Receptor-selective somatostatin analogs

Details Receptor-selective somatostatin analogs Receptor-selective somatostatin analogs

1995-10-18

1998-05-12

Tsang, Cecilia J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 11, 514 13, 514 14, 530311, 530327, A61K 3812, A61K 3831, C07K 14655

Patent

active

057504997

ABSTRACT:
Analogs of SRIF which are selective for SSTR1 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR1 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor the cloned human receptor SSTR1 but do not bind to mouse SSTR2 and SSTR3, human SSTR4 or rat SSTR5. By incorporating an iodinated tyrosine in position-2 in these selective SRIF analogs, a labelled compound useful in drug-screening methods is provided.

REFERENCES:
patent: 4428942 (1984-01-01), Rivier et al.
patent: 4581169 (1986-04-01), Nestor et al.
patent: 4816438 (1989-03-01), Spiess et al.
patent: 5436155 (1995-07-01), Bell et al.
Hirst et al., `Structure-activity studies with somatostatin: role of lysine in position 4 and 9 for gastric activity`, Regulatory Peptides, vol. 8, pp. 267-271, 1984.

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