Moreau J P, Kim S, Dong J Z, Ignatious F, Jackson S, Moreau S C, Morgan B A, Touraud F, Taylor J E, Tissier B, Pellet M, Murphy W, Davis T
Biomeasure Inc., Milford, MA 01757-3650, USA.
Metabolism. 1996 Aug;45(8 Suppl 1):24-6. doi: 10.1016/s0026-0495(96)90074-8.
Appropriate N-terminus modification can result in somatostatin (SRIF) octapeptide analogs that are both more potent and more selective in vitro for the human SRIF receptor type 2 (hsst2). In addition, these modifications can improve the duration of action and bioavailability of SRIF analogs following parenteral administration, as shown by both pharmacological and distribution studies in vivo with BIM-23190 and BIM-23197 in the rat.
适当的N端修饰可产生生长抑素（SRIF）八肽类似物，这些类似物在体外对人2型SRIF受体（hsst2）更有效且更具选择性。此外，如在大鼠体内对BIM-23190和BIM-23197进行的药理学和分布研究所示，这些修饰可提高SRIF类似物经肠胃外给药后的作用持续时间和生物利用度。
