Protirelin (Synthetic thyrotropin-releasing factor)
(Synonyms: 普罗瑞林; Thyrotropin-releasing-hormone; TRH) 目录号 : GC30588
A tropic hormone
Cas No.:24305-27-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[2]Ninety male Wistar rats weighing 200-250 g are subjected to the study. In the first experiment, 50 rats are divided into five groups randomly. Four doses of Protirelin dissolved in physiological saline, i. e., 1 mg/kg, 5mg/kg, 10 mg/kg and 20 mg/kg, are administered intraperitoneally to the four groups and saline to the remaining control group. Rectal temperature is measured at the place 5 cm inner from the anus with the electronic thermister before and after treatment with Protirelin or saline. In the second experiment, 40 rats are thyroidectomized or sham-operated under the anesthesia by thiopental sodium. Ten days after the operation, 20 mg/kg of Protirelin or saline is administered to the thyroidectomized and sham-operated animals by i. p. and rectal temperature is measured using the same method as used in the first experiment. These two experiments are undertaken from 1 p, m, to 4 p. m. and the room temperature is kept at 24±1°C through the experiments including the breeding period. For a statistical analysis, Student's t test (two-tailed) is adopted. |
References: [1]. Van Sinay E, et al. Evolutionarily conserved TRH neuropeptide pathway regulates growth in Caenorhabditis elegans. Proc Natl Acad Sci U S A. 2017 May 16;114(20):E4065-E4074. | |
Thyrotropin-releasing Hormone (TRH) is a tropic hormone that stimulates release of thyroid-stimulating hormone (TSH) and prolactin.1 It binds to the human TRH receptor (TRHR) expressed in CHO cells and to rat TRHR in rat brain membranes (IC50s = 25 and 198 nM, respectively).2,3 TRH (1 μM) decreases polyphosphoinositide and increases arachidonic and oleic acid diacylglycerol incorporation into lipids of GH3 rat pituitary tumor cells.4 In vitro, it dose-dependently increases TSH release from rat anterior pituitary slices and prolactin release from cultured anterior pituitary cells.5,6 In vivo, TRH (0.01 mg/kg) increases TSH and prolactin plasma levels in rats.1
1.Dettmar, P.W., Lynn, A.G., Metcalf, G., et al.The ability of RX 77368 - a stabilised analogue of TRH - to provoke the secretion of prolactin and TSH in vivoNeuropeptides3(1)1-8(1982) 2.Yamada, M., Iwasaki, T., Satoh, T., et al.Activation of the thyrotropin-releasing hormone (TRH) receptor by a direct precursor of TRH, TRH-GlyNeurosci. Lett.196(1-2)109-112(1995) 3.Bhargava, H.N., and Das, S.Evidence for opiate action at the brain receptors for thyrotropin-releasing hormoneBrain Res.368(2)262-267(1986) 4.Martin, T.F.J.Thyrotropin-releasing hormone rapidly activates the phosphodiester hydrolysis of polyphosphoinositides in GH3 pituitary cells. Evidence for the role of a polyphosphoinositide-specific phospholipase C in hormone actionJ. Biol. Chem.258(24)14816-14822(1983) 5.Iriuchijima, T., Michimata, T., Miyashita, K., et al.Thyroid hormones regulate the formation of inositol phosphate in response to thyrotropin-releasing hormone in rat anterior pituitariesNeuropeptides21(1)49-53(1992) 6.Apfelbaum, M.E.Role of vasoactive intestinal peptide and 5-HT2 receptor subtype in serotonin stimulation of basal and thyrotropin-releasing-hormone-induced prolactin release in vitro from rat pituitary cellsNeuroendocrinology67(1)45-50(1998)
| Cas No. | 24305-27-9 | SDF | |
| 别名 | 普罗瑞林; Thyrotropin-releasing-hormone; TRH | ||
| Canonical SMILES | {pGlu}-His-Pro-NH2 | ||
| 分子式 | C16H22N6O4 | 分子量 | 362.38 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7595 mL | 13.7977 mL | 27.5953 mL |
| 5 mM | 0.5519 mL | 2.7595 mL | 5.5191 mL |
| 10 mM | 0.276 mL | 1.3798 mL | 2.7595 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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Protirelin (thyrotropin-releasing hormone) in amyotrophic lateral sclerosis. The role of androgens
Arch Neurol.1989 Mar;46(3):330-5.PMID:2563937DOI: 10.1001/archneur.1989.00520390096025.
Protirelin (thyrotropin-releasing hormone) appears to be a neuromodulator in the extrahypothalamic nervous system and has been suggested as an adjunct in the treatment of amyotrophic lateral sclerosis (ALS). Clinical studies have been divided on the efficacy of protirelin (TRH) despite strong experimental findings that are consistent with a role for the peptide in ALS. Recent findings provide evidence of a gender-related specificity in the ability of protirelin to potentiate the monosynaptic reflex. While castration in male neonatal rats lowered the sensitivity to protirelin, testosterone treatment restored that sensitivity. An examination of the clinical studies reveals a failure either to identify patients' sex or to separate the results on the basis of sex. These findings provide convincing evidence for the potential efficacy of protirelin in ALS if the patient's sex and underlying hormonal status are taken into account.
Dose-response studies with protirelin
Arch Gen Psychiatry.1994 Nov;51(11):875-83.PMID:7944876DOI: 10.1001/archpsyc.1994.03950110035006.
Background: A reduced thyrotropin (TSH) response to thyrotropin-releasing hormone (protirelin [TRH]) has been found consistently in a portion of patients with major depression. One hypothesis to explain this observation is that pituitary TRH receptors are down-regulated in major depression. One prediction stemming from this hypothesis is that prolactin (PRL) as well as TSH responses to TRH should be attenuated. To adequately test the pattern of protirelin-induced TSH and PRL responses with a protirelin dose-response design is necessary. Methods: Four doses of protirelin (25, 100, 500, and 800 micrograms) were infused in an ascending schedule at intervals of 3 to 7 days in patients with major depression and in control subjects. Seven women and six men with major depression were compared with age- and gender-matched controls (five women and seven men). The TSH and PRL responses were measured at regular intervals following each dose of protirelin. Results: No significant group differences in baseline levels of thyroid hormones or cortisol were present. Depressed men exhibited significant reductions in both TSH and PRL responses to protirelin across all doses compared with control men. Depressed women exhibited significant reductions in TSH responses but not in PRL responses compared with control women. Conclusions: The findings that men with major depression exhibit reductions in both protirelin-induced TSH and PRL responses support the hypothesis that TRH receptors are downregulated in depression. The findings in women are less clear and may represent the greater variance in the protirelin-induced PRL responses found in women.
Diagnostic dosages of protirelin (TRH) elevate BP by noncatecholamine mechanisms
Arch Intern Med.1984 Jun;144(6):1149-52.PMID:6428340
While performing thyroid function tests, we noticed that protirelin (TRH) raised BP, and, therefore, we investigated the effect of diagnostic dosages of protirelin (500 micrograms) on plasma catecholamine levels and cardiovascular function in eight patients one day before, one day after, and four weeks following heart surgery. Mean arterial pressure (MAP), heart rate (HR), plasma norepinephrine (NE), epinephrine (EPI), dopamine (DA), thyroid hormone (triiodothyronine [T3], thyroxine), and thyrotropin (TSH) levels were measured before and after the intravenous injection of protirelin. Protirelin increased MAP transiently from 88 +/- 2 to 103 +/- 3 mm Hg (before surgery), 86 +/- 4 to 102 +/- 4 mm Hg (one day after surgery), and 86 +/- 4 to 104 +/- 5 mm Hg (four weeks after surgery). There were no notable changes in HR or plasma NE, EPI, or DA levels. The T3 and TSH response to protirelin was normal on all three study days. Protirelin raised MAP by an effect on systemic vascular resistance (SVR) rather than an increase in cardiac output. We conclude the following: (1) diagnostic dosages of protirelin transiently elevate MAP and SVR by a noncatecholamine mechanism, (2) clinicians who perform protirelin tests should be aware of protirelin's transient pressor effects.
Protirelin stimulation test and thyroid function during treatment of depression
Arch Gen Psychiatry.1975 Sep;32(9):1115-8.PMID:810113DOI: 10.1001/archpsyc.1975.01760270047004.
Thyroid levels were estimated in 15 patients with endogenous depressions. Before electroconvulsive treatment (ECT), serum thyroxine (T4) and free T4 index values were elevated (P less than .02). After recovery from depression, the levels were normal. Serum triiodothyronine (T3) and free T3 index were normal both before and after ECT. Serum thyrotropin (TSH) levels were also normal and not substantially altered by the ECT procedure. The mean maximal TSH response to protirelin (thyrotropin-releasing hormone) was diminished in the depressed patients and normal after recovery. In three patients, the increase in TSH response to protirelin after recovery did not occur and they relapsed within six months, while in seven patients with increased TSH response to protirelin after recovery only one relapse occurred. The disturbances in the free T4 index, T4, and the protirelin test may in some depressed patients resemble hyperthyroidism, but this condition can be excluded by means of serum, T3 and free T3 index.
TRH (protirelin) in depressed alcoholic men. Behavioral changes and endocrine responses
Arch Gen Psychiatry.1979 May;36(5):540-7.PMID:107908DOI: 10.1001/archpsyc.1979.01780050050005.
Chronic alcoholics with secondary depression were treated with protirelin in a double-blind, placebo-controlled study. Behavioral data, collected only during the acute alcohol withdrawal state, indicated a beneficial effect of protirelin three hours after injection, but not during subsequent days. Injections caused only mild and infrequent subjective side effects and no cardiovascular effects. Endocrine data were recorded in the acute withdrawal state and after clinical remission. Findings in the acute state suggested thyroid activation and increased central dopaminergic activity, as evidenced by elevated baseline levels of growth hormone, low baseline levels of prolactin, and blunted thyroid-stimulating hormone (TSH) response to protirelin. The first two abnormalities returned to normal levels in the remission state. A blunted TSH response was observed in both the acute and the remission states. Partial persistence of this finding suggests that TSH blunting may not be solely state-dependent. In the acute withdrawal state, TSH blunting was associated with favorable behavioral responses to protirelin.