To study MTII-mediated MC4R internalization and the effect of GRP78 knockdown on MC4R internalization. Results showed that GRP78 knockdown attenuated MTII-mediated receptor internalization.
Exp Mol Med. 2018 Sep 12;50(9):1-14
HDC neurons
100 nM
MTII induced excitation of HDC neurons, leading to membrane depolarization and increased spontaneous firing rate.
Mol Metab. 2020 May;35:100956
B16-F10 melanoma cells
0.1 nM
7 days
MTII dose-dependently suppressed the anchorage-independent growth of melanoma cells.
Int J Mol Sci. 2020 Jan 20;21(2):681
B16-F10 melanoma cells
0.1 nM–1 μM
16 hours
MTII dose-dependently inhibited the invasiveness of B16-F10 melanoma cells.
Int J Mol Sci. 2020 Jan 20;21(2):681
B16-F10 melanoma cells
10 nM
48 hours
MTII significantly attenuated the migration of B16-F10 melanoma cells but had no effect on cell proliferation.
Int J Mol Sci. 2020 Jan 20;21(2):681
Melanotan II/美拉诺坦 (MT)-II 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Ob/ob mice and diet-induced obese (DIO) mice
Intracerebroventricular injection
3 nmol
5 days
To study the effect of MTII on body weight and food intake. Results showed that 4-PBA pretreatment overcame the antagonistic effect of AgRP and prolonged the effect of the MC4R agonist on food intake and body weight control.
Exp Mol Med. 2018 Sep 12;50(9):1-14
Mice
Hdc-Cre::hM4Di mice
Intracerebroventricular injection
1 nmol
Single injection
Inhibition of HDC neurons strikingly enhanced the anorexigenic effects of MTII, suggesting that MC4R activation of histaminergic neurons may restrain the anorexigenic effects of melanocortin system activation.
Mol Metab. 2020 May;35:100956
C57BL/6 mice
B16-F10 melanoma model
Topical administration
0.1 mL of 1 μg/mL MTII in PBS
Once daily for 10 days
Topical MTII therapy significantly suppressed the progression of melanoma in mice through proliferation inhibition, apoptosis induction, and neovascularization blockade.
Int J Mol Sci. 2020 Jan 20;21(2):681
Prairie voles
Female and male prairie voles
Intraperitoneal injection
10 mg/kg
Single injection
MTII facilitated partner preference formation in both female and male prairie voles, and this effect persisted for 7 days post-injection.
Neuropsychopharmacology. 2015 Jul;40(8):1856-65
Sprague-Dawley rats
Myocardial infarction model
Intracerebroventricular injection
10 ng/h
28 consecutive days
Activation of CNS MC4R significantly improved cardiac function post-MI and attenuated the progression of heart failure.
JACC Basic Transl Sci. 2021 Jan 25;6(1):55-70
Mice
Obesity model
Intraperitoneal injection
3 mg/kg
Single dose
To evaluate the effect of MT-II on food intake and body weight, results showed that MT-II significantly reduced food intake.
Mol Metab. 2023 Feb;68:101665
Mice
ArcPomc-/- obese mouse model
Intraperitoneal injection
100μg/animal
Single dose with measurements within 4 hours
To evaluate MTII's effect on circulating adiponectin levels; Results showed MTII treatment significantly reduced adiponectin levels in both ArcPomc-/- and wild-type mice
Mol Metab. 2020 May;35:100957
Mice
ArcPOMC-deficient mice
Intracerebroventricular injection
0.5 mg
Three times daily, lasting 30 minutes
MTII treatment reversed the improved glucose tolerance and glycosuria phenotype in mutant mice
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