| CAS NO: | 23113-43-1 |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| Storage | Store at -20°C |
| M.Wt | 267.5 |
| Cas No. | 23113-43-1 |
| Formula | C8H8Cl2N4·HCl |
| Synonyms | Wytensin |
| Solubility | ≥4.3 mg/mL in H2O; ≥4.37 mg/mL in EtOH; ≥9.25 mg/mL in DMSO |
| Chemical Name | 2-[(2,6-dichlorophenyl)methylene]-hydrazinecarboximidamide, monohydrochloride |
| Canonical SMILES | ClC1=C(/C=N/NC(N)=N)C(Cl)=CC=C1.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Guanabenz is an orally active α2-adrenoceptor agonist with hypotensive effects [1]. The α2 adrenergic receptors belong to a family of G protein-coupled receptor (GPCR), mediate many physiological actions of the endogenous catecholamines adrenaline and noradrenaline. The α2-adrenoceptor agonists have been currently used as antihypertensives and as veterinary sedative anaesthetics. They have also been used experimentally in humans as adjuncts to anaesthesia, as spinal analgesics, and to treat opioid, nicotine and alcohol dependence and withdrawal [2].
In vitro: Maximum concentrations of guanabenz in plasma (1.2 to 5.2 ng/ml) reached 2 to 5 hours after administration of capsules containing 16 or 32 mg of 14C-labelled guanabenz. Guanabenz was 90% bound to human plasma proteins [1]. Guanabenz competed for imidazoline I2-binding sites in brown adipose tissue with Ki of 97 nM [3].
Clinical trials: Guanabenz has undergone trials in patients with mild to moderate hypertension. The dosage was in the range of 8 to 64 mg daily, the majority of patients being controlled on up to 32 mg/day. Guanabenz was an effective antihypertensive agent in about 70% of patients in double-blind placebo-controlled trials. Guanabenz (16 to 64mg) produced a similar response rate. The most frequent side effects of guanabenz were drowsiness, dry mouth, dizziness and weakness, and such effects may lead to discontinuation of therapy in some patients [1].
References:
[1] Holmes B, Brogden R N, Heel R C, et al. Guanabenz[J]. Drugs, 1983, 26(3): 212-229.
[2] Aantaa R, Marjam ki A, Scheinin M. Molecular pharmacology of α2-adrenoceptor subtypes[J]. Annals of medicine, 1995, 27(4): 439-449.
[3] Rmer L, Wurster S, Savola J M, et al. Identification and characterization of the imidazoline I2b-binding sites in the hamster brown adipose tissue as a study model for imidazoline receptors[J]. Archives of physiology and biochemistry, 2003, 111(2): 159-166.
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