Structure Activity Studies on Somatostatin

Sarantakis, Dimitri; McKinley, W. A.; Jaunakais, Ivars; Clark, Donald R.; Grant, Norman H.

doi:10.1111/j.1365-2265.1976.tb03835.x

Cited by 40 publications

(25 citation statements)

References 11 publications

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“…The first such analog, found by the group at the Wyeth Research Laboratories, was [des-Asn5]-somatostatin. This analog has approximately 4, 10, and 1 percent of the activity of somatostatin in inhibiting, respectively, the secretion of GH, insulin, and glucagon (87). Although such an analog was not of clinical interest, it showed that dissociation of the biological activities of the native somatostatin on three of its receptors could be achieved.…”

Section: Biological Activity Of Somatostatinmentioning

confidence: 99%

Peptides in the Brain: The New Endocrinology of the Neuron

Guillemin

1978

Science

466

150

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Section: Biological Activity Of Somatostatinmentioning

confidence: 99%

Peptides in the Brain: The New Endocrinology of the Neuron

Guillemin

1978

Science

466

150

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“…Recently a series ofAsn5 (asparagine in position 5) deleted somatostatin analogs were reported to preferentially inhibit insulin rather than glucagon or GH secretion (10,11). These studies suggested the feasibility of developing analogs with selective activities.…”

mentioning

confidence: 99%

Somatostatin: Analogs with Selected Biological Activities

Brown

Rivier

Vale

1977

Science

101

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[D-Cys14]-Somatostatin is the first analog of somatostatin found to be more potent in inhibiting glucagon and growth hormone secretion that it is in inhibiting insulin secretion. [D-Trp8]-Somatostatin is eight to ten times more potent than somatostatin in inhibiting insulin, glucagon, and growth hormone secretion. [D-Trp8, D-Cys14]-Somatostatin is more potent than [D-Cys14]-Somatostatin, but retains its relative selectivity in being a more potent inhibitor of the secretion of glucagon and growth hormone than of insulin.

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“…Ala5-somatostatin has similar activity when tested against glucagon, insulin and GH release Brown et al 1976a) but removal of Asn5 without substitution results in a compound which inhibits insulin but not glucagon release (Sarantakis, McKinley, Jaunakais, Clark & Grant, 1976;Effendic, Luft & Sievertsson, 1975;Brown, Rivier & Vale, 1976b). It is possible, therefore, that the Asn5 acts as a spacer in the somatostatin molecule which is important in the inhibition of glucagon release, but not GH or insulin.…”

Section: Discussionmentioning

confidence: 99%

Structure‐activity relationships of eighteen somatostatin analogues on gastric secretion.

Brown¹,

Coy²,

Gómez-Pan³

et al. 1978

The Journal of Physiology

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SUMMARY1. The effect of somatostatin and eighteen somatostatin analogues on pentagastrin-stimulated gastric acid and pepsin secretion was investigated in the conscious vagotomized cat prepared with chronic gastric fistulae. The majority of the analogues are peptides where D-amino acids are incorporated into the molecule instead of the natural L-isomers.2. The ID50 for cyclic-somatostatin inhibition of near-maximal gastric acid secretion stimulated by pentagastrin 8 jug kg-1 hr-1 was found to be 1-29 + 0-13 n-mole kg-1 hr-1. Pentagastrin-stimulated pepsin secretion had a lower threshold to somatostatin inhibition than did acid secretion.3. D-Phe6, D-Phe7, D-Thr10, D-Thr12 and D-Phe6-D-Trp5 analogues all show low biological activity against the secretion of gastric acid and pepsin, growth hormone, insulin and glucagon. None of these analogues are antagonists of the cyclic-somatostatin inhibition of gastric secretion, suggesting that they have low affinity for this somatostatin receptor.4. The analogues under investigation show parallel changes in activity against gastric and growth hormone secretion, suggesting a similarity between the gastric and growth hormone receptors for somatostatin.5. D-Cys14 analogues are equipotent with or have a greater potency than cyclicsomatostatin in inhibiting the secretion of gastric acid, growth hormone and glucagon but show low insulin inhibiting activity.

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Structure Activity Studies on Somatostatin

Cited by 40 publications

References 11 publications

Peptides in the Brain: The New Endocrinology of the Neuron

Peptides in the Brain: The New Endocrinology of the Neuron

Somatostatin: Analogs with Selected Biological Activities

Structure‐activity relationships of eighteen somatostatin analogues on gastric secretion.

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