Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C60H86N16O13.C2H4O2 |
Molecular Weight | 1299.4762 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(O)=O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@H](CO)NC(=O)[C@H](CC3=CNC4=C3C=CC=C4)NC(=O)[C@H](CC5=CNC=N5)NC(=O)[C@@H]6CCC(=O)N6
InChI
InChIKey=PYMDEDHDQYLBRT-DRIHCAFSSA-N
InChI=1S/C60H86N16O13.C2H4O2/c1-7-64-57(87)48-15-11-23-76(48)58(88)41(14-10-22-65-59(61)62)69-51(81)42(24-33(2)3)70-56(86)47(31-89-60(4,5)6)75-52(82)43(25-34-16-18-37(78)19-17-34)71-55(85)46(30-77)74-53(83)44(26-35-28-66-39-13-9-8-12-38(35)39)72-54(84)45(27-36-29-63-32-67-36)73-50(80)40-20-21-49(79)68-40;1-2(3)4/h8-9,12-13,16-19,28-29,32-33,40-48,66,77-78H,7,10-11,14-15,20-27,30-31H2,1-6H3,(H,63,67)(H,64,87)(H,68,79)(H,69,81)(H,70,86)(H,71,85)(H,72,84)(H,73,80)(H,74,83)(H,75,82)(H4,61,62,65);1H3,(H,3,4)/t40-,41-,42-,43-,44-,45-,46-,47+,48-;/m0./s1
DescriptionSources: http://products.sanofi.ca/en/suprefact.pdfCurator's Comment: http://www.netdoctor.co.uk/medicines/sexual-health/a7588/suprecur-buserelin/
Sources: http://products.sanofi.ca/en/suprefact.pdf
Curator's Comment: http://www.netdoctor.co.uk/medicines/sexual-health/a7588/suprecur-buserelin/
Buserelin is a synthetic peptide analog of the luteinizing hormone-releasing hormone (LHRH) agonist, which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin is used for palliative treatment of prostate cancer, and for treatment of endometriosis. Buserelin is also used for infertility treatment to prepare the pituitary gland before starting treatment with gonadotrophins (FSH and LH) to artificially stimulate ovulation.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1855 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6777213 |
0.12 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | SUPREFACT Approved UseThe palliative treatment (initial and maintenance treatment) of patients with hormonedependent advanced carcinoma of the prostate gland |
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Primary | SUPREFACT Approved UseSUPREFACT® (buserelin acetate) nasal solution is indicated for the treatment of endometriosis in patients who do not require surgery as primary therapy. The duration of treatment is usually six months and should not exceed nine months. |
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Primary | SUPERCUR Approved UseThis medicine is used to prepare the pituitary gland before starting treatment with gonadotrophins (FSH and LH) to artificially stimulate ovulation. |
Sample Use Guides
In Vivo Use Guide
Sources: http://products.sanofi.ca/en/suprefact.pdf
Buserelin is marketed as a nasal spray or as a solution for subcutaneous injections. For palliative treatment of patients with prostate cancer, for the first seven days of treatment give 500 mcg (0.5 mL) every 8 hours should be given by subcutaneous injection. The dose of buserelin in patients with endometriosis is 400 mcg (200 mcg into each nostril) three times daily using the metered-dose pump (nebulizer) provided.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6777213
Binding affinity of buserelin towards gonadotrophin-releasing hormone receptor was measured using rat Leydig cells and iodinated buserelin as a radioligand. The iodinated buserelin to a single class of high affinity sites at a KD value of 0.12 nM and the number of binding sites is approx. 2500 per interstitial cell. The agonistic activitt was measured as the potency of the peptides to stimulate and inhibit LHRH-induced LH release in rat anterior pituitary cells in primary culture.
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C1910
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ACTIVE MOIETY
SUBSTANCE RECORD