Ornipressin (POR-8)
(Synonyms: 鸟氨酸加压素; POR-8) 目录号 : GC32460
Ornipressin (POR-8) 是一种有效的血管收缩剂、止血剂和肾脏剂。
Cas No.:3397-23-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ornipressin is a potent vasoconstrictor, hemostatic and renal agent.
[1]. Fruhstorfer H, et al. Dose-response relation of ornipressin with regard to vasoconstriction in human skin. Br J Anaesth. 1994 Aug;73(2):220-4. [2]. De Kock M, et al. Ornipressin (Por 8): An efficient alternative to counteract hypotension during combined general/epidural anesthesia. Anesth Analg. 2000 Jun;90(6):1301-7.
| Cas No. | 3397-23-7 | SDF | |
| 别名 | 鸟氨酸加压素; POR-8 | ||
| Canonical SMILES | Cys-Tyr-Phe-Gln-Asn-Cys-Pro-{Orn}-Gly-NH2 (Disulfide bridge: Cys1-Cys6) | ||
| 分子式 | C45H63N13O12S2 | 分子量 | 1042.19 |
| 溶解度 | Water : ≥ 100 mg/mL (95.95 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9595 mL | 4.7976 mL | 9.5952 mL |
| 5 mM | 0.1919 mL | 0.9595 mL | 1.919 mL |
| 10 mM | 0.096 mL | 0.4798 mL | 0.9595 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。
An Integrated Review of the Hepatorenal Syndrome
Ann Hepatol 2021 May-Jun;22:100236.PMID:32846202DOI:10.1016/j.aohep.2020.07.008.
Among the complications of cirrhosis, hepatorenal syndrome (HRS) is characterized by having the worst survival rate. HRS is a disorder that involves the deterioration of kidney function caused primarily by a systemic circulatory dysfunction, but in recent years, systemic inflammation and cirrhotic cardiomyopathy have been discovered to also play an important role. The diagnosis of HRS requires to meet the new International Club of Ascites-Acute Kidney Injury (ICA-AKI) and Hepatorenal Syndrome-Acute Kidney Injury (HRS-AKI) criteria after ruling out other causes of kidney injury. At the time of diagnosis, it is important to start the medical treatment as soon as possible where three types of vasoconstrictors have been recognized: vasopressin analogs (Ornipressin and terlipressin), alpha-adrenergic agonists (norepinephrine and midodrine) and somatostatin analogues (octreotide); all should be combined with albumin infusion. Among them, terlipressin and albumin are the first lines of treatment in most cases, although terlipressin should be monitor closely due to its adverse events. The best treatment of choice is a liver transplant, because it is the only definitive treatment for this disease.
Ornipressin (Por 8): An efficient alternative to counteract hypotension during combined general/epidural anesthesia
Anesth Analg 2000 Jun;90(6):1301-7.PMID:10825311DOI:10.1097/00000539-200006000-00008.
We sought to evaluate the efficacy and side effect profile of a small dose of Ornipressin, a vasopressin agonist specific for the V1 receptor, administered to reverse the hypotension associated with combined general/epidural anesthesia. A total of 60 patients undergoing intestinal surgery were studied. After the induction of anesthesia, 7-8 mL of bupivacaine 0.5% with 2 microg/kg clonidine and 0.05 microg/kg sufentanil after an infusion of 5 mL of bupivacaine 0.06% with 0.5 microg x kg(-1) x h(-1) clonidine and 0.1 microg/h of sufentanil were administered by an epidural catheter placed at T7-8 vertebral interspace. When 20% reduction of baseline arterial blood pressure developed, patients were randomly assigned to receive, in a double-blinded design, dopamine started at 2 microg x kg(-1) x min(-1), norepinephrine started at 0.04 microg x kg(-1) x min(-1), or Ornipressin started at 1 IU/h. Fifteen patients presenting without hypotension were used as control subjects. Beside routine monitoring, S-T segment analysis, arterial lactacidemia, and gastric tonometry were performed. Ornipressin restored arterial blood pressure after 8 +/- 2 vs 7 +/- 3 min in the norepinephrine group and 11 +/- 3 min in the dopamine group (P < 0.05). This effect was achieved with 2 IU/h of Ornipressin in most of the patients (11 of 15). Ornipressin did not induce any modification of the S-T segment; however, it significantly increased intracellular gastric PCO(2) (P < 0.05), indicating splanchnic vasoconstriction. Implications: In the population studied, small-dose Ornipressin was effective to restore arterial blood pressure without causing major ischemic side effects.
[POR 8 (Ornipressin). Local vasoconstrictive effect and hemodynamic activity during surgery in ENT clinics]
Anaesthesist 1984 Mar;33(3):149-53.PMID:6721128doi
POR 8 (Ornipressin) at a concentration of 5 IU in 10 ml of 1% lidocaine was used as a local vasoconstrictor in 262 ENT operations. Anaesthesia was carried out with either halothane or enflurane, or with diazepam and fentanyl. The doses of POR 8 lay between 2.7 IU and 3.5 IU. Under inhalational anaesthesia there was a good vasoconstriction in 85% to 90%, and anaesthesia with diazepam-fentanyl in 60% to 83% of cases, depending on the site of operation. There should be a 10-20 minute interval between infiltration and the beginning of surgery. Under inhalational anaesthesia the systolic blood pressure fell by 10% after infiltration of POR 8, when the diastolic blood pressure rose by 6%. During diazepam-fentanyl anaesthesia the systolic blood pressure increased by 23%, the diastolic by 27%. POR 8 was not found to have an antidiuretic effect. There was no difference between the osmolality, sodium and potassium levels of 30 patients measured before infiltration and 24 hours later. Because of the minimal side effects of POR 8 on the cardiovascular system during inhalational anaesthesia we recommend the use of these substance as a local vasoconstrictor instead of epinephrine.
[Ornipressin (POR 8)--effect on coronary blood circulation and the peripheral circulation. An animal experimental study]
Anaesthesist 1993 Sep;42(9):597-604.PMID:8214531doi
Ornipressin (POR 8), referred to below as OR, is a synthetic derivative of natural vasopressin. It was introduced into clinical practice to replace epinephrine as a local vasoconstrictor because OR was presumed to produce fewer undesirable side-effects. However, mayor cardiovascular complications following local infiltration of OR have been reported in recent time. Beside increased blood pressure and changes in heart rate, there is evidence that the systemic effects of OR include a distinct vasopressor activity on coronary arteries. This study was planned to investigate the effects of OR in haemodynamics and the coronary vascular system. METHODS. The effects of OR on systemic haemodynamics and coronary circulation were studied in nine anaesthetized closed-chest mongrel dogs. Anaesthesia was administered using N2O/O2 (FiO2:0.33) and enflurane (1.0 vol% endtidal). Saline-filled catheters were used to measure intravascular pressures. Left ventricular pressure change (dP/dt) was monitored with a tip catheter manometer. Cardiac output (CO) was determined using thermodilution and coronary sinus blood flow, using a Pitot catheter. Recording of baseline values was followed by bolus injection of OR (0.03 U/kg) and changes in haemodynamics were measured for 90 min at fixed time intervals. Statistical analysis was performed by analysis of variance for repeated measures. A value of P < or = 0.05 was considered to indicate statistical significance. RESULTS. Significant maximum changes occurred within 3-5 min after administration of OR. Systolic and diastolic arterial pressures increased by 33% and 39%, respectively. With only minor changes in heart rate, cardiac output markedly decreased by 44% and total peripheral resistance increased by 159%. Impaired pump function of the left ventricle became obvious by a decrease in maximum dP/dt, a decrease in ejection fraction by 35%, and a concomitant sharp increase in left ventricular enddiastolic pressure by 68% and in endosystolic volume by 41%. At the same time, OR produced a marked impairment of coronary perfusion. Myocardial blood flow fell by 32%, while coronary vascular resistance rose by 112%. Increased myocardial oxygen demand and reduced oxygen supply resulted in very low values of coronary venous oxygen saturation (< 20%). CONCLUSIONS. Systemic effects of OR are characterized by a sharp rise in arterial blood pressure. Concomitantly a decrease of myocardial contractility leads to a compromised left ventricular function with marked increases in left ventricular enddiastolic pressure. These haemodynamic changes are associated with an imbalance of myocardial oxygen demand and delivery due to the distinct OR-induced coronary constriction. With regard to the deterioration of systemic and cardiac haemodynamics the indications and use of Ornipressin in clinical practice need to be reevaluated.
[The effect of nitroglycerin on Ornipressin (POR 8)-induced systemic and cardiovascular circulatory changes. An animal experimental study]
Anasthesiol Intensivmed Notfallmed Schmerzther 1994 Apr;29(2):108-14.PMID:8199279DOI:10.1055/s-2007-996696.
Objective: Local infiltration of Ornipressin (OR) is widely used to reduce intraoperative bleeding. However, OR can cause severe side effects including hypertension, deterioration of cardiac performance and coronary vasoconstriction. Suggestions for therapy of haemodynamic side effects of OR include the use of nitroglycerin (TNG). This experimental study was designed to investigate the influence of TNG on changes of systemic haemodynamics and coronary perfusion produced by i.v. administration of OR. Methods: 16 anesthetized closed-chest mongrel dogs were studied. Anaesthesia was administered using N2O/O2 (FiO2: 0.33) and enflurane (1Vol%ET). Saline-filled catheters were used to measure intravascular pressures. Left ventricular pressure change (dP/dt) was monitored with a cathetertip manometer. Cardiac output (CO) was determined using thermodilution, myocardial blood flow (MBF) using a Pitot catheter. Baseline values were taken (control) followed by a bolus injection of 0.03 U/kg OR i.v. The dogs were randomly assigned to two groups. Group I (Gr.I) (n = 9) received OR only and group II (Gr.II) (n = 7) was treated by infusion of 4 mg/kg.min TNG 7 to 30 min after injection of OR. Haemodynamic and cardiovascular changes were measured for 60 min at fixed time intervals. Results: In both groups (Gr.I; Gr.II) OR produced significant changes in systolic (APS) (+29%; +32%) and diastolic (APD) (+47%; +37%) aortic pressure, cardiac index (CI) (-33%; -33%), peripheral vascular resistance (TPR) (+116%); +104%), stroke volume index (SVI) (-23%; -34%), ejection fraction (EF) (-29%; -29% endsystolic volume (ESV) (+39%; +45%) and left ventricular enddiastolic pressure (LVEDP) (+50%; +66%). Myocardial blood flow (MBF) was reduced by 30% and 29% respectively and coronary vascular resistance (CVR) was increased (+97%; +84%). Coronary venous O2 saturation (SO2cor) decreased to 19% and 20% resulting in high AVDO2cor. As compared to Gr.I the administration of TNG resulted in significant decreases of APS, APD, TPR, ESV and LVEDP close to control values. However, administration of TNG did not effect MBF, CVR, SO2cor and AVDO2cor. Conclusion: Systemic haemodynamic effects of OR include hypertension due to peripheral vasoconstriction and impaired cardiac performance resulting in reduced cardiac output with low EF, high ESV and LVEDP. Concomitantly, OR produces coronary constriction with a distinct fall in MBF. Thus, myocardial oxygen balance is impaired. With TNG peripheral vascular effects of OR can be abolished but there is no effect of TNG on OR-induced reduction of coronary blood flow. Therefore, use of TNG for treatment of cardiovascular complications following the administration of OR must be considered with extreme caution.