57982-77-1

• 常用中文名：布舍瑞林
• 常用英文名：Buserelin
• CAS号：57982-77-1
• 分子式：C₆₀H₈₆N₁₆O₁₃
• 分子量：1239.424
• 相关类别： 原料药 激素及调节内分泌功能类药 促性激素类药
• 发布时间：2018-07-17 19:31:51
• 更新时间：2024-01-04 22:30:52

名称

• 中文名: 布舍瑞林
• 英文名: Buserilin,1-9-Luteinizing hormone-releasing factor (swine), 6-[O-(1,1-dimethylethyl)-D-serine]-9-(N-ethyl-L-prolinamide)
• 中文别名: 布赛来灵
• 英文别名: (d-ser(tbu)(sup6)-ea(sup10))-lhrh; d-ser-(tbu)(sup6)-lhrh-ethylamide; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-(2-methyl-2-propanyl)-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; etilamide; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-(tert-butyl)-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; BUSERELIN; (DES-GLY10,D-SER(TBU)6,PRO-NHET9)-LHRH; Receptal; BUSERELIN PH. EUR.; HOE 766A; hoe766a; 5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-(1,1-dimethylethyl)-D-seryl-L-leucyl-L-arginyl-N-ethyl-; Buserilin; HOE 766MP; Profact

物化性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₆₀H₈₆N₁₆O₁₃
• 分子量: 1239.424
• 精确质量: 1238.656006
• PSA: 438.27000
• LogP: 0.70
• 折射率: 1.671

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : OK6690000 CHEMICAL NAME : Luteinizing hormone-releasing hormone (pig), 6-(O-(1,1-dimethylethyl)-D-serine)-9-(N-ethyl- L-prolinamide)-10-deglycinamide- CAS REGISTRY NUMBER : 57982-77-1 LAST UPDATED : 199610 DATA ITEMS CITED : 23 MOLECULAR FORMULA : C60-H86-N16-O13 MOLECULAR WEIGHT : 1239.62 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TCLo - Lowest published toxic concentration ROUTE OF EXPOSURE : Inhalation SPECIES OBSERVED : Human - woman DOSE/DURATION : 1620 ug/kg/13W-I TOXIC EFFECTS : Vascular - BP elevation not characterized in autonomic section REFERENCE : BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 294,1101,1987 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Inhalation DOSE : 1080 ug/kg SEX/DURATION : female 90 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Fertility - other measures of fertility REFERENCE : LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 2,215,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Inhalation DOSE : 6960 ng/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - other effects REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 19,497,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Inhalation DOSE : 129 ug/kg SEX/DURATION : female 37 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 19,497,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Inhalation DOSE : 144 ug/kg SEX/DURATION : female 12 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 22,287,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Inhalation DOSE : 1456 ug/kg SEX/DURATION : female 26 week(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Maternal Effects - other effects Reproductive - Fertility - other measures of fertility REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 23,187,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Inhalation DOSE : 1456 ug/kg SEX/DURATION : female 26 week(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 23,187,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 8500 ug/kg SEX/DURATION : male 17 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male REFERENCE : ACENA7 Acta Endocrinologica (Copenhagen). (Periodica, Skolegade 12 E, DK-2500 Valby, Denmark) V.1- 1948- Volume(issue)/page/year: 91,601,1979 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 2200 ng/kg SEX/DURATION : female 22 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Maternal Effects - other effects Reproductive - Fertility - other measures of fertility REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 17,537,1978 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 100 ng/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 25,31,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 2800 ng/kg SEX/DURATION : female 14 day(s) pre-mating TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 21,191,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 8 ug/kg SEX/DURATION : male 8 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands REFERENCE : INJFA3 International Journal of Fertility. (Allen Press, 1041 New Hampshire, St., Lawrence, KS 66044) V.1- 1955- Volume(issue)/page/year: 25,213,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 70 ug/kg SEX/DURATION : male 28 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) REFERENCE : INJFA3 International Journal of Fertility. (Allen Press, 1041 New Hampshire, St., Lawrence, KS 66044) V.1- 1955- Volume(issue)/page/year: 25,213,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 560 ng/kg SEX/DURATION : male 28 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands REFERENCE : ACENA7 Acta Endocrinologica (Copenhagen). (Periodica, Skolegade 12 E, DK-2500 Valby, Denmark) V.1- 1948- Volume(issue)/page/year: 94,489,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 80 ug/kg SEX/DURATION : female 28-31 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 39,218,1983 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 30 ug/kg SEX/DURATION : male 60 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - impotence Reproductive - Effects on Newborn - biochemical and metabolic REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 43,187,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 15 ug/kg SEX/DURATION : male 30 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male Endocrine - androgenic REFERENCE : CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 43,187,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 840 ug/kg SEX/DURATION : male 15 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - other effects on male Endocrine - androgenic REFERENCE : ANDRDQ Andrologia. (Grosse Verlag GmbH, Kurfuerstenstr. 112-113, D-1000 Berlin 30, Fed. Rep. Ger.) V.6- 1974- Volume(issue)/page/year: 22,567,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 12500 ng/kg SEX/DURATION : male 5 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male Endocrine - aldosteronism REFERENCE : IJANDP International Journal of Andrology. (Scriptor Publisher ApS, 15 Gasvaerksvej, DK-1656 Copenhagen V, Denmark) V.1- 1978- Volume(issue)/page/year: 5,607,1982 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 16 ug/kg SEX/DURATION : female 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Maternal Effects - menstrual cycle changes or disorders REFERENCE : JANSAG Journal of Animal Science. (American Soc. of Animal Science, 309 W. Clark St., Champaign, IL 61820) V.1- 1942- Volume(issue)/page/year: 70,1904,1992 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 25 ug/kg SEX/DURATION : female 70 day(s) after conception TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Maternal Effects - other effects Endocrine - changes in luteinizing hormone REFERENCE : JOENAK Journal of Endocrinology. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1939- Volume(issue)/page/year: 141,317,1994 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 25 ug/kg SEX/DURATION : female 10-16 week(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - endocrine system REFERENCE : JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 96,785,1992 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 86400 ug/kg SEX/DURATION : male 72 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male REFERENCE : JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 80,257,1987