorticotrophic-properties
#14
G ENNIS, R GORDON, B HUDSON
No abstract text is available yet for this article.
April 18, 1964: Medical Journal of Australia
https://www.readbyqxmd.com/read/14093855/-the-antihistaminic-properties-of-the-blood-interpretative-considerations-and-therapeutic-possibilities-role-of-gamma-globulin
#15
REVIEW
A C NEGRINI, L BELLONI
No abstract text is available yet for this article.
October 1963: Archivio "E. Maragliano" di Patologia e Clinica
https://www.readbyqxmd.com/read/13208741/-investigations-on-chemical-characteristics-and-certain-properties-of-acth-from-cattle-pituitary
#16
L M BROUDE, T S SAKHATSKAIA, N G SEREBRENNIKOVA
No abstract text is available yet for this article.
July 1954: Biokhimii︠a︡
https://www.readbyqxmd.com/read/12436936/nonpeptide-vasopressin-receptor-antagonists-development-of-selective-and-orally-active-v1a-v2-and-v1b-receptor-ligands
#17
REVIEW
C Serradeil-Le Gal, J Wagnon, G Valette, G Garcia, M Pascal, J P Maffrand, G Le Fur
The involvement of vasopressin (AVP) in several pathological states has been reported recently and the selective blockade of the different AVP receptors could offer new clinical perspectives. During the past few years, various selective, orally active AVP V1a (OPC-21268, SR49059 (Relcovaptan)), V2 (OPC-31260, OPC-41061 (Tolvaptan), VPA-985 (Lixivaptan), SR121463, VP-343, FR-161282) and mixed V1a/V2 (YM-087 (Conivaptan), JTV-605, CL-385004) receptor antagonists have been intensively studied in various animal models and have reached, Phase IIb clinical trials for some of them...
2002: Progress in Brain Research
https://www.readbyqxmd.com/read/12379511/recombinant-interleukin-1-beta-activates-the-hypothalamic-pituitary-interrenal-axis-in-rainbow-trout-oncorhynchus-mykiss
#18
J W Holland, T G Pottinger, C J Secombes
The present study provides the first direct evidence that implicates fish cytokines as the effector molecules by which the immune system signals the neuroendocrine system and activates the hypothalamic-pituitary-interrenal stress axis. I.p. injections of trout recombinant interleukin-1 beta (rIL-1 beta) or E. coli lipopolysaccharide (LPS), at concentrations known to induce immune/inflammatory responses in vivo (0.1-0.6 nmol/kg and 1.3 mg/kg respectively), significantly elevated plasma cortisol levels in a dose- and/or time-dependent manner...
October 2002: Journal of Endocrinology
https://www.readbyqxmd.com/read/9404305/effects-of-progestin-administration-on-the-hypothalamic-pituitary-adrenal-axis-and-glucose-homeostasis-in-dogs
#19
P J Selman, J A Mol, G R Rutteman, E van Garderen, T S van den Ingh, A Rijnberk
The effects of medroxyprogesterone acetate (MPA) and proligestone (PROL) on the hypothalamic-pituitary-adrenocortical axis and glucose homeostasis were studied in two groups of eight ovariohysterectomized beagle bitches. In addition, the binding characteristics of MPA and PROL for the progesterone and glucocorticoid receptor were investigated. The administration of both progestins resulted in suppression of the hypothalamic-pituitary-adrenal axis. Whereas basal plasma concentrations of adrenocorticotrophic hormone (ACTH) were only moderately affected, the basal plasma concentrations of cortisol and the cortisol:creatinine ratio in urine were significantly decreased after the first administration of both progestins...
1997: Journal of Reproduction and Fertility. Supplement
https://www.readbyqxmd.com/read/9220373/characterization-of-corticotropin-releasing-hormone-binding-sites-in-the-human-placenta
#20
B O Saeed, D R Weightman, C H Self
The human placenta synthesizes and secretes large amounts of corticotropin-releasing hormone (CRH) which has been implicated in the triggering of parturition. The placental CRH was found to act in a paracrine manner to stimulate secretion of ACTH and beta-endorphin. In view of this we sought to characterize CRH binding sites in the human placenta. The specific binding of 125I-tyrosyl-ovine CRH (125I-oCRH) to placental membranes was dependent on time, temperature, pH, divalent cations and was reversible on addition of excess oCRH...
July 1997: Journal of Receptor and Signal Transduction Research
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