Analytical process and agents for the detection of esterolytic and/or
proteolytic enzymes
    11.
    发明授权
    Analytical process and agents for the detection of esterolytic and/or proteolytic enzymes 失效
    用于检测酯水解和/或蛋白水解酶的分析方法和试剂

    公开(公告)号:US4755462A

    公开(公告)日:1988-07-05

    申请号:US710625

    申请日:1985-03-11

    Applicant: Eugen Schnabel

    Inventor: Eugen Schnabel

    Abstract: Agent for the detection of esterolytic and/or proteolytic enzymes, containing (a) an amino acid ester or peptide ester of a phenol, as the chromogenic enzyme substrate, and (b) a substance which accelerates the enzymatic cleavage of the amino acid ester or peptide ester bond of component (a), characterized in that it contains a polyamino acid with a molecular weight of between 1,000 and 2,000,000 as the accelerating substance.

    Abstract translation: 用于检测含有(a)苯酚的氨基酸酯或肽酯作为显色酶底物的酯水解和/或蛋白水解酶的试剂,和(b)加速氨基酸酯的酶裂解的物质或 组分(a)的肽酯键,其特征在于其含有分子量为1,000至2,000,000的聚氨基酸作为促进物质。

    Peptide derivatives and use thereof as substrates for quantitatively
assaying enzymes
    13.
    发明授权
    Peptide derivatives and use thereof as substrates for quantitatively assaying enzymes 失效
    肽衍生物及其用作定量测定酶的底物

    公开(公告)号:US4629695A

    公开(公告)日:1986-12-16

    申请号:US616257

    申请日:1984-06-01

    Inventor: Lars G. Svendsen

    Abstract: Peptide derivatives of formula ##STR1## wherein R.sup.1 represents a substituted amino group which is capable of being split off enzymatically with formation of a colored or fluorescent compound R.sup.1 -H. The said peptide derivatives are used for quantitatively assaying the enzyme C.sub.1 -esterase. The assaying is carried out by reacting a medium which contains C.sub.1 -esterase or in which the latter is formed or consumed with a peptide derivative as defined above and measuring photometrically, spectrophotometrically, fluorescence-spectrophotometrically or electrochemically the quantity of split product R.sup.1 -H released per time unit by the catalytic hydrolytic action of the said enzyme on the peptide derivative.

    Abstract translation: 其中R1代表能够通过形成有色或荧光化合物R1-H酶分解的取代氨基的肽衍生物。 所述肽衍生物用于定量测定酶C1-酯酶。 测定是通过使包含C1-酯酶的培养基或后者被形成或消耗的培养基与如上所定义的肽衍生物反应进行的,并用光度法,分光光度法,荧光分光光度法或电化学方法测量裂解产物R1-H的释放量 每个时间单位通过所述酶对肽衍生物的催化水解作用。

    Radiolabelled substrates for assaying mammalian enzymes
    14.
    发明授权
    Radiolabelled substrates for assaying mammalian enzymes 失效
    用于测定哺乳动物酶的放射性标记底物

    公开(公告)号:US4563305A

    公开(公告)日:1986-01-07

    申请号:US222980

    申请日:1981-01-07

    Abstract: Compounds which are substrates for mammalian enzymes, especially proteolytic and peptidase enzymes, are disclosed. These compounds, in general, have the general formula X-T, W-Y or X-(Pep)-Y, wherein X is a radiolabelled benzoyl or hydroxyphenylpropanoyl group, T is the --NH residue of a known chromogenic or fluorogenic substrate comprising at least one amino acid group which may be substituted with other organic groups, Y is a radiolabelled benzylamine group, W is the ##STR1## residue of a known chromogenic or fluorogenic substrate comprising at least one amino acid group which may be substituted with other organic groups, and (Pep) is a difunctional or polyfunctional residue from a known chromogenic or fluorogenic substrate comprising at least two amino acid groups in peptide linkage, which residue may be substituted with other organic groups. These substrates exhibit many advantages over the chromogenic and fluorogenic analogs, including greater sensitivity, surprising and unpredictable affinity and specificity, and the like.

    Abstract translation: 公开了作为哺乳动物酶底物,特别是蛋白水解酶和肽酶的化合物。 这些化合物通常具有通式XT,WY或X-(Pep)-Y,其中X是放射性标记的苯甲酰基或羟基苯基丙酰基,T是已知的显色或荧光底物的-NH残基,其包含至少一个氨基 可以被其它有机基取代的酸基,Y是放射性标记的苄胺基,W是包含至少一个可被其它有机基团取代的氨基酸基团的已知显色或荧光底物的“ Pep)是来自已知显色或荧光底物的双官能或多官能残基,其包含肽键中的至少两个氨基酸基团,该残基可被其它有机基团取代。 这些底物相对于显色和荧光类似物具有许多优点,包括更高的灵敏度,惊人的和不可预测的亲和性和特异性等。

    Glycine.sup.8 -D-arginine.sup.24 calcitonin
    17.
    发明授权
    Glycine.sup.8 -D-arginine.sup.24 calcitonin 失效
    甘氨酸8-D-精氨酸24降钙素

    公开(公告)号:US4414149A

    公开(公告)日:1983-11-08

    申请号:US471982

    申请日:1983-03-04

    CPC classification number: C07K14/5855 A61K38/00 Y10S930/28

    Abstract: New peptides are disclosed which have biological activity of the same type as known calcitonins which have both a D-amino acid in position 24 instead of the natural L-amino acid and are substitution analogs of the natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.

    Abstract translation: 公开了具有与已知降钙素相同类型的生物活性的新肽,其具有位置24的D-氨基酸而不是天然L-氨基酸,并且是天然降钙素的取代类似物。 还公开了可以转化成具有这种生物活性的肽的树脂肽; 以及用于制备所述树脂肽和所述降钙素肽的方法。

    Polypeptide compositions
    18.
    发明授权
    Polypeptide compositions 失效
    多肽组合物

    公开(公告)号:US4305852A

    公开(公告)日:1981-12-15

    申请号:US198415

    申请日:1980-10-20

    Inventor: Victor M. Garsky

    CPC classification number: C07K14/662 A61K38/00 Y10S930/18 Y10S930/28

    Abstract: There are disclosed polypeptides having the formula:R-Arg-Lys-Asp-Val-D-Ala-R.sub.1whereinR is hydrogen, alkanoyl of 1-4 carbon atoms or aroyl of 6-10 carbon atoms; andR.sub.1 is amino, monoalkylamino of 1-4 carbon atoms, dialkylamino of 1-4 carbon atoms, hydroxy, alkoxy of 1-4 carbon atoms, ##STR1## the fully protected peptide-resin intermediates thereof, or pharmaceutically acceptable salts thereof. These polypeptides have the capability of inducing the differentiation of t-lymphocytes and thus are useful in a number of therapeutic areas.

    Abstract translation: 公开了具有下式的多肽:R-Arg-Lys-Asp-Val-D-Ala-R1其中R是氢,1-4个碳原子的烷酰基或6-10个碳原子的芳酰基; R1为氨基,1-4个碳原子的单烷基氨基,1-4个碳原子的二烷基氨基,羟基,1-4个碳原子的烷氧基,其完全保护的肽 - 树脂中间体或药学上 其可接受的盐。 这些多肽具有诱导t淋巴细胞分化的能力,因此可用于许多治疗领域。

    Chromogenic method of detecting endotoxins in blood
    19.
    发明授权
    Chromogenic method of detecting endotoxins in blood 失效
    检测血液中内毒素的显色法

    公开(公告)号:US4301245A

    公开(公告)日:1981-11-17

    申请号:US154360

    申请日:1980-05-29

    CPC classification number: G01N33/579 G01N33/52 Y10S930/28

    Abstract: An improved method is provided for detecting endotoxins in blood serum and/or plasma, particularly human blood fractions. The method employs king crab amebocyte lysate, preferably Limulus amebocyte lysate, in the presence of a substrate which has a selected colorimetric indicator bound to it. The indicator is capable of being split from the substrate by an enzyme which can be generated in the lysate by endotoxins in the blood. Thus, the endotoxins convert proenzyme in the lysate to the enzyme which effects the splitting off of the colorimetric indicator from the substrate. The endotoxin concentration in the blood can thus be determined colorimetrically, that concentration being proportional to the concentration of color indicator split from the substrate. The blood sample need not be extracted, as is required in prior methods, with a solvent such as chloroform to remove inhibitors therein which would interfere with a lysate gelation reaction. Heparin is utilized in the present method in a concentration sufficient to stabilize the lysate against loss of potency but insufficient to inhibit the reaction whereby endotoxin generates the described splitting enzyme from proenzyme in the lysate and the reaction of the enzyme to cause the split. The blood fraction need not be diluted with water and the lysate may be one which has been reconstituted from dry powder, if desired. The method is simple, highly effective, reproducible, inexpensive and rapid.

    Abstract translation: 提供了一种用于检测血清和/或血浆,特别是人血液级分中的内毒素的改进方法。 该方法在具有与其结合的选定的比色指示剂的底物存在下使用王蟹血小板裂解物,优选鲎变形细胞溶解产物。 指示剂能够通过可以通过血液中的内毒素在裂解物中产生的酶从底物分裂。 因此,内毒素将溶胞产物中的酶转化成酶,其从底物分解比色指示剂。 因此可以比色测定血液中的内毒素浓度,该浓度与从底物分离的颜色指示剂的浓度成比例。 如先前方法所需,血液样品不需要用溶剂如氯仿提取,以除去其中会干扰裂解物凝胶化反应的抑制剂。 肝素以本发明的方法用于足以稳定溶胞产物的效力而不失去效力,但不足以抑制反应,由此内毒素在裂解物中从酶原产生所述裂解酶和酶引起分裂的反应。 血液部分不需要用水稀释,如果需要,裂解液可以是由干粉重新构成的。 该方法简单,高效,可重现,价格低廉。

    Enkephalin analogues
    20.
    发明授权
    Enkephalin analogues 失效
    脑啡肽类似物

    公开(公告)号:US4216128A

    公开(公告)日:1980-08-05

    申请号:US54550

    申请日:1979-07-05

    Abstract: The polypeptides of the formula: ##STR1## in which R.sup.1 is hydrogen, methyl, allyl, cyclopropylmethyl, cyclobutylmethyl or Arg;R.sup.2 is hydrogen or methyl;R.sup.3 is hydrogen, (lower) alkylthio or a repeating unit of the depicted polypeptide forming a dimeric dithio ether;R.sup.4 is hydrogen or methyl;X is D-Ser, D-Thr, D-Asn, D-Asp, D-Gln, D-Glu, D-His, D-Lys, D-Arg, D-Leu and D-Met;and R.sup.5 represents hydroxyl, (lower) alkyl ester amide or (lower)alkyl amide of the 1-carboxyl group of the C-terminal amino acid or a --CH.sub.2 OH group replacing said 1-carboxyl group,or a pharmaceutically acceptable salt thereof, exert an analgesic effect in warm-blooded animals.

    Abstract translation: 下式的多肽:其中R 1是氢,甲基,烯丙基,环丙基甲基,环丁基甲基或者Arg; R2是氢或甲基; R3是氢,(低级)烷硫基或所述多肽的重复单元,形成二聚二硫醚; R4是氢或甲基; X是D-Ser,D-Thr,D-Asn,D-Asp,D-Gln,D-Glu,D-His,D-Lys,D-Arg,D-Leu和D-Met; R5表示羟基,取代所述1-羧基的C-末端氨基酸的1-羧基的(低级)烷基酯酰胺或(低级)烷基酰胺或其药学上可接受的盐,发挥 温血动物的镇痛作用。

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