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普罗瑞林

普罗瑞林用途

Protirelin 是一种高度保守的神经肽,发挥促甲状腺激素 (TSH) 水平的激素控制作用,及神经调节功能。

普罗瑞林名称

[ CAS 号 ]:
24305-27-9

[ 中文名 ]:
促甲状腺素释放激素

[ 英文名 ]:
TRH

[中文别名 ]:

[英文别名 ]:

thyrotropin-releasing hormone
MFCD00038640
5-Oxo-L-prolyl-L-histidyl-L-proline
TRF
TRH
<Glu-His-Pro-NH2
Thypinone
Prem
THR 2-3
L-pGlu-L-His-L-ProNH2

普罗瑞林生物活性

[ 描述 ]:

Protirelin 是一种高度保守的神经肽,发挥促甲状腺激素 (TSH) 水平的激素控制作用,及神经调节功能。

[ 相关类别 ]:

信号通路 >> 其他 >> 甲状腺激素受体

研究领域 >> 炎症/免疫

多肽产品

研究领域 >> 内分泌

[ 靶点 ]

Thyroid hormone receptor

[体内研究]

Protirelin(TRH)是一种进化上古老的神经肽,起源于原始体和后躯体之间的分化,并且可能是祖先参与控制胚后生长和繁殖[1]。在大鼠中研究了促甲状腺素释放激素(Protirelin,TRH)(一种下丘脑释放激素)对体温的影响。将剂量为1,5,10和20mg/kg的Protirelin腹膜内注射到体重为200-250g的雄性Wistar大鼠中。 Protirelin剂量依赖性地导致体温暂时升高。甲状腺切除的大鼠注射20mg/kg的Protirelin,其在假手术动物中诱导显着的体温过高,未显示出体温升高。目前的研究结果表明,甲状腺激素的释放可能参与了Protirelin的高热作用[2]。

[动物实验]

大鼠[2]对体重为200-250g的90只雄性Wistar大鼠进行研究。在第一个实验中，将50只大鼠随机分成5组。将溶于生理盐水中的4剂Protirelin，即1mg / kg，5mg / kg，10mg / kg和20mg / kg，腹膜内给予四组，并将盐水给予剩余的对照组。在用Protirelin或盐水处理之前和之后，使用电子热敏电阻在肛门内部5cm处测量直肠温度。在第二个实验中，40只大鼠在麻醉下通过硫喷妥钠进行甲状腺切除或假手术。手术后10天，通过ip和直肠温度给予甲状腺手术和假手术动物20mg / kg的Protirelin或盐水，使用与第一次实验中使用的相同的方法测量。这两个实验从1p，m到4pm进行，室温通过包括育种期的实验保持在24±1℃。对于统计分析，采用学生t检验（双尾）。

[参考文献]

[1]. Van Sinay E, et al. Evolutionarily conserved TRH neuropeptide pathway regulates growth in Caenorhabditis elegans. Proc Natl Acad Sci U S A. 2017 May 16;114(20):E4065-E4074.

[2]. Noda Y, et al. Hyperthermia induced by thyrotropin-releasing hormone (TRH, Protirelin) in the rat. Kurume Med J. 1979;26(2):107-12.

[相关活性小分子]

普罗瑞林物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
942.1±65.0 °C at 760 mmHg

[ 分子式 ]:
C₁₆H₂₂N₆O₄

[ 分子量 ]:
362.38

[ 闪点 ]:
523.6±34.3 °C

[ PSA ]:
144.49000

[ LogP ]:
-2.43

[ 外观性状 ]:
白色或近乎于白色粉末

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.617

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
H2O: 10 mg/mL, clear, colorless

普罗瑞林MSDS

详细MSDS(安全技术说明书)

普罗瑞林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TW3580000

CHEMICAL NAME :: L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-

CAS REGISTRY NUMBER :: 24305-27-9

LAST UPDATED :: 199209

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C16-H22-N6-O4

MOLECULAR WEIGHT :: 362.44

WISWESSER LINE NOTATION :: T5NTJ BVZ AVYMV- ET5MVTJ&1- BT5NJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5714 ng/kg/1M-C

TOXIC EFFECTS :: Behavioral - coma Cardiac - pulse rate Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 143,264,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5333 ng/kg/2M-C

TOXIC EFFECTS :: Behavioral - coma Vascular - BP lowering 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: 287,532,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 8 ug/kg/2M-C

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate increase, without fall in BP

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 287,532,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,727,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,727,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 514 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,727,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,727,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >20 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,727,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 921 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,727,1982 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 2 mg/kg

SEX/DURATION :: female 7-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - stillbirth

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 8,807,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 20 mg/kg

SEX/DURATION :: female 7-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 8,807,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 200 mg/kg

SEX/DURATION :: female 7-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - sex ratio

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 8,807,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 150 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 8,807,1974

普罗瑞林安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
TW3580000

普罗瑞林合成路线

详细合成路线

普罗瑞林上下游产品

普罗瑞林上游产品

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普罗瑞林文献

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