Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P61278 (somatostatin)
 22,083 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Four adult patients with active acromegaly underwent studies of their 24-hour secretory pattern of hGH and Prl prior to and at the end of 3 months of treatment with the octreotide (somatostatin analog SMS 201-995) 100 micrograms s.c. every 8 h. Blood was withdrawn at 30-min intervals with the aid of a constant withdrawal pump. The best fit cosinor method was used to define the following rhythm parameters: mesor, amplitude, acrophase and periodicity. Prior to treatment, hGH secretion was increased in all patients. The mean 24-hour ranged from 9-47 ng/ml with amplitude 5.2-23 and observed maximal pulse 41-95 ng/ml. Computed rhythms were circadian in 3 patients and ultradian in 1; in 2 patients the acrophases were shifted to daytime. hPrl secretion was altered in 3 of the patients. Two had elevated mean 24-hour of 17.7 and 22.2 ng/ml, while computed rhythms showed semicircadian periodicity in 1 of them and circadian periodicity with a shift of acrophase to daytime in the other. The third patient who had normal hPrl levels, showed ultradian 8-hour periodicity. At the end of treatment there was a marked reduction in hGH secretion in 1 patient and a lesser reduction in the other 3. The rhythm was influenced by the masking effect of the drug, to yield an 8-hour period with acrophases related to injection clock time having equal amplitudes.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effect of octreotide on 24-hour growth hormone and prolactin secretory patterns in acromegalics. 182 80

Electroencephalographic (EEG) seizures were measured in rats after intrahippocampal injection of 120 nmol quinolinic acid into the stratum radiatum CA1 or 0.19 nmol kainic acid in the dentate gyrus or in the stratum radiatum. Injection of 5 micrograms SMS 201-995, a peptidase-resistant cyclic octapeptide analogue of somatostatin, into the stratum radiatum, 15 min before quinolinic acid, did not significantly modify the number of seizures and the total time in seizures. Five micrograms SMS 201-995 injected into the stratum radiatum reduced the number of seizures induced by kainic acid in the same area and the total time spent in seizures by 58% and 75%, respectively (Student's t-test; P less than 0.01). In both instances the latency to the first ictal episode was not significantly modified. Lesions of the medial septum, which reduced the activity of choline-o-acetyl-transferase (CAT) in the dorsal hippocampus by greater than 90% after one week did not significantly affect seizures induced by quinolinic acid. In rats lesioned in the medial septum, 5 micrograms SMS 201-995 reduced the total time spent in seizures by 43%, without changing the number of ictal episodes and raised the latency to the first quinolinic acid-induced seizure by 53% (ANOVA 2 x 2, P less than 0.05) but had no effect on these measures in the corresponding sham-operated group.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:A peptidase-resistant cyclic octapeptide analogue of somatostatin (SMS 201-995) modulates seizures induced by quinolinic and kainic acids differently in the rat hippocampus. 183 Jan 35

Chronic overproduction of growth hormone in man and the cat is most often caused by a GH-producing tumour of the pituitary gland. In dogs the usual cause is quite different. In this species endogenous progestins (during metestrus) and exogenous progestins (used to prevent estrus) cause excessive GH secretion that is reversible. For a better understanding of the mechanism of progestin-induced GH synthesis and secretion, studies were carried out in healthy dogs and in dogs presented with GH excess. The effectiveness of stimulation of GH secretion by hGHRH, and clonidine and of the inhibition with the somatostatin analogue SMS 201-995 were evaluated in healthy male dogs. SMS 201-995 had no influence on basal plasma GH levels, but significantly inhibited the hGHRH and clonidine-evoked GH release. In healthy female dogs the basal concentrations of plasma GH were significantly higher during metestrus than during anestrus. The elevated basal plasma GH levels were associated with a diminished responsiveness to stimulation with clonidine. In female dogs with experimental or spontaneous progestin-induced chronic overproduction of GH (and IGF-I), plasma GH levels were completely unresponsive to stimulation with hGHRH and clonidine and to inhibition with SMS 201-995. It is concluded that in the female dog the progestin-induced GH excess has characteristics of autonomous secretion.
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PMID:Progestins and growth hormone excess in the dog. 183 44

The presence of somatostatin receptors was investigated in 57 primary human ovarian tumors using in vitro receptor autoradiography with three different somatostatin radioligands, 125I-[Tyr11]-somatostatin-14, 125I-[Leu8, D-Trp22, Tyr25]-somatostatin-28, or 125I-[Tyr3]-SMS 201-995. Three cases, all belonging to epithelial tumors, were receptor positive; specifically 1 of 42 adenocarcinomas, 1 of 3 borderline malignancies, and 1 of 2 cystadenomas. Four other epithelial tumors (3 fibroadenomas, 1 Brenner tumor), 4 sex cord-stromal tumors (2 fibrothecomas, 2 granulosa cell tumors), and 2 germ cell tumors (1 dysgerminoma, 1 teratoma) were receptor negative. In the positive cases, the somatostatin receptors were localized on epithelial cells exclusively, were of high affinity (KD = 4.6 nmol/l [nanomolar]), and specific for somatostatin analogs. These receptors bound somatostatin-14 and somatostatin-28 radioligands with a higher affinity than the octapeptide [Tyr3]-SMS 201-995. Healthy ovarian tissue had no somatostatin receptors. A subpopulation of relatively well-differentiated ovarian tumors, therefore, was identified pathobiochemically on the basis of its somatostatin receptor content. This small group of somatostatin receptor-positive tumors may be a target for in vivo diagnostic imaging with somatostatin ligands.
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PMID:Somatostatin receptors in differentiated ovarian tumors. 185 Sep 62

An invasive TSH-secreting adenoma inducing mild hyperthyroidism was diagnosed in a 16-year-old male. Initial surgical treatment led to a temporary clinical and biological improvement. Recurrence of the thyrotoxicosis was treated with the somatostatin analogue, SMS 201-995 (octreotide) with normalization of the serum thyroid hormone levels with a dose of 200 micrograms per day. With immunoelectron microscopy, the tumour cells appeared poorly granulated with small secretory granules located at the periphery of the cells; only part of those were immunoreactive with an anti-TSH beta monoclonal antibody. No specific TRH binding site was found in a tumour membrane preparation. By quantitative autoradiography, somatostatin specific binding sites were as numerous in the TSH-secreting tumour as in control GH-secreting tumours. Binding kinetics and guanosine triphosphate dependency of the binding were equivalent in the TSH and GH tumours tested. Although all of the tumour cells displayed the same ultrastructural features, some were non-immunoreactive, suggesting that they could secrete an altered form of TSH. The absence of TRH receptors in the tumour cells is in accordance with previous reports on this type of tumour. We confirm the efficiency of octreotide treatment in this case of neoplastic TSH inappropriate secretion. The therapeutic effect of octreotide goes along with the presence of a high density of guanine nucleotide-dependent somatostatin binding sites in the tumour cells.
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PMID:A human TSH-secreting adenoma: endocrine, biochemical and morphological studies. Evidence of somatostatin receptors by using quantitative autoradiography. Clinical and biological improvement by SMS 201-995 treatment. 185 93

Treatment with the somatostatin analogue octreotide, SMS 201-995 (Sandostatin), has been carried out in a series of 23 patients with malignant midgut carcinoid tumours. The patients received initially 50 micrograms twice a day for six months, thereafter a median of 100 micrograms twice daily. Six of 22 evaluable patients (28%) showed objective tumour response lasting for 6 to 30 months. Stable disease was observed in 8 of the 22 patients (36%) and progressive disease in a further 8 patients (36%). A subjective response with decrease of diarrhoea or flushing was noted in 11 out of 22 patients (50%). Two out of 6 patients with objective response demonstrated a significant decrease of tumour size lasting for 6 and 30 months respectively. In order to maintain the clinical response, the dose had to be increased in all 6 responders. The adverse effects included development of diabetic blood glucose levels in 8 out of 22 patients (36%). Albumin-modified serum calcium levels were significantly reduced after treatment with octreotide 50 micrograms twice a day. One patient developed symptoms of hypocalcemia which was reversed by supplementation with calcium and D-vitamins. The somatostatin analogue SMS 201-995 has a beneficial effect in the treatment of patients with the carcinoid syndrome. However, the precise role of the drug in the long-term management of these patients has to be further investigated.
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PMID:Treatment of malignant midgut carcinoid tumours with a long-acting somatostatin analogue octreotide. 185 8

The effects of 4-h incubation in the presence of bombesin on the incorporation of [3H]-thymidine into DNA of the rat thyroid lobes, collected from animals treated in vivo with a long-acting somatostatin analog (SMS 201-995) or with 0.9% NaCl, were investigated. It was shown that not only in vivo injections of SMS 201-995, but also, unexpectedly, in vitro incubation with bombesin inhibited [3H]-thymidine incorporation. The two examined substances did not reveal any additive action in their inhibitory effects on the thyroid growth.
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PMID:Inhibitory effect of bombesin and SMS 201-995 on DNA synthesis in the rat thyroid lobes incubated in vitro. 185 12

In the present study we used the model of cultured somatostatin-receptor-positive prolactin (PRL)-secreting rat pituitary tumor cells to investigate the possible interrelationships between the anti-mitotic and hormone-release-inhibitory effects of the somatostatin analog octreotide (SMS 201-955) and the effects of vincristine, methotrexate, fluouracil and suramin. Dose-dependent inhibitory effects of all compounds were shown both on the DNA content and on PRL release. Octreotide and these cytostatic compounds were slightly additive in their anti-proliferative and anti-secretory effects. The somatostatin analog did not alter drug sensitivity in these tumor cells, however. The data obtained in this tumor model suggest that octreotide can be effectively administered in combination with cytostatic drugs and/or suramin.
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PMID:The interrelationship between the anti-mitotic action of the somatostatin analog octreotide and that of cytostatic drugs and suramin. 186 Jul 38

In the present study we have investigated the effects of proglumide (PRO) and somatostatin analog (SMS 201-995) on the mitotic activity of colonic mucosa in rats under basal conditions and after omeprazole (OM). The stathmokinetic method was used. Proglumide and OM were administered for 5 days, twice daily, SMS 201-995 on the 5th day of the experiment only, also twice daily. It was found that: 1) OM enhanced the proliferation of colonic mucosa, as well as increased serum gastrin, when compared to controls, 2) OM and PRO, when applied jointly, decreased the mitotic activity of the colonic epithelium, 3) PRO alone increased the colonic cell proliferation.
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PMID:Effect of omeprazole-induced hypergastrinaemia on the proliferation of colonic mucosal epithelial cells in the rat. 186 13

A 46-year-old woman with acromegaly and hyperthyroidism due to a pituitary adenoma. She had high serum thyroid-stimulating hormone (TSH) levels and very high serum growth hormone (GH) levels. Transsphenoidal removal of the tumor, post-operative irradiation, frontal craniotomy for removal of residual tumor and large-dose bromocriptine therapy were carried out consecutively. After therapy, serum GH levels gradually decreased, but not to the normal range, and serum TSH levels remained at inappropriately normal levels. Using immunoperoxidase techniques, GH-, TSH- and follicle-stimulating hormone (FSH)-containing cells were demonstrated in the adenoma. A long-acting somatostatin analogue (SMS 201-995, 600 micrograms/day) suppressed the serum GH level to the normal range with a concomitant suppression of TSH. Furthermore, the paradoxical serum GH responses to TRH and LH-RH were slightly improved. No important subjective side-effects were noted. Therefore, SMS 201-995 appeared to be a very effective drug in this patient with a GH- and TSH-producing pituitary tumor.
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PMID:Effect of a long-acting somatostatin analogue (SMS 201-995) on a growth hormone and thyroid stimulating hormone-producing pituitary tumor. 186 12


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