Dermorphin (acetate)
目录号 : GC47188
An opioid peptide
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dermorphin is an opioid peptide originally isolated from the skin of South American frogs (Ph. sauvagei).1 It binds to μ-opioid receptors (Ki = 0.54 nM) and is selective for μ- over δ-opioid receptors in radioligand binding assays (Ki = 929 nM). In vivo, dermorphin (1.9 µmol/kg, i.p.) inhibits noxious stimuli-induced neuronal firing in the nucleus lateralis anterior and ventrobasal complex in rats.2 It inhibits the electrical stimulation-induced C fiber response in rat dorsal horn nociceptive neurons. Dermorphin (10-120 pmol/animal, i.c.v.) delays gastric emptying, inhibits gastric acid secretion, and slows colonic motility in pylorus-ligated rats.
1.Usenko, A.B., Emel'yanova, T.G., and MIasoedov, N.F.Dermorphins are natural opioids with an unique primary structure that determines their biological specificityBiol. Bull. Russ. Acad. Sci.29154-164(2002) 2.Melchiorri, P., and Negri, L.The dermorphin peptide familyGen. Pharmacol.27(7)1099-1107(1996)
| Cas No. | N/A | SDF | |
| Canonical SMILES | OC(C=C1)=CC=C1C[C@H](NC(CNC([C@@H](NC([C@@H](C)NC([C@@H](N)CC2=CC=C(C=C2)O)=O)=O)CC3=CC=CC=C3)=O)=O)C(N4[C@H](C(N[C@@H](CO)C(N)=O)=O)CCC4)=O.CC(O)=O | ||
| 分子式 | C40H50N8O10.XC2H4O2 | 分子量 | 802.9 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2455 mL | 6.2274 mL | 12.4549 mL |
| 5 mM | 0.2491 mL | 1.2455 mL | 2.491 mL |
| 10 mM | 0.1245 mL | 0.6227 mL | 1.2455 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Detection, quantification, and identification of Dermorphin in equine plasma and urine by LC-MS/MS for doping control
Anal Bioanal Chem 2013 May;405(14):4707-17.PMID:23571464DOI:10.1007/s00216-013-6907-0.
Dermorphin is a unique opioid peptide that is 30-40 times more potent than morphine. It was misused and went undetected in horse racing until 2011 when intelligence obtained from a few North American race tracks suggested its use. To prevent such misuse, a reliable analytical method became necessary for detection and identification of Dermorphin in post-race horse samples. This paper describes the first liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for such a purpose. Equine plasma and urine samples were pre-treated with ethylenediamine tetra-acetic acid and urea prior to solid-phase extraction (SPE) on Oasis MCX cartridges. Resulting eluates were dried under vacuum and analyzed by LC-MS/MS for Dermorphin. The matrix effect, SPE efficiency, intra-day and inter-day accuracy and precision, and stability of the analyte were assessed. The limit of detection was 10 pg/mL in plasma and 20 pg/mL in urine, and the limit of confirmation was 20 pg/mL in plasma and 50 pg/mL in urine. Dermorphin in plasma is stable at ambient temperature, but its diastereomer is unstable. With isotopically labeled Dermorphin as an internal standard, the quantification range was 20-10,000 pg/mL in plasma and 50-20,000 pg/mL in urine. The intra-day and inter-day accuracy was from 91 % to 100 % for the low, intermediate, and high concentrations. The intra-day and inter-day coefficients of variation were less than 12 %. The method differentiates Dermorphin from its diastereomer. This method is very specific for identification of Dermorphin in equine plasma and urine, as assessed by BLAST search and targeted SEQUEST search, and by MS/MS spectrum library search. The method has been successfully applied to analysis of samples collected following Dermorphin administration to research horses and of official post-race samples.
Dermorphin decreases plasma LH levels in human: evidence for a modulatory role of gonadal steroids
Peptides 1985 Sep-Oct;6(5):869-72.PMID:3936026DOI:10.1016/0196-9781(85)90317-1.
The purpose of this study was to evaluate the effects of Dermorphin, a new synthetic powerful opiate-like heptapeptide, on plasma luteinizing hormone (LH) and follicle stimulating hormone (FSH) levels in fertile and postmenopausal women. In fertile subjects, Dermorphin (5.5 micrograms/kg min for 30 min) decreases plasma LH (p less than 0.01 vs. baseline and placebo values), but not plasma FSH. The area under the curve during Dermorphin infusion was significantly lower than during placebo infusion (p less than 0.01). Pretreatment with the opioid receptor antagonist naloxone, blocked the decrease of plasma LH levels. In postmenopausal women not subjected to any treatment, Dermorphin infusion did not significantly modify plasma LH and FSH levels. On the contrary, its administration to postmenopausal subjects treated with conjugated estrogens and medroxyprogesterone acetate significantly decreased plasma LH levels (p less than 0.01, vs. baseline, placebo and area under the curve). Considering the modulatory role exerted by ovarian steroids on the activity of such receptors, these data also indicate that opioid systems play a very important part in the hypothalamus-pituitary-ovarian axis.
Antinociceptive effect of D-Lys(2), Dab(4)N-(ureidoethyl)amide, a new cyclic 1-4 Dermorphin/deltorphin analog
Pharmacol Rep 2014 Aug;66(4):600-5.PMID:24948060DOI:10.1016/j.pharep.2014.01.007.
Background: A preliminary evaluation of antinociceptive activity of a new cyclic Dermorphin/deltorphin tetrapeptide analog restricted via a urea bridge and containing C-terminal ureidoethylamid {[H-Tyr-d-Lys(&(1))-Phe-Dab(&(2))-CH2CH2NHCONH2][&(1)CO&(2)]} (cUP-1) revealed a significant and long-lasting increase of pain threshold to thermal stimulation after systemic application. The current studies were aimed at further evaluation of cUP-1 activity in animal models of somatic and visceral pain. The influence of cUP-1 on motor functions was also investigated. Methods: The influence of cUP-1 (0.5-2mgkg(-1), iv) on nociceptive threshold to mechanical pressure and analgesic efficacy in formalin and acetic acid-induced writhing tests were estimated. The antinociceptive effect of cUP-1 was compared to that of morphine (MF). The influence of cUP-1 (1, 4 and 8mgkg(-1), iv) on locomotor activity, motor coordination and muscle strength was estimated using open field and rota-rod tests and a grip strength measurement. Results: Administration of cUP-1 in doses of 1 and 2mgkg(-1) elicited a significant increase of nociceptive threshold to mechanical pressure. MF applied in the same doses induced an antinociceptive effect only at the higher dose (2mgkg(-1)). There were no marked differences between the effect of cUP-1 and MF at each dose, at relative time points. In the writhing test and both phases of the formalin test, cUP-1 showed a significant, dose-dependent antinociceptive effect which did not markedly differ from that of MF. cUP-1 did not significantly affect motor functions of mice. Conclusions: Systemic application of cUP-1 elicited a dose-dependent antinociceptive effect. The analgesic efficacy of cUP-1 on mechanical nociception, visceral and formalin-induced pain was comparable to that of MF. cUP-1 did not impair motor functions of mice.
Radioimmunoassay of dermorphin-like peptides in mammalian and non-mammalian tissues
Peptides 1981;2 Suppl 2:45-9.PMID:6979743DOI:10.1016/0196-9781(81)90009-7.
A selective RIA for D-Ala2-Dermorphin (Der), a natural peptide extracted from amphibian skin, has been developed using an antibody raised in rabbits against Der which has been coupled to BSA through its phenolic hydroxyl groups of tyrosine residues with 2,4-Dichloro-6-methoxy-1,3,5-triazine. The cross-reactivity of this antibody with Dermorphin analogs, C- and N-terminal fragments of Dermorphin molecule, some opioid and gastrointestinal peptides was tested. Der-like immunoreactivity has been identified in tissue extracts of rats, frog and cephalopoda. Der-like peptides were purified by passing methanol extracts of the tissues through a Sephadex G25 column (16 x 100 cm) eluted with 0.1 M acetic acid at 4 degrees C. Der-like immunoreactivity from neural tissue of Dosidicus gigas, Eledone moscata, and rat brain showed a good agreement with an authentic sample of synthetic Dermorphin.
[Comparative analysis of analgesic activities of Dermorphin, [DPro6]-dermorphin, and their C-terminal tripeptides]
Izv Akad Nauk Ser Biol 2007 Sep-Oct;(5):577-82.PMID:18038625doi
Analgesic activities of Dermorphin (DM), [DPro6]-DM, and their C-terminal tripeptides were comparatively studied. Analgesic activity was evaluated in tail flick, hot plate, tail pinch, formalin, and acetic acid writhing tests describing different levels of organization of pain sensitivity. Intraperitoneal administration of the peptides decreased the pain threshold in all these tests. The C-terminal tripeptides DM(5-7) and [DPro6]-DM(5-7) demonstrated analgesics activity comparable or sometimes higher than that of the full-length molecules. The effect of DM, [DPro6]-DM, and C-terminals fragments DM(5-7) and [DPro6]-DM(5-7) decreased after co-administration with naloxone, which points to the opioid nature of analgesic activity of the peptides.