Guancydine
(Synonyms: 胍西定,Guancidine) 目录号 : GC34608
Guancydine(Guancidine)是一种抗高血压剂。
Cas No.:1113-10-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Guancydine (Guancidine) is an antihypertensive agent[1].
[1]. Clark DW, et al. Guancydine: a new antihypertensive agent. Use with quinethazone and guanethidine or propranolol. Ann Intern Med. 1972 Apr;76(4):579-85.
| Cas No. | 1113-10-6 | SDF | |
| 别名 | 胍西定,Guancidine | ||
| Canonical SMILES | N=C(NC(C)(C)CC)NC#N | ||
| 分子式 | C7H14N4 | 分子量 | 154.21 |
| 溶解度 | DMSO : ≥ 125 mg/mL (810.58 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 6.4847 mL | 32.4233 mL | 64.8466 mL |
| 5 mM | 1.2969 mL | 6.4847 mL | 12.9693 mL |
| 10 mM | 0.6485 mL | 3.2423 mL | 6.4847 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Guancydine, a new hypotensive agent with complex action
Cor Vasa 1977;19(3):214-9.PMID:562730doi
Guancydine (1-cyano-3-tert-amylguanidine) lowered within normal limits the tensional values in an interval of four hours after its administration in eight out of nine hypertensive patients under experiment. The hypotensive effect of a single oral dose of 500-750 mg persists for about 6-7 hours after its administration. Guancydine does not impair the vasopressor response to angiotensin II but reduces the action of this peptide on the excretion of water, Na, K and Ca through urine. The hypotensive effect of Guancydine is associated with a decrease of platelet adhesiveness and an activation of fibrinolysis. In view of this fact, Guancydine might play a role in the prophylaxis of complications of arterial hypertension - atherosclerosis and trombosis. The increase of venous blood oxygenation after Guancydine could be attributed to the opening of arterio-venous shunts or to the reduction of tissular extraction of oxygen. Guancydine does not seem to be toxic. It produced, in some patients, slight headache and orthostatic hypotension, especially during the first hours after administration.
Effect of Guancydine on systemic and renal hemodynamics in arterial hypertension
Mayo Clin Proc 1977 Jun;52(6):383-6.PMID:325301doi
The effect of Guancydine (1-cyano-3-tert-amylguanidine) on systemic and renal hemodynamics was studied in nine patients with arterial hypertension. Antihypertensive drugs were withheld for 15 days before beginning the investigation. Average sodium intake was 105 meq/24 hours in some patients and 25 meq/24 hours in others. Patients received placebo during a control period that averaged 14 days. Guancydine was given for 7 to 18 days at an average dose of 21 mg/kg of body weight. Although mean arterial blood pressure decreased significantly in all patients, it reached normal levels in only two. There was no change in cardiac output. Glomerular filtration rate and renal plasma flow remained unchanged, whereas urinary sodium excretion diminished, suggesting an activation of the renin-angiotensin-aldosterone system. A substantial gain in body weight was noted. Nausea, vomiting, constipation, somnolence, restlessness, mental confusion, asthenia, and urine retention were observed. The anti-angiotensin effect of Guancydine that has been described in animals was not observed.
Synthesis and hypotensive activity of N-alkyl-N"-cyano-N'-pyridylguanidines
J Med Chem 1978 Aug;21(8):773-81.PMID:691003DOI:10.1021/jm00206a011.
A variety of N-alkyl-N'-pyridyl-N"-cyanoguanidines III was prepared as potential bioisosteres of hypotensive N-alkyl-N'-pyridylthioureas Ia. Optimal activity of the N,N'-disubstituted cyanoguanidines III was assoicated with the presence of four to seven carbon branched alkyl and 3- or 4-pyridyl groups. Maximum potency was displayed by N-tert-pentyl-N'-3 pyridyl-N"-cyanoguanidine (20). This compound proved to be 200 times more potent than the corresponding thiourea in hypertensive rats and dogs. In comparison with Guancydine, which is the de-3-pyridyl analogue of 20, a 150-fold increase of potency in spontaneously hypertensive rats was obtained with 20 and its tert-butyl analogue 19. The observed activity appears to be due to direct vascular relaxation. On a weight basis compounds 19, 20, 50, and 101 compared favorably with hydralazine.
Sequential method for combined screening antihypertensive and diuretic agents in the same spontaneously hypertensive rat (SHR)
Clin Exp Hypertens (1978) 1979;1(6):817-30.PMID:551899DOI:10.3109/10641967909068641.
A combined method for detecting compounds with antihypertensive and diuretic activity simultaneously in the same spontaneously hypertensive (SH) rat is described. The present method, utilizing the advantages of sequential probability test analysis, the spontaneously hypertensive rats and the direct measurement of arterial blood pressure, proves to be feasible and efficient in detecting both activities. This ia s 3-stage sequential test requires one to three rats per compound. One adult SH rat was dosed by gavage with compound at 100 mg/kg, p.o. and loaded with 0.9% NaCl at 25 ml/kg, p.o. at 0-hr. The rat was put in a metabolism cage. The 0-5 hr. urine was collected and urinary Na+, K+ and CL- were determined. A second identical dose was given without NaCl loading at 24-hr. Mean arterial blood pressure (MABP) of conscious rats was measured directly by fermoral-iliac artery puncture at 28-hr. The criteria to accept, retest or reject a compound were based on the testing of known antihypertensives and diuretics. A 2nd and 3rd rat may be needed for a test compound depending on the outcome of the MABP and urinary electrolytes of the 1st rat. Based on MABP, Guancydine, hydralazine, clonidine, reserpine, alpha-methyldopa, guanethidine and parglyine were accepted as active. Based on urinary sodium excretion, furosemide, quinethazone, acetazolamide, hydrochlorothiazide, metolazone, triamterene and clonidine were accepted as active.
Current therapy of hypertension. A pharmacologic approach
Am J Med 1975 Apr;58(4):489-94.PMID:235841DOI:10.1016/0002-9343(75)90121-7.
Adequate treatment of hypertension requires that the physician understand the pharmacologic actions of antihypertensive agents. Although no drug is without adverse reactions, it should be possible to choose an agent or combination of agents which can effectively lower blood pressure and be tolerated by the patient. The indications, proposed mechanisms of actions and adverse effects of the following antihypertensive drugs are discussed: thiazide diuretics, spironolactone, triamterene, trimethaphan, Rauwolfia alkaloids. guanethidine, bethanidine, methyldopa, clonidine, pargyline, propranolol, hydrazaline, minoxidil, Guancydine, diazoxide and sodium nitroprusside.