Leuprolide acetate (Leuprorelin) is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors.
Description
Leuprolide acetate (Leuprorelin) is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors.
IC50 Value:
Target: GnRH receptor
By interrupting the normal pulsatile stimulation of, and thus desensitizing, the GnRH receptors, it indirectly downregulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to hypogonadism and thus a dramatic reduction in estradiol andtestosterone levels in both sexes.
in vitro: The number of DNA 3"-end-labeled cells/cm2 in leiomyomas of control patients and in leiomyomas at the 2nd, 8th, 12th, and 16th weeks of Leuprolide Acetate treatment were at low levels [1]. Testosterone, estradiol and progesterone were also reduced by LA, even though this reduction occurred for progesterone only at the highest LA dosage (10(-6)M; 606.0+/-114.3 ng/ml versus 1524.0+/-246.5 ng/ml; p=0.02) [2].
in vivo: Leuprolide acetate treatment decreases the severity of clinical signs of locomotion, induces a significantly greater body weight gain, increases the MBP and NFs expression, axonal area and cell infiltration in EAE animals [3]. Leuprolide (200 and 300 microg kg(-1) s.c.) per se showed anti-compulsive effect, causing statistically significant inhibition of marble-burying behavior of mice [4].
Clinical trial: Neoadjuvant Abiraterone Acetate Plus Leuprolide Acetate in Men With Localized High Risk Prostate Cancer . Phase 2
Clinical Trial
View MoreCollapse
References
[1]. Mizutani T, Sugihara A, Nakamuro K, Suppression of cell proliferation and induction of apoptosis in uterine leiomyoma by gonadotropin-releasing hormone agonist (leuprolide acetate). J Clin Endocrinol Metab. 1998 Apr;83(4):1253-5.
[2]. Silva AL, Abreu LG, Rosa-e-Silva AC, Leuprolide acetate reduces both in vivo and in vitro ovarian steroidogenesis in infertile women undergoing assisted reproduction. Steroids. 2008 Dec 22;73(14):1475-84.
[3]. Guzmán-Soto I, Salinas E, Hernández-Jasso I, Leuprolide acetate, a GnRH agonist, improves experimental autoimmune encephalomyelitis: a possible therapy for multiple sclerosis. Neurochem Res. 2012 Oct;37(10):2190-7.
[4]. Gaikwad U, Parle M, Kumar A, Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7.
Preparing Stock Solutions
ConcentrationVolumeMass
1 mg
5 mg
10 mg
1 mM
0.7877 mL
3.9387 mL
7.8774 mL
5 mM
0.1575 mL
0.7877 mL
1.5755 mL
10 mM
0.0788 mL
0.3939 mL
0.7877 mL
Please refer to the solubility information to select the appropriate solvent.
References
[1]. Mizutani T, Sugihara A, Nakamuro K, Suppression of cell proliferation and induction of apoptosis in uterine leiomyoma by gonadotropin-releasing hormone agonist (leuprolide acetate). J Clin Endocrinol Metab. 1998 Apr;83(4):1253-5.
[2]. Silva AL, Abreu LG, Rosa-e-Silva AC, Leuprolide acetate reduces both in vivo and in vitro ovarian steroidogenesis in infertile women undergoing assisted reproduction. Steroids. 2008 Dec 22;73(14):1475-84.
[3]. Guzmán-Soto I, Salinas E, Hernández-Jasso I, Leuprolide acetate, a GnRH agonist, improves experimental autoimmune encephalomyelitis: a possible therapy for multiple sclerosis. Neurochem Res. 2012 Oct;37(10):2190-7.
[4]. Gaikwad U, Parle M, Kumar A, Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7.
Molecular Weight
1269.45
Formula
C₆₁H₈₈N₁₆O₁₄
CAS No.
74381-53-6
Storage
Powder
-80°C
2 years
-20°C
1 year
In solvent
-80°C
6 months
-20°C
1 month
Shipping
Room temperature in continental US; may vary elsewhere
[1]. Mizutani T, Sugihara A, Nakamuro K, Suppression of cell proliferation and induction of apoptosis in uterine leiomyoma by gonadotropin-releasing hormone agonist (leuprolide acetate). J Clin Endocrinol Metab. 1998 Apr;83(4):1253-5.
[2]. Silva AL, Abreu LG, Rosa-e-Silva AC, Leuprolide acetate reduces both in vivo and in vitro ovarian steroidogenesis in infertile women undergoing assisted reproduction. Steroids. 2008 Dec 22;73(14):1475-84.
[3]. Guzmán-Soto I, Salinas E, Hernández-Jasso I, Leuprolide acetate, a GnRH agonist, improves experimental autoimmune encephalomyelitis: a possible therapy for multiple sclerosis. Neurochem Res. 2012 Oct;37(10):2190-7.
[4]. Gaikwad U, Parle M, Kumar A, Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7.
Single Primer ("Semi-Random") PCRJuly 26, 2000 ECKDescriptionSingle primer PCR allows amplification from known to unknown regions in chromosomes, phage, plasmi 查看更多>
