Zaidi M, Breimer L H, MacIntyre I
Royal Postgraduate Medical School, London.
Q J Exp Physiol. 1987 Oct;72(4):371-408. doi: 10.1113/expphysiol.1987.sp003084.
Despite being products from the same gene, there is clearly a marked divergence in the distribution and physiological role of calcitonin and CGRP. Whereas calcitonin is predominantly distributed in the thyroid, CGRP is abundant in the nervous system throughout the body. Though the peptides have only weak structural homologies, a generally similar conformation enables them to interact at each other's receptors. Hence the pharmacological effects of the peptides faintly resemble one another. Calcitonin receptors are mainly found on osteoclasts and at certain sites in the nervous system. CGRP binding sites are abundant in the cerebellum and blood vessels. Calcitonin is a circulating hormone controlling osteoclastic activity. CGRP acts as a neurotransmitter or neuromodulator centrally, and released from perivascular nerve terminals, it modulates arteriolar tone. Released from motoneurones, CGRP may also play a trophic role regulating the muscle acetylcholine receptor state. The next decade should establish the physiological role of CGRP and the regulation of the expression of the calcitonin/CGRP gene complex.
尽管降钙素和降钙素基因相关肽(CGRP)是来自同一基因的产物,但它们在分布和生理作用上显然存在显著差异。降钙素主要分布在甲状腺,而CGRP在全身的神经系统中含量丰富。尽管这两种肽只有微弱的结构同源性,但总体相似的构象使它们能够与彼此的受体相互作用。因此,这两种肽的药理作用有微弱的相似之处。降钙素受体主要存在于破骨细胞和神经系统的某些部位。CGRP结合位点在小脑和血管中丰富。降钙素是一种控制破骨细胞活性的循环激素。CGRP在中枢作为神经递质或神经调节剂起作用,从血管周围神经末梢释放后,它调节小动脉张力。从运动神经元释放后,CGRP也可能在调节肌肉乙酰胆碱受体状态方面发挥营养作用。未来十年应该能明确CGRP的生理作用以及降钙素/CGRP基因复合体表达的调控机制。