Deslorelin (acetate)

一种GnRH（促性腺激素释放激素）的肽类激动剂；与GnRHR（促性腺激素释放激素受体）结合，Ki值为0.1nM；通过皮下植入剂（每只动物3mg、6mg和12mg）在犬中减少睾丸体积、精液量、精子活力和总精子数，同时增加异常精子的百分比；在患有ACD（可能指腺垂体功能减退症）的雪貂中，以3mg/植入剂/动物的剂量降低疾病严重程度以及血浆中雌二醇、17-羟孕酮和雄烯二酮的水平；在猫中，以4.7mg/植入剂/动物的剂量抑制排卵和发情期。A peptide agonist of GnRH; binds to GnRHR (Ki = 0.1 nM); decreases testicular volume, semen volume, sperm motility, and total sperm count, as well as increases the percentage of abnormal sperm, in dogs via a subcutaneous implant at 3, 6, and 12 mg per animal; decreases disease severity and plasma levels of estradiol, 17-hydroxyprogesterone, and androstenedione in ferrets with ACD at 3 mg/implant per animal; suppresses ovulation and estrus in cats at 4.7 mg/implant per animal.分子式C64H83N17O12 • XC2H4O2分子量1282.5OC(C=C1)=CC=C1C[C@H](NC([C@H](CO)NC([C@@H](NC([C@@H](NC([C@H]2NC(CC2)=O)=O)CC3=CN=CN3)=O)CC4=CNC5=CC=CC=C45)=O)=O)C(N[C@@H](C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N6[C@@H](CCC6)C(NCC)=O)=O)=O)=O)CC7=CNC8=CC=CC=C78)=O.CC(O)=O