Improved analogs and novel delivery systems for somatostatin octapeptides.
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.
Moreau
J P
JP
Biomeasure Inc., Milford, MA 01757-3650, USA.
Kim
S
S
Dong
J Z
JZ
Ignatious
F
F
Jackson
S
S
Moreau
S C
SC
Morgan
B A
BA
Touraud
F
F
Taylor
J E
JE
Tissier
B
B
Pellet
M
M
Murphy
W
W
Davis
T
T
D000595:Amino Acid Sequence; D000818:Animals; D002214:Capsules; D003692:Delayed-Action Preparations; D015198:Designer Drugs; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D008297:Male; D008969:Molecular Sequence Data; D051381:Rats; D017207:Rats, Sprague-Dawley; D013004:Somatostatin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000378:metabolism
D002214:Capsules; D003692:Delayed-Action Preparations; D015198:Designer Drugs; D013004:Somatostatin