Introduction
Corticotropin-releasing factor (CRF) is a 41 amino acid peptide that is an important hormone in the hypothalamic-pituitary-adrenalin axis (HPA axis) and is closely related to stress regulation in vivo. It plays an important role in mental and neurodegenerative diseases. CRF can alleviate the symptoms of Parkinson's disease by affecting the release of dopamine, and CRF (ovine) Trifluoroacetate is the commonly used and effective CRF artificial extract.
Pharmacologic Action
The degeneration of dopaminergic neurons in the substantial nigra and the formation of Lewy bodies is a characteristic pathological change of PD. Therefore, promoting the release of dopamine and anti-apoptosis is an important method for alleviating the symptoms of PD. In addition, when the level of CRF expression in the cerebral cortex is significantly reduced, it is accompanied by microglia activation, which affects the loss of axonal terminals in dopaminergic neurons and promotes the deterioration of PD. By ingesting CRF (ovine) Trifluoroacetate, it can activate its receptor, and thereby activating the function of dopaminergic neurons, promoting the release of dopamine and the stability of microglia, and achieving the effect of alleviating PD.
Function
When CRF (ovine) Trifluoroacetate is ingested, the CRF component can activate its receptor, and its receptor can be divided into CRF receptor 1 and CRF receptor 2. Activation of these two receptors can regulate the degradation and release of dopamine; CRF receptor 1 activation has Helps the survival of dopaminergic neurons with anti-apoptotic effects; and CRF receptor 1 activation stimulates dopamine D2 and GABAB receptors, increasing the amplitude of inhibitory postsynaptic currents; for CRF receptor 2, it can be activated Acts on the glutamate NMDA receptor, promotes the release of dopamine in the midbrain, and reduces the excitatory neurotoxic effects of glutamate.
Pharmacokinetics and Metabolism
CRF (ovine) Trifluoroacetate is a CRF extracted from sheep, and its amino acid arrangement is highly similar to the CRF arrangement order in the human body, and there is a carboxyl terminal end in the form of an α-helix linkage, which can be well linked to the receptor. In addition, due to the high similarity of human CRF, its metabolism does not affect the human body. However, excessive CRF can cause mental illnesses such as depression, anxiety, and anorexia nervosa, so the dosage needs to be determined based on relevant test parameters.
References:
1. Zhang Di, Liu Chunna, Liu Xinyu, et al. Effects of neuropeptide urocortin II on spontaneous discharge and GLU neurotransmission in rat striatum neurons [J]. Chinese Pharmacological Bulletin, 2012,28: 1443-1447.
2. Var in M, Bentea E, Roosens S, et al. Involvement of CＲH receptors in the neuroprotective action of r-apomorphine in the striatal 6-OHDA rat model[J]. Neurosci Med,2013, 4: 299-318.
3. Abuirmeileh A, Harkavyi A, Kingsbury A, et al. The CＲF-like peptide urocortin greatly attenuates loss of extracellular striatal dopamine in rat models of Parkinson's disease by activating CRF(1) receptors[J]. Eur J Pharmacol, 2009, 604:45-50.
4. Beckstead MJ, Gantz SC, Ford CP, et al. CRF enhancement of GIRK channel-mediated transmission in dopamine neurons[J]. Neuropsychopharmacology, 2009, 34:1926-1935.
Zhou Rui, Hunag Dujiuan, et al. Advances in research on the function of CRF and its relationship with Parkinson's disease [J]. Chinese Journal of Neuroanatomy, 2017, 33(6): 58-762.
