Molecular Formula | C142H224N40O39S |
Molar Mass | 3147.6101 |
Density | 1.45±0.1 g/cm3(Predicted) |
Storage Condition | Room Temprature |
Physical and Chemical Properties | Chemical properties This product is made by dehydration, drying and grinding of the posterior pituitary gland of pigs, cattle, sheep and other animals. Contains oxytocin (oxytocin, oxytocin, about 20 units) and a small amount of vasopressin (vasopressin,0.5 units), both of which are very similar in structure and are nonapeptide containing disulfide bonds. The powder is light yellow or light gray amorphous powder, which is extremely smelly and almost insoluble in water. It can excite the uterus and promote milk discharge. When the dose of oxytocin is large, it can dilate blood vessels, but when the dose of vasopressin is large, it can constrict blood vessels and have diuretic effect. |
Use | Uses vasoconstrictors and antidiuretic agents. For postpartum hemostasis, promote uterine contraction and incomplete abortion; Also for the treatment of esophageal and gastric varices bleeding, diabetes insipidus. Adverse reactions and contraindications: injection for induction of labor should be cautious, should be a small dose of slow intravenous drip. Abnormal fetal position and cesarean section are contraindicated. Patients with hypertension, coronary heart disease, heart failure, pulmonary heart disease and allergic to this product are not to use. After Nausea, palpitation, palpitation, chest tightness, Abdominal Pain, and urgency, the drug was discontinued immediately. Nasal inhalants on respiratory tract inflammation, paranasal sinusitis, bronchial asthma are not used. Inhalation of too deep can cause throat tightness, shortness of breath, chest tightness, and inhalation of too much can cause Abdominal Pain. Long-term medication can cause atrophic rhinitis. |
storage conditions | −20°C |
morphology | solid |
color | white |
application
Neurohypophytin can be applied to the application and nursing of hemodialysis patients with chronic hypotension.
biological activity
PACAP (1-27), human, ovine, rat (PACAP 1-27), an N-terminal fragment of PACAP-38, is a potent PACAP receptor antagonist with IC50 values of 3 nM,2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively.
target
IC50: 3 nM (rat PAC1), 2 nM (rat VPAC1), 5 nM (human VPAC2)
in vitro study
Radioligand receptor binding assays with I-monoiodinated PACAP (1-27), human, ovine, rat confirms the presence of PAC -receptors on AR4-2J cells, since PACAP (1-27), human, ovine, rat and PACAP(1-38) equipotently displaces radioligand binding with a K d of 1-2 nM, whereas vasoactive intestinal peptide (VIP) is 1000-fold less potent. PACAP (1-27), human, ovine, rat exhibits a distinct and much higher susceptibility to VIP-amino acid substitutions. PACAP (1-27), human, ovine, rat has potency and binding affinity to stimulate IP3 and cAMP formation in AR4-2J cells.
in vivo studies
The inhibitory effect of pituitary adenylate cyclase activating polypeptide (PACAP (1-27), human, ovine, rat) on the increase in total pulmonary resistance (RL) causes either by allergen or histamine in anaesthetized, ventilated guinea-pigs is studied. PACAP (1-27), human, ovine, rat given via I .v. infusion (0.045-4.5 nmol/kg/min) dose-dependently reduces the increase in RL caused by inhaled ovalbumin and histamine. At the highest dose, PACAP (1-27), human, ovine, rat prevented the increase in RL caused by ovalbumin and histamine completely. Infusion of PACAP (1-27), human, ovine, rat and the β2-adrenoceptor agonist, salbutamol (0.045-4.5 nmol/kg/min) inhibit the increase in RL similarly, but salbutamol increases the heart rate more than PACAP (1-27), human, ovine, rat.
production method
extraction of posterior pituitary leaf powder the posterior leaf is dried in a phosphorus pentoxide vacuum dryer (water content is less than 3%), and ground into powder by a ball mill to obtain coarse posterior leaf powder. Then add 90% acetone (3-6 times), stir at 25 ℃ for 4 hours, and leave overnight. Repeat the treatment for 2-3 times, take a small amount of acetone solution and add a small amount of distilled water until it no longer becomes turbid. Then use ether (3 times the amount) to treat it once, filter, and the ether volatilizes naturally until it is dry to obtain the leaf powder.
acetone and ether treatment is to remove low molecular substances and lipids to ensure clarity.
porcine neurohypophysis [P2O5]& rarr; Crude posterior leaf powder [acetone, ether] & rarr;[25 ℃, 4h] posterior pituitary leaf powder
Refining of Posterior Pituitary Leaf Powder Add 0.25% acetic acid to extract twice, add 5 times the amount for the first time and 2 times the amount for the second time. Stir at 50 ℃ for extraction for 15min and filter. After the two extracts are completed, the filtrates are combined, the filtrates are quickly heated to 100 ℃, kept for 15min, 0.5% trichlorotert-butanol is added while it is hot (volume ratio is 1:1, activated carbon is added if necessary), quickly cooled to below 30 ℃, refrigerated overnight, and filtered repeatedly until clarified. Acetic acid leachate contains ineffective protein and self-hydrolytic enzyme, which can be solidified and destroyed by heating (note: oxytocin's oxytocin potency is easy to fail under alkaline or strong acid. It is stable in weak acid such as pH3-4, and it is also stable in flow steam sterilization at 100 ℃ for 30min or hot pressing sterilization).
posterior pituitary leaf powder [0.25% acetic acid] & rarr;[50 ℃, 15min] filtrate [0.5% trichloroterbutanol] & rarr;[refrigerated, filtered] refined posterior leaf powder
preparation of posterior leaf powder injection preparation after determining the titer of posterior leaf powder solution, add water for injection to reach 10.5 U/ml, add appropriate amount of trichlorotert-butanol to reach 0.5%, adjust the pH to 3.5 with glacial acetic acid, filter with vertical melting funnel, potting, and steam sterilization at 100 ℃ for half an hour to obtain the finished product of posterior pituitary injection.
posterior leaf powder [measured titer] & rarr;[pH3.5] posterior leaf injection [filtration, sterilization] & rarr; Finished product of posterior leaf injection.
WGK Germany | 3 |