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| 化学名: | バソトシン | | 英語化学名: | Vasopressin | | 别名: | Vasopressin;Vasopressin acetate salt;TIANFU-CHEM Vasopressin;2H7]-Vasopressin acetate salt | | CAS番号: | 9034-50-8 | | 分子式: | C43H67N15O12S2 | | 分子量: | 1050.22 | | EINECS: | | | カテゴリ情報: | hormones | | Mol File: | Mol File | ![バソトシン]() |
| シーケンス | CYS-TYR-ILE-GLN-ASN-CYS-PRO-ARG-GLY-NH2 | | CAS データベース | 9034-50-8 |
| | バソトシン Usage And Synthesis |
| 解説 | バソプレッシン略称VP．下垂体後葉ホルモンの一つ．一般にウシまたはブタの凍結下垂体後葉から抽出して精製する．ウシや多くのほ乳類からのものはアルギニン-バソプレッシンといわれ，9個のアミノ酸からなるペプチドである．C46H65N15O12S2(1084.27)． "ブタからのものはアルギニンのかわりにリシンを含む．C47H65N13O12(1004.11)．バソプレッシンは抗利尿ホルモン(antidiuretic hormone， ADHと略称)ともいうように，作用の本質は尿細管の透過性を調節して尿量を調節することにある．ほかに末梢血管収縮作用，平滑筋収縮作用などが知られている．尿崩症の治療，手術時のショック症状の改善に用いられる． | | 説明 | Vasopressin, also called antidiuretic hormone (A D H) or arginine vasopressin
(AVP), is another hormone key to water homeostasis and blood pressure
regulation. A rginine vasopressin is produced in the neurones of the
hypothalamus and stored in vesicles within the posterior pituitary.
Vasopressin is released in response to increased blood osmolality detected
by hypothalamic osmoreceptors; systemic hypotension or hypovolaemia
detected by cardiopulmonary baroreceptors of the great veins and atria; or
angiotensin I I acting on the hypothalamus. | | 使用 | Vasopressin is a peptide hormone secreted by the hypothalamus via the
posterior pituitary. Its primary role is the regulation of body fluid balance. It
is secreted in response to hypotension and promotes retention of water by
action on specific cAMP-coupled V2 receptors. It causes vasoconstriction by
stimulating V1 receptors in VSM and is particularly potent in hypotensive
patients. It is increasingly used in the treatment of refractory vasodilatory
shock which is resistant to catecholamines. The vasopressin analogue
desmopressin is used to treat diabetes insipidus and in the management of
von Willebrand's disease. Terlipressin (another analogue) is used to limit
bleeding from oesophageal varices in patients with portal hypertension.
When used for the management of low SVR states, vasopressin is
administered as an i.v. infusion at a rate of 0.01–0.1 units min–1. | | 使用 | Hormone (antidiuretic). | | brand name | Pitressin
(Parke-Davis). | | 生物学の機能 | Human vasopressin, or Arg-vasopressin, is chemically very similar to oxytocin and therefore
sometimes is referred to as [Phe3, Arg8]oxytocin. The physiological role of
vasopressin is the regulation of water reabsorption in the renal tubules (an antidiuretic action,
thus often referred to as the antidiuretic hormone). In high doses, vasopressin promotes the
contraction of arterioles and capillaries, resulting in an increase in blood pressure, thus the
name vasopressin. An inadequate output of pituitary antidiuretic hormone can cause diabetes
insipidus, which is characterized by the chronic excretion of large amounts of pale urine and
results in dehydration and extreme thirst. | | 臨床応用 | lly as a long-lasting and selective V2aR agonist for the
treatment of central diabetes insipidus. For X-CNDI, the
use of nonpeptide antagonists (pharmacological chaperones) and nonpeptide agonists (vaptans) has been
tested. These cell-permeable reagents stabilize ERretained misfolded V2aR mutants, allowing the receptors
to reach the plasma membrane or to initiate a cAMP
response, leading to AQP2 translocation. Strategies
bypassing nonfunctional or mislocalized V2aR to induce
AQP2 translocation and phosphorylation have also been
tested. OPC41061 (V2aR antagonist, tolvaptan) has
been approved in the United States and Europe for the
treatment of hyponatraemia in SIADH. Recently, the
VP system (V1aR) was proposed as a novel therapeutic
target for castration-resistant prostate cancer. The
results of clinical trials to improve autism spectrum disorder by targeting the AVP/V1aR pathway have been
reported. | | 臨床応用 | The nonapeptide vasopressin is well known for its role on fluid metabolism, but it also is a
key regulator of the HPA axis. Stress stimulates the release of vasopressin in the pituitary gland, where it
strongly potentiates the effects of CRF on adrenocorticotropic hormone release. These findings suggest that HPA axis dysregulation in depression might be associated with
the development of centrally acting vasopressin receptor antagonists for the treatment of depression. |
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