Title: Histrelin
CAS Registry Number: 76712-82-8
CAS Name: 6-[1-(Phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-10-deglycinamide luteinizing hormone-releasing factor (pig)
Additional Names: 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-Nt-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide; L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-Nim-benzyl-histidyl-L-leucyl-L-arginyl-L-proline ethylamide; [(im-Bzl)-D-His6,Pro9-NEt]-gonadotropin-releasing hormone
Manufacturers' Codes: ORF-17070; RWJ-17070
Molecular Formula: C66H86N18O12
Molecular Weight: 1323.50
Percent Composition: C 59.89%, H 6.55%, N 19.05%, O 14.51%
Literature References: Synthetic nonapeptide agonist analog of LH-RH, q.v. Prepn: J. E. F. Rivier, W. W. Vale, Jr., EP 21620; eidem, US 4244946 (both 1981 to Salk Inst.). See also: J. E. Rivier, W. W. Vale, Life Sci. 23, 869 (1978). Pharmacology: Y-Q. Cao et al., Int. J. Androl. 5, 158 (1982); J. W. Gunnet et al., J. Endocrinol. 131, 211 (1991). HPLC purification: J. Rivier et al., J. Chromatogr. 288, 303 (1984). Amino acid sequence: C. J. Shaw, M. L. Cotter, Chromatographia 21, 197 (1986). Clinical evaluations in polycystic ovarian disease: K. Steingold et al., J. Clin. Endocrinol. Metab. 65, 773 (1987); in endometriosis: idem et al., Obstet. Gynecol. 69, 403 (1987); in porphyria: K. E. Anderson et al., Arch. Int. Med. 150, 1469 (1990); in PMS: J. F. Mortola et al., J. Clin. Endocrinol. Metab. 72, 252A (1991). Review of pharmacology and therapeutic use in central precocious puberty: L. B. Barradell, D. McTavish, Drugs 45, 570-588 (1993).
Properties: [a]D20 -33.9° (c = 1 in acetic acid).
Optical Rotation: [a]D20 -33.9° (c = 1 in acetic acid)
Derivative Type: Acetate
Trademarks: Supprelin (Roberts)
Line Formula: C66H86N18O12.xC2H4O2.yH2O
Therap-Cat: Treatment of central precocious puberty.
Keywords: LH-RH Agonist. |