デスロレリン 化學(xué)特性,用途語(yǔ),生産方法
効能
抗悪性腫瘍薬, 性腺刺激ホルモン放出ホルモン受容體作動(dòng)薬 (獣醫(yī)薬)
説明
Deslorelin is an injectable gonadotropin releasing hormone super-agonist also known as an LHRH agonist. It stops the production of sex hormones with potential antineoplastic activity. Deslorelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Continuous, prolonged administration of goserelin in males results in pituitary GnRH receptor desensitization and inhibition of pituitary secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH), leading to a significant decline in testosterone production; in females, prolonged administration results in a decrease in estradiol production.
化學(xué)的特性
White powder, tens of times more biologically active than natural LH-RH, is synthesized by solid-phase or liquid-phase synthesis method using the corresponding protected amino acid monomers as raw materials.
使用
Induction of ovulation in estrous mares
Reproduction control in dogs
brand name
Somagard [as acetate] (Roberts Pharmaceutical).
副作用
The most common side effects include swelling, sensitivity, and redness or warmth at the injection site. Rarely reported side effects in dogs include prolonged estrus and uterine infections.
Veterinary Drugs and Treatments
Deslorelin is approved for inducing ovulation in estrual mares.
There is also interest in developing dosages and dosage forms as a
long-term, reversible contraceptive in a variety of animal species, as
a treatment for prostatic disease in male dogs, and incontinence in
ovariectomized dogs. At the time of writing, deslorelin in not available
in the USA, but is marketed in Canada.
In humans, deslorelin has been investigated for treating children
with precocious puberty, and in adults for prostate carcinoma, dysmenorrhea,
fibroids, and endometriosis.
參考文獻(xiàn)
[1] CLAIRE GROSSET. Contraceptive effect and potential side-effects of deslorelin acetate implants in rats (Rattus norvegicus): preliminary observations.[J]. Canadian journal of veterinary research = Revue canadienne de recherche veterinaire, 2012, 76 3: 209-214.
[2] STEFANO ROMAGNOLI. Chronic Use of Deslorelin in Dogs: Six Cases (2005-2022).[J]. Animals, 2023, 13 2. DOI:
10.3390/ani13020265.
[3] K E OERTER. Adult height in precocious puberty after long-term treatment with deslorelin.[J]. Journal of Clinical Endocrinology & Metabolism, 1991, 73 6: 1235-1240. DOI:
10.1210/jcem-73-6-1235.
デスロレリン 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品