127317-03-7
127317-03-7 結(jié)構(gòu)式
基本信息
垂體后葉粉
神經(jīng)垂體素
垂體腺苷酸環(huán)化酶激活肽-27
人,羊,大鼠PACAP (1-27)肽
M-PACAP
PACAP-27
PACAP 1-27
PACAP-27 (human
PACAP (1-27) AMIDE
Human PACAP-(1-27)
PACAP 27 AMIDE, OVINE
powdered posterior pitultary
PACAP-27 (HUMAN, OVINE, RAT)
物理化學(xué)性質(zhì)
有興奮子宮、促進(jìn)乳汁排出作用，縮宮素劑量大時(shí)可使血管擴(kuò)張，但升壓素劑量大時(shí)可收縮血管，還有利尿作用。
制備方法
丙酮、乙醚處理是為了除去低分子物質(zhì)和脂類，保證澄明度。
豬神經(jīng)垂體[P2O5]→粗后葉粉[丙酮、乙醚]→[25℃, 4h]垂體后葉粉
垂體后葉粉的精制 將垂體后葉粉加入0.25%的乙酸分別提取兩次，第1次加入5倍量，第2次加入2倍量，各于50℃攪拌提取15min，過(guò)濾。兩次提取完畢，合并濾液，將濾液迅速加熱至100℃，保持15min，趁熱加入0.5%三氯叔丁醇(體積比為1:1，必要時(shí)加活性炭處理)，速冷至30℃以下，冷藏過(guò)夜后，反復(fù)過(guò)濾至澄清。乙酸浸出液含無(wú)效蛋白質(zhì)與自解酶，加熱可使其凝固和破壞(注意：縮宮素的催產(chǎn)效價(jià)在堿性或強(qiáng)酸下易失效。在弱酸如pH3-4時(shí)穩(wěn)定，且100℃流通蒸氣滅菌30min或熱壓滅菌亦穩(wěn)定)。
垂體后葉粉[0.25%乙酸]→[50℃, 15min]濾液[0.5%三氯叔丁醇]→[冷藏， 過(guò)濾]精制后葉粉液
后葉粉注射液制劑的制備 測(cè)定后葉粉液的效價(jià)后，加注射用水使其達(dá)到10.5 U/ml，并加適量三氯叔丁醇達(dá)到0.5%，用冰醋酸調(diào)pH為3.5，用垂熔漏斗過(guò)濾，灌封，100℃流通蒸氣滅菌半小時(shí)，即得垂體后葉注射液成品。
后葉粉液[測(cè)效價(jià)]→[pH3.5]后葉注射液[過(guò)濾，滅菌]→后葉注射液成品。
應(yīng)用領(lǐng)域
常見(jiàn)問(wèn)題列表
神經(jīng)垂體素可用于血液透析慢性低血壓患者中的應(yīng)用及護(hù)理；治療肺結(jié)核咯血；治療食管靜脈曲張破裂出血等。
IC50: 3 nM (rat PAC1), 2 nM (rat VPAC1), 5 nM (human VPAC2)
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.
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.