Application of estradiol and derivatives thereof in preparation of medicines for preventing and treating oxytocin receptor related diseases

A derivative, the technology of estradiol, is applied in the field of medicine to achieve the effect of receptor sensitization, improve the effect, and improve the effect of receptor sensitization

Inactive Publication Date: 2020-12-25
骞保民
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention utilizes estradiol and its derivatives and salts of derivatives to significantly increase the level of oxytocin receptors in biological tissues, and can be applied to resolve oxytocin receptors in diseases caused by the lack of oxytocin receptors Lack of problems, and then realize the treatment of the corresponding disease. At the same time, the increase of the oxytocin receptor can re-improve the sensitivity of the corresponding tissue to oxytocin, making it respond to the original unresponsive oxytocin level, so the use of estrogen Diol and its derivatives, and salts of their derivatives can also solve the problem of oxytocin receptor desensitization in the prior art, achieve the sensitization effect of oxytocin receptors, and improve the therapeutic effect of related diseases

Method used

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  • Application of estradiol and derivatives thereof in preparation of medicines for preventing and treating oxytocin receptor related diseases
  • Application of estradiol and derivatives thereof in preparation of medicines for preventing and treating oxytocin receptor related diseases
  • Application of estradiol and derivatives thereof in preparation of medicines for preventing and treating oxytocin receptor related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Uterine smooth muscle cells in vitro experiments:

[0036] 1. Isolation and culture of uterine smooth muscle cells

[0037] Select normal full-term expectant mothers, take a small amount of uterine smooth muscle tissue during cesarean section, about 0.5cm×0.5cm×1.5cm, and immediately place it in the double-antibody solution that has added penicillin 1 000ug / mL and streptomycin 1 000ug / mL in the ice-cold D-Hanks solution. Mince the tissue repeatedly to about 1mm×1mm×1mm, suck the tissue into a centrifuge tube and let it stand. Remove the supernatant, add 3mL of digestion solution (D-Hanks solution containing 0.12% collagenase and 200ug / mL DNase), and digest in a 37°C water bath for 12-16h. Centrifuge at 1000r / min for 5min, remove the supernatant, add a little DMEM containing 10% fetal bovine serum to make cell suspension, and inoculate the culture flask. 37°C, 5% CO 2 Let the incubator stand for 1 day, change the medium once every 2 days after the cells stretch and a...

Embodiment 2

[0061] Prevention experiment of postpartum hemorrhage

[0062] 1. The parturients were randomly divided into 3 groups, including:

[0063] (1) Oral prevention group: 100 cases (age: 29.2±3.2 years old; gestational age: 37.6±1.3 weeks): among them, 46 cases of primiparous women, 54 cases of multiparas; mode of delivery: 62 cases of vaginal delivery, 38 cases of cesarean section ;

[0064] (2) 98 patients in the intravenous injection prevention group (age: 30.1±2.8 years old; gestational age: 37.8±1.4 weeks); among them, 42 cases of primiparous women and 58 cases of multiparas; mode of delivery: 61 cases of transvaginal, 37 cases of cesarean section example;

[0065] (3) 100 cases in the control group (age 28.6±2.3 years old; gestational week 37.9±1.6 weeks); among them, 51 cases of primiparous women and 49 cases of multiparous women; delivery methods: 56 cases of vaginal delivery and 44 cases of cesarean section;

[0066] The age, gestational week, parity, and mode of delive...

Embodiment 3

[0070] Experimental treatment of postpartum hemorrhage

[0071] 1. Divide women with postpartum hemorrhage into 6 groups randomly, including:

[0072] (1) 50 cases in the oral treatment group (age: 32.1±3.6 years old; gestational age: 38.2±2.3 weeks; prenatal weight: 68.2±17.8 kg); among them, 21 cases of primipara and 29 cases of multipara; mode of delivery: multipara 22 cases of vagina, 28 cases of cesarean section;

[0073] (2) 52 cases in the intravenous injection treatment group (age: 32.1±3.6 years old; gestational age: 38.2±2.4 weeks; prenatal weight: 65.7±13.4 kg); among them, 23 cases of primiparous women and 29 cases of multiparas; mode of delivery: 22 cases of transvaginal delivery, 30 cases of cesarean section;

[0074] (3) A46 cases of combined drug control group (age: 31.8±3.3 years old; gestational age: 37.6±2.8 weeks; prenatal weight: 68.7±14.1 kg); among them, 21 cases of primipara and 25 cases of multipara; mode of delivery: 24 cases of transvaginal delive...

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Abstract

The invention discloses an application of estradiol and the derivatives thereof in preparation of the medicines for preventing and treating oxytocin receptor related diseases. The estradiol, the derivatives of the estradiol and salts of the derivatives can remarkably improve the level of oxytocin receptors in biological tissues, can be applied to the diseases caused by oxytocin receptor deficiencyto solve the problem of oxytocin receptor deficiency, and realize treatment of corresponding diseases; and meanwhile, the sensitivity of the tissues corresponding to the oxytocin receptors to oxytocin can be improved again, so that the oxytocin receptors respond to the original non-reactive oxytocin level again, namely the problem of oxytocin receptor desensitization in the prior art can be solved, and the treatment effect of related diseases is improved. The estradiol and the derivatives thereof not only can realize treatment, but also can realize the prevention effect of the diseases on thebasis of the same mechanism. For example, the inventor applies the estradiol and the derivatives of the estradiol and the salts of the derivatives of the estradiol to postpartum hemorrhage diseases,so that postpartum hemorrhage can be prevented or remarkably improved, and life risks and sequelae caused by postpartum hemorrhage to parturient pregnant women can be effectively avoided.

Description

technical field [0001] The invention relates to the field of medicine, and more specifically relates to the application of estradiol and its derivatives in the preparation of drugs for preventing and treating oxytocin receptor-related diseases. Background technique [0002] Oxytocin receptor (OTR) is a member of the G-protein coupled receptor (GPCR) superfamily, and is the receptor for oxytocin (OT) to exert specific physiological effects. body. OTR is distributed in both peripheral tissues and the central nervous system. OTR on different tissue cells receives and combines with OT to play a role through a variety of signal transduction pathways. [0003] The cooperation between oxytocin receptor and oxytocin plays an important role in various physiological processes. For example, in the process of childbirth, the level of oxytocin receptor and oxytocin in human myometrium is higher than that of non-pregnancy period, and the combination to promote The contraction of uterine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/567A61K31/565A61P15/00A61P7/04
CPCA61K31/565A61K31/567A61P7/04A61P15/00
Inventor 周骞周沫骞保民项毅帆
Owner 骞保民
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