Current review on the link between BH4 and pain.Latremoliere A, Costigan M. GCH1, BH4 and pain. Curr Pharm Biotechnol 2011 ; 12 : 1728-41.Latremoliere, A., and Costigan, M. (2011). GCH1, BH4 and pain. Curr. Pharm. Biotechnol. 12, 1728-1741....
多光子成像显示,术后肥大细胞与感觉神经末梢之间存在稳定的相互作用,表明肥大细胞可能通过释放BH4和血清素参与术后疼痛的调节。 研究还发现,肥大细胞特异性GCH1缺失小鼠表现出机械性和热性疼痛敏感性的显著降低,并伴随着足部BH4和血清素水平的减少。相反,GCH1过表达的小鼠在术后表现出更高的疼痛敏感性,且皮肤中血清素...
We explain the nature of the GCH1 reduced-function haplotype and set out the potential for a ‘BH4 blocking’ drug as a novel analgesic.Alban LatremoliereMichael CostiganotherLatremoliere A, Costigan M. GCH1, BH4 and pain. Curr Pharm Biotechnol 2011: 12: 1728-1741....
Studies assessing the role of GCH1 and BH4 in pain consist of human and animal studies, including DOPA-responsive dystonia (DRD) patients and hph-1 mice (a genetic mouse model of DRD) having mutations in the GCH1 gene as well as preclinical studies with the GCH1 inhibitor 2,4-diamino-6...
It was confirmed that the GCH1 targeting siRNA according to the present invention has the effect of reducing the concentration of BH4, a neurotransmitter produced by GCH1, by suppressing the mRNA and protein expression of GCH1. Accordingly, the GCH1-targeting siRNA according to the present ...
BH4 therapy has been studied in a Phase 2a clinical trial in SCD. The GCH1 association study with ACh dependent vasodilation in humans and animals suggests the need for additional studies to determine if polymorphisms in GCH1 and variability in BH4 synthesis modulates SCA pain, and if ...
Based on their roles in pain pathways, it is suggested that GTP cyclohydrolase, an enzyme that regulates the biosynthesis of the enzyme cofactor tetrahydobiopterin (BH4), is a modulator of peripheral neuropathic, inflammatory and even experimental pain in humans (Tegeder et al, Nature Med 2006)...