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Buserelin Acetate Sale

目录号 : GC34099

Buserelin(INN)Acetate是一个GnRH的激动剂。

Buserelin Acetate Chemical Structure

Cas No.:68630-75-1

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产品描述

Buserelin (INN) Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).target: GnRHIn vivo: Buserelin treatment reduced the number of neurons along the entire gastrointestinal tract, with increased relative numbers of CRF-immunoreactive submucosal and myenteric neurons in colon (p < 0.05 and p < 0.01, respectively).[1]Compared with controls, buserelin treatment caused loss of myenteric neurons in the ileum and colon (P<0.01), a thinner circular muscle layer in ileum (P<0.05) and longitudinal muscle layer in colon (P<0.05). Long term follow up of buserelin induced enteric neuropathy reveals reduced body weight, loss of myenteric neurons, thinning of muscle layers, and increased numbers of eosinophils and T lymphocytes in the gastrointestinal tract.[2] A marked enteric neuronal loss with modest effects on GI function is found after buserelin treatment. Increased feces fat content is suggested an early sign of dysfunction.[3]

[1]. Sand E et al. Buserelin treatment to rats causes enteric neurodegeneration with moderate effects on CRF-immunoreactive neurons and Enterobacteriaceae in colon, and in acetylcholine-mediated permeability in ileum. BMC Res Notes. 2015 Dec 28;8:824. [2]. Jnsson A et al. Long term follow up of buserelin induced enteric neuropathy in rats. Mol Med Rep. 2016 Apr;13(4):3507-13. [3]. Sand E et al. Structural and functional consequences of buserelin-induced enteric neuropathy in rat. BMC Gastroenterol. 2014 Dec 11;14:209.

Chemical Properties

Cas No. 68630-75-1 SDF
Canonical SMILES {pGlu}-His-Trp-Ser-Tyr-{d-Ser(tBu)}-Leu-Arg-Pro-NHEt
分子式 C62H90N16O15 分子量 1299.48
溶解度 Water : 50 mg/mL (38.48 mM; Need ultrasonic) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.7695 mL 3.8477 mL 7.6954 mL
5 mM 0.1539 mL 0.7695 mL 1.5391 mL
10 mM 0.077 mL 0.3848 mL 0.7695 mL
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Research Update

Effect of addition of Buserelin Acetate to the extender on motility and viability of bovine spermatozoa

Anim Biotechnol 2019 Apr;30(2):99-104.PMID:30595097DOI:10.1080/10495398.2018.1521821.

The present study was aimed to determine the effect of GnRH analog (Buserelin Acetate) on the quality of bovine spermatozoa stored at 16° C for 24 h. Semen collected in the summer season from June to September from healthy Polish Holstein-Friesian bulls. Ejaculates were centrifuged, divided and diluted to the final concentration of 240 × 106 spermatozoa/mL using animal protein-free commercial BIOXcell® extender (IMV Technologies, L'aigle, France) (Control) or with BIOXcell® extender supplemented with Buserelin Acetate and stored 0, 8 and 24 h. Sperm motility parameters analysis was performed using a computer-assisted sperm analysis (CASA) system. The viability of spermatozoa was performed using flow cytometer. The addition of Buserelin Acetate to BIOXcell® extender did positively affect the total motility (was higher in the observed samples with the addition of 2 µg/mL and 4 µg/mL than in the control group), progressive motile (forward progressing sperm was significantly increased (p < 0.05) over the control group at the 0 h and 8 h of incubation following the supplementation of 2, 4 and 8 μg/mL Buserelin Acetate) and viability of spermatozoa (the number of live spermatozoa was significantly higher (p < 0.05) in 2 µg/mL and 4 µg/mL samples with Buserelin Acetate at 8th hour of incubation and in sample with 4 µg/mL at 24th hour of incubation compared to the control group). We recommend adding 4 µg/mL to the extender to improve the quality of bovine semen.

Efficacy and safety of intranasal Buserelin Acetate in the treatment of endometriosis: a review of six clinical trials and comparison with danazol

Prog Clin Biol Res 1990;323:357-82.PMID:2106146doi

The efficacy and safety of Buserelin Acetate in the treatment of endometriosis was studied in 4 open non-comparative trials and 2 open randomized comparative trials with danazol. 444 women were enrolled in the buserelin group and 89 in the danazol group. Treatment was for 6-10 months using 900-1200/micrograms intranasal buserelin/day and 400-800/micrograms oral danazol/day; patients were followed up for 6-8 months. Endometriotic lesions improved or disappeared in most women; pain (dysmenorrhoea, dyspareunia and pelvic pain) subsided rapidly. Most women had no, or alleviated, symptoms throughout follow-up, although ovarian function resumed promptly. Nearly a quarter of infertile women with a desire for children became pregnant. No significant differences between treatments emerged. Buserelin treatment was characterized by menopausal-like symptoms in most women, as well as by headache and nausea. Danazol treatment, which also gave rise to these effects, was accompanied by weight gain, myalgia and acne in a considerable proportion of women, as well as other anabolic and androgenic side effects. Buserelin would thus appear to be a safe and effective alternative to the standard therapy, danazol, in the treatment of endometriosis.

Single injection of triptorelin or Buserelin Acetate in saline solution induces ovulation in mares the same as a single injection of hCG

Reprod Domest Anim 2020 Mar;55(3):374-383.PMID:31930759DOI:10.1111/rda.13632.

The aim of this study was to assess the efficacy of different doses of Buserelin Acetate and another GnRH agonist, triptorelin acetate, in saline solution in a single subcutaneous injection, to induce ovulation of growing pre-ovulatory follicle in mare and compare it with the classical treatment of a single injection of hCG. The study is split into 3 experiments over different breeding seasons in the same stud with a random distribution of treatment. The first one was to compare the injection of 6 mg of buserelin with 1,500 IU of hCG; the second one consisted of comparing different doses of buserelin (6 mg and 3 mg); and the third one compared three different doses of buserelin (3, 2 and 1 mg), 0.1 mg of triptorelin with 1,500 IU of hCG as a control group. The results of all experiments showed the same efficacy between all treatments with mares ovulating between 24 and 48 hr after injection: experiment 1: hCG (78% n = 41) and buserelin 6 mg (90% n = 50); experiment 2: buserelin 6 mg (78,1% n = 192) and buserelin 3 mg (78% n = 341); and experiment 3: hCG (87% n = 106), buserelin 3 mg (84,7% n = 137), buserelin 2 mg (82,7% n = 104), buserelin 1 mg (87% n = 54) and triptorelin 0.1 mg (84,7% n = 72). In conclusion, this study contributes to erasing the dogma that has been established since 1975 that a single injection in solution without any long-acting excipient of a GnRH agonist cannot induce ovulation in the mare. This study also shows that a injection of 0.1 mg of triptorelin in solution is a good alternative for ovulation induction and is comparable to small doses of Buserelin Acetate in solution (1 mg) and 1,500 IU of the gold standard trigger hCG, mainly in countries where human formulation of buserelin is not available.

Tambaqui females (Colossoma macropomum) spawn after hormonal induction with Buserelin Acetate

Anim Reprod Sci 2020 Oct;221:106594.PMID:32931986DOI:10.1016/j.anireprosci.2020.106594.

The aim of this study was to evaluate induced reproduction in tambaqui females using Buserelin Acetate as compared with the traditional treatment regimen with carp pituitary extract (CPE). Reproductive traits of females with a body weight (BW) of 8.47 ± 1.52 kg were evaluated in ten females treated with Buserelin Acetate at the dose of 0.5 mL/kg BW, in a single application, and in ten females treated with CPE at the dose of 5.5 mg/kg BW, in two applications (10 % and 90 %, with a 12-h interval between applications). Spawning rate did not differ between the females treated with Buserelin Acetate (40 %) and CPE (40 %). Weight, fertilization rate and hatching rate did not differ between the two treatment groups. Degree-hours (determined as the average temperature multiplied by time, in hours, for spawning after the treatment with the second dose of CPE and after the single treatment with Buserelin Acetate) for spawning and number of oocytes per gram of gametes collected were greater (P < 0.05) in the females treated with Buserelin Acetate than in the females treated with CPE. Production index, absolute fecundity and relative fecundity were greater (P < 0.05) in the females treated with CPE. The hormone Buserelin Acetate promotes reproduction in tambaqui females with there being a similar spawning rate and oocyte quality, however, lesser production indices and fecundity than when there is the conventional treatment regimen imposed with carp pituitary extract.

A prospective randomized comparison of routine Buserelin Acetate and a decreasing dosage of nafarelin acetate with a low-dose gonadotropin-releasing hormone agonist protocol for in vitro fertilization and intracytoplasmic sperm injection

Fertil Steril 2001 Sep;76(3):532-7.PMID:11532477DOI:10.1016/s0015-0282(01)01977-x.

Objective: To compare the efficacy of a draw-back nafarelin acetate protocol with routine Buserelin Acetate administration for in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI). Design: Prospective clinical study. Setting: Mie University School of Medicine, Tsu, Mie, Japan. Patient(s): One hundred sixty-nine women treated with IVF and 183 women treated with ICSI. Intervention(s): Nafarelin acetate and Buserelin Acetate in ovarian hyperstimulation in IVF and ICSI were administered. Main outcome measure(s): The concentrations of estradiol (E(2)), FSH, LH, gonadotropin dosages; the number of oocytes retrieved, oocytes fertilized, and embryos; and pregnancy rates. Result(s): A prospective study was conducted with 44 cycles for 34 couples with nafarelin acetate (group 1) and 47 cycles for 40 couples with Buserelin Acetate (group 2) with a long IVF protocol; 68 cycles for 46 couples with nafarelin acetate (group 3) and 56 cycles for 39 couples with Buserelin Acetate (group 4) with a short IVF protocol; 39 cycles for 32 couples with nafarelin acetate (group 5) and 50 cycles for 30 couples with Buserelin Acetate (group 6) with a long ICSI protocol; and 87 cycles for 60 couples with nafarelin acetate (group 7) and 81 cycles for 61 couples with Buserelin Acetate (group 8) with a short ICSI protocol. Patients were randomized to receive either full-dose nafarelin acetate (200 microg b.i.d.) treatment for 7 days followed by half-dose nafarelin acetate (200 microg daily) or Buserelin Acetate (300 microg t.i.d.). There were no statistically significant differences in baseline concentrations of E(2) and FSH, concentrations of E(2), P4, FSH, LH on hCG administration, gonadotropin dosage, the number of oocytes retrieved and embryos transferred, or pregnancy rates between groups 1 and 2, groups 3 and 4, groups 5 and 6, and groups 7 and 8. Conclusion(s): Full-dose nafarelin acetate treatment for 7 days followed by half-dose nafarelin acetate ("draw-back" protocol) is an effective new protocol for IVF and ICSI.