| Stereochemistry | ABSOLUTE |
| Molecular Formula | C60H86N16O13 |
| Molecular Weight | 1239.4266 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 9 / 9 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
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=CUWODFFVMXJOKD-UVLQAERKSA-N
InChI=1S/C60H86N16O13/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/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)/t40-,41-,42-,43-,44-,45-,46-,47+,48-/m0/s1
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
PubMed
Patents
Sample Use Guides
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
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.
ACTIVE MOIETY
SALT/SOLVATE (PARENT)
