Deslorelin
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Deslorelin

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Deslorelin is a synthetic nonapeptide analogue of the natural gonadotrophin releasing hormone super-agonist (GnRH agonist) with potential antineoplastic activity. It binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. It stops the production of sex hormones. It is currently used to induce ovulation in mares as part of the artificial insemination process. It is also used to stabilize high-risk pregnancies, mainly of livestock and is also used to treat benign prostate hyperplasia in dogs. It is manufactured by Thorne BioScience LLC and was introduced to the USA market following the withdrawal of Ovuplant. It has been listed.

Category
Peptide Inhibitors
Catalog number
BAT-010033
CAS number
57773-65-6
Molecular Formula
C64H83N17O12
Molecular Weight
1282.45
Deslorelin
IUPAC Name
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Synonyms
H-Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHEt; L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-tryptophyl-L-leucyl-L-arginyl-L-proline ethylamide; 1-9-Luteinizing hormone-releasing factor (swine), 6-D-tryptophan-9-(N-ethyl-L-prolinamide)-; Luteinizing hormone-releasing factor (pig), 6-D-tryptophan-9-(N-ethyl-L-prolinamide)-10-deglycinamide-; D-Trp6-Pro9-N-ethylamide-LH-RH; [D-Trp6,des-Gly-NH210]-LH-RH ethylamide; [D-Trp6,des-Gly10]-LH-RH ethylamide; [D-Trp6,Pro9-NHEt]LH-RH; [de-Gly10,D-Trp6,Pro-NHEt]-LH-RH; [Des-Gly10,D-Trp6]-LH-RH ethylamide; Bachem 9022; D-Trp LHRH-PEA; H 4065; PTL 3001; Somagard; Somagorad
Related CAS
1642579-30-3 (x-acetate salt) 82318-06-7 (monoacetate salt) 785814-26-8 (x-citrate salt) 2768499-18-7 (TFA salt) 67190-19-6 (Deleted CAS)
Appearance
White powder
Purity
98%
Density
1.48±0.1 g/cm3
Boiling Point
1783.4°C at 760 mmHg
Sequence
Pyr-HWSYwLRP-NHEt
Storage
Store at -20°C
Solubility
Soluble in DMSO, not in water
InChI
InChI=1S/C64H83N17O12/c1-4-68-62(92)53-16-10-24-81(53)63(93)46(15-9-23-69-64(65)66)74-56(86)47(25-35(2)3)75-58(88)49(27-37-30-70-43-13-7-5-11-41(37)43)77-57(87)48(26-36-17-19-40(83)20-18-36)76-61(91)52(33-82)80-59(89)50(28-38-31-71-44-14-8-6-12-42(38)44)7
InChI Key
GJKXGJCSJWBJEZ-XRSSZCMZSA-N
Canonical SMILES
CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CC7=CN=CN7)NC(=O)C8CCC(=O)N8
1.New approaches to non-surgical sterilization for dogs and cats: Opportunities and challenges.
Rhodes L Reprod Domest Anim. 2017 Apr;52 Suppl 2:327-331. doi: 10.1111/rda.12862. Epub 2016 Nov 28.
Over the last 40 years, researchers have explored methods to non-surgically suppress fertility in animals. Immunocontraception has been used to control wildlife populations but does not confer long-term immunity. The gonadotropin-releasing hormone (GnRH) agonist deslorelin, formulated as an implant to provide 6-month to 1-year suppression of fertility in male dogs, is available commercially in some countries. Neither of these approaches provide permanent sterility. A single-dose, permanent treatment would be a valuable tool in dog and cat population control. The Michelson Prize and Grants (MPG) programme was initiated "to eliminate shelter euthanasia of healthy, adoptable companion animals and reduce populations of feral and free-roaming cats and dogs" offering a $25 million US prize for a non-surgical sterilant that is effective as a single treatment in both male and female dogs and cats. Michelson Prize and Grants programme has offered US $50 million in grant money for research and has attracted scientists worldwide. Approaches under study include gene therapy, small interfering RNA to inhibit reproductive targets and delivery of cytotoxins to pituitary gonadotrophs or GnRH producing neurons in the hypothalamus.
2.Postponement of puberty in queens treated with deslorelin.
Cecchetto M;Salata P;Baldan A;Milani C;Mollo A;Fontaine C;Sontas H;Gelli D;De Benedictis G;Stelletta C;Romagnoli S J Feline Med Surg. 2017 Dec;19(12):1224-1230. doi: 10.1177/1098612X16688406. Epub 2017 Feb 14.
Objectives The purpose of this study was to assess efficacy of deslorelin, a gonadotropin-releasing hormone (GnRH) agonist marketed in Europe for the control of male dog reproduction, for the postponement of puberty in queens. Methods Nine prepubertal queens aged 3-9 months were selected for this study; their general and reproductive health was checked through clinical, haematological, vaginal cytology and hormonal tests. Following treatment with a 4.7 mg deslorelin implant, each cat received a monthly clinical examination and blood was collected for hormonal assay every third month. Cats were monitored for 14.1 ± 5.2 (range 7-23) months. Results All cats were in good body condition and normal health prior to treatment. Their health status remained unchanged throughout the study and no significant variation was observed with regard to serum progesterone or oestradiol. Seven days post-treatment, 1/9 queens showed signs of heat, and one other queen showed complete vaginal keratinisation. No other signs of heat were subsequently observed in any other queen. Five queens were lost during the study after 7, 7, 16, 17 and 18 months of observation (during which time they did not show signs of heat).
3.Characteristics of luteinizing hormone (LH) and testosterone secretion, pituitary responses to LH-releasing hormone (LHRH), and reproductive function in young bulls receiving the LHRH agonist deslorelin: effect of castration on LH responses to LHRH.
D'Occhio MJ;Aspden WJ Biol Reprod. 1996 Jan;54(1):45-52.
Young bulls were treated with graded dosages of the LHRH agonist deslorelin to ascertain 1) whether increased testosterone secretion persisted over a wide dose range of agonist; 2) whether elevated testosterone was maintained long-term and, if so, what effects there were on reproductive function; and 3) what pituitary responses to exogenous LHRH occurred in intact and castrated bulls receiving deslorelin. In three experiments, bulls received dosages of agonist ranging from approximately 0.15 to 29.0 micrograms deslorelin/kg live weight/day, by means of either bioimplants or injections. At all dosages, deslorelin induced an acute increase in plasma LH concentrations that declined after 24 h but remained at greater concentrations than in controls, although the differences were relatively small. Profiles of LH in bulls treated with deslorelin were characterized by tonic secretion with no clear evidence of LH pulses. Plasma testosterone concentrations were increased at all dosages of deslorelin and in one experiment remained greater than in controls for over 100 days of treatment. This increase was associated with an increase in the rate of testis growth; however, there were no apparent improvements in semen parameters.
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