ACTH 1-17 (α1-17-ACTH)
(Synonyms: α1-17-ACTH) 目录号 : GC31109
ACTH 1-17 (α1-17-ACTH) 是一种促肾上腺皮质激素类似物，是一种有效的人黑皮质素 1 (MC1) 受体激动剂，Ki 为 0.21 nM。
Cas No.:7266-47-9
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.00%
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Cell experiment: | Rat pituitary cells are incubated in the presence of varying concentrations of ACTH (1-17) (0.1 nM-1 μM). A significant increase of growth hormone secretion is documented with each concentration[1]. |
Animal experiment: | Mice[3]The effects of ACTH (1-17) on the rate of DNA labeling in the metaphyseal bone of CD2F1 mice are tested on a chronopharmacological dosing schedule. Groups of mice that has been conditioned to a 12-hr light/12-hr dark schedule are injected at one of six different timepoints, 4 hr apart during ,a single 24-hr span with either a low (0.021 I.U/kg) or a high (20 I.U./kg) dose of ACTH (1-17). Control groups receive injections of a placebo at corresponding timepoints. Subgroups of mice are injected with [3H]thymidine ([3H]Tdr) to follow the changes in DNA labeling in the proximal tibial metaphysis at 15 min and 2, 4, 8, 12 and 24 hr after ACTH (1-17) or placebo treatment[3]. |
References: [1]. Tsatmali M et al. ACTH1-17 is a more potent agonist at the human MC1 receptor than alpha-MSH. Cell Mol Biol (Noisy-le-grand). 1999 Nov;45(7):1029-34. | |
ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
ACTH (1-17) is a potent agonist at the hMC1R. ACTH (1-17) shows high affinity for the hMC1R with a Ki value of 0.21±0.03 nM which is slightly higher than that of 0.13±0.005 nM for alpha-MSH[1]. ACTH (1-17) induces a slight and not significant increase in growth hormone secretion even when micromolar concentrations of the peptide are employed in rat pituitary cultures[2].
Inhibition of DNA labeling is noted when the ACTH (1-17) is administered at 2 hr after the beginning of the daily dark span when nocturnal animals become active. When administered at this circadian stage, the larger dose in particular is associated with an inhibition of DNA labeling lasting for 24 hr. The inhibitory effect is much shorter when the same dose is injected 4 hr earlier[3].
[1]. Tsatmali M et al. ACTH1-17 is a more potent agonist at the human MC1 receptor than alpha-MSH. Cell Mol Biol (Noisy-le-grand). 1999 Nov;45(7):1029-34. [2]. Ceda GP, et al. The effects of ACTH (1-17) on GH secretion in vitro. Horm Metab Res. 1987 Aug;19(8):361-3. [3]. Walker WV, et al. Effect of an adrenocorticotropin analogue, ACTH (1-17), on DNA synthesis in murine metaphyseal bone. Biochem Pharmacol. 1985 Apr 15;34(8):1191-6.
| Cas No. | 7266-47-9 | SDF | |
| 别名 | α1-17-ACTH | ||
| Canonical SMILES | Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg | ||
| 分子式 | C95H145N29O23S | 分子量 | 2093.41 |
| 溶解度 | Soluble in Water | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.4777 mL | 2.3884 mL | 4.7769 mL |
| 5 mM | 0.0955 mL | 0.4777 mL | 0.9554 mL |
| 10 mM | 0.0478 mL | 0.2388 mL | 0.4777 mL |
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ACTH 1-17 and pituitary-adrenal function in human
In this study we have compared the effects of the ACTH 1-17 analogue, alsactide (Synchrodyn 1-17,) and of the ACTH 1-24 fragment, on the dynamics of ACTH-cortisol secretion. In 2 healthy women, 100 micrograms alsactide injected i.m. at 07(00) caused a much greater and sustained cortisol secretion than 100 micrograms ACTH 1-24. However, adrenocortical stimulation effected by alsactide terminated within 24 h, since plasma cortisol levels recorded 24 h after alsactide injection were even lower than the corresponding values of the previous day. In 8 other women, daily administration of 100 micrograms alsactide at 07(00) for 15-days resulted in a significant blunting (p less than 0.05) of the ACTH secretion in response to insulin-induced hypoglycemia. This finding is even more meaningful in view of the more marked blood glucose fall (p less than 0.01) observed in the post treatment insulin tolerance test. Both baseline and insulin-stimulated cortisol levels were reduced after alsactide (p less than 0.02) so that cortisol increments above baseline were of comparable magnitude before and after treatment with the ACTH analogue. In 8 additional women, no significant changes in the cortisol response to hypoglycemia, in spite of more profound blood glucose fall (p less than 0.05), were noted after a 15-day treatment with 250 micrograms ACTH 1-24 daily. In all, these findings show that ACTH 1-17, compared to ACTH 1-24, effects a much more potent stimulation of cortisol secretion which, however, terminates within 24 h.(ABSTRACT TRUNCATED AT 250 WORDS)
ACTH 1-17 and sexual behavior
The influence of the administration of ACTH 1-17 on the sexual behavior has been studied in a group of male patients affected by psychogenic impotence, i.e. without any detectable organic reason for such disturbance. The administration of the drug led to a notable increase in the sexual performance of the patients. By the way, all the hormonal parameters taken into account (gonadotropins, sexual steroids, adrenal steroids, etc.), were not affected by the treatment. The AA. conclude therefore that the beneficial effect of the ACTH 1-17 on the sexual behavior was due to a direct action on the CNS and was not hormone-mediated.
ACTH 1-17 effects on intermediary metabolites in healthy subjects
Some acute and chronic metabolic effects of a new ACTH analogue (ACTH 1-17, Synchrodyn) were evaluated in healthy subjects and compared to those of the synthetic fragment ACTH 1-24. The peptides were injected at doses reportedly comparable with regard to their corticotropic effect, i.e. 100 micrograms ACTH 1-17 and 250 micrograms ACTH 1-24. A similar increase in blood glucose, NEFA and ketone bodies concentrations, without any significant modification of insulin, C-peptide and glucagon levels, was observed after injecting both peptides. The chronic treatment with ACTH 1-24 induced a significant increase in basal lactate, pyruvate and alanine blood concentrations. The levels of these metabolites resulted unaffected or slightly reduced after the corresponding treatment with ACTH 1-17. Our data are compatible with a certain degree of exhaustion of the adrenocortical reserve or, alternatively, a resetting of the circadian cortisol rhythm after prolonged treatment with the ACTH 1-17 analogue.
ACTH 1-17 stimulates GH pituitary secretion in humans
Nineteen normal subjects (12 men and 7 women) were injected with 100 micrograms of ACTH 1-17. Additionally 6 male subjects were studied twice at 3-day intervals with random infusions of ACTH 1-17 and saline. A clear GH response to ACTH 1-17 infusions (GH peak higher than 5 ng/ml) was documented in 10 out of 12 males and in 6 out of 7 women. In the 6 male subjects studied twice, clear-cut GH increments were observed only after peptide administration. PRL levels decreased throughout the study period both in male and female subjects; however, when the PRL percentage decline was evaluated in the same group of subjects after saline and ACTH 1-17, the more obvious decrease of PRL levels after the peptide infusion was not statistically significant. No variation of LH, FSH and TSH levels was documented. With the exception of the specific increase of cortisol levels, no significant change in peripheral steroid pattern (Te, E2, DHEA-S) was observed. In this experiment the effect on GH secretion was quite evident in both sexes. This effect was obtained using the lowest dosage of ACTH preparation documented in the literature.
Clinical chronopharmacology of ACTH 1-17. I. Effects on plasma cortisol and urinary 17-hydroxycorticosteroids
The aim of the investigation was to study the effects of ACTH 1-17 on both plasma cortisol and urinary 17-OHCS in health adult young males with regard to the time (clock hours) at which this polypeptide was injected. Eight healthy adults (males from 18-30 years) volunteered for the study. They were synchronized with a diurnal activity from 0700 to 0000 and a nocturnal rest. Each week, during 6 consecutive weeks (January 19 to February 25, 1980), a 3-day test was performed on Saturday, Sunday and Monday. On Sundays 3 control-tests and 3 ACTH-tests were programmed during which either saline or 100 micrograms ACTH 1-17 were injected i.m. at respectively 0700, 1400 and 2100. During each 3 day-test (72 h) the urinary excretion of 17-OHCS was determined every 4 h at fixed clock hours. In addition, on Sundays, venous blood was sampled prior to control or ACTH injections at respectively 0700, 1400, and 2100 and 20, 40, 60, 90, 120, 150 and 180 min thereafter. Plasma cortisol (radioimmunoassay) was determined in samples thus collected. Both conventional and cosinor methods were used for statistical analyses. A strong and statistically significant rise of plasma cortisol was observed after all of the ACTH 1-17 injections. The obtained mean response curves were observed after all of the ACTH 1-17 injections. The obtained mean response curves were similar in form and parallel. The highest plasma cortisol curve corresponded to ACTH injected at 0700, the lowest to ACTH injected at 2100. The curve corresponding to ACTH injected at 1400 went in-between. The 24-h urinary excretion of 17-OHCS after ACTH 1-17 was approximately 4 times greater than the control value when injected at 0700, approximately 3 times greater than control when injected at 1400 and only twice greater than control when injected at 2100. In terms of changes in plasma cortisol and 17-OHCS the greatest best benefit of ACTH 1-17 is achieved when this polypeptide is injected at 0700, rather than at 1400 or 2100 in diurnally active subjects.