Product Name :
Guanabenz (hydrochloride)
Description:
Guanabenz is an orally active α2-adrenoceptor agonist with hypotensive effects . 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 . 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 . Guanabenz competed for imidazoline I2-binding sites in brown adipose tissue with Ki of 97 nM . 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.{{Ketoconazole} MedChemExpress|{Ketoconazole} Bacterial|{Ketoconazole} Biological Activity|{Ketoconazole} Formula|{Ketoconazole} custom synthesis|{Ketoconazole} Epigenetic Reader Domain} 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 .
CAS:
23113-43-1
Molecular Weight:
267.54
Formula:
C8H9Cl3N4
Chemical Name:
N-[(E)-[(2,6-dichlorophenyl)methylidene]amino]guanidine hydrochloride
Smiles :
Cl.NC(=N)N/N=C/C1C(Cl)=CC=CC=1Cl
InChiKey:
UNWWUUPHJRAOMZ-GAYQJXMFSA-N
InChi :
InChI=1S/C8H8Cl2N4.ClH/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12;/h1-4H,(H4,11,12,14);1H/b13-4+;
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Pritelivir} web|{Pritelivir} Anti-infection|{Pritelivir} Technical Information|{Pritelivir} References|{Pritelivir} supplier|{Pritelivir} Epigenetic Reader Domain}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Guanabenz is an orally active α2-adrenoceptor agonist with hypotensive effects . 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 . 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 .PMID:23756629 Guanabenz competed for imidazoline I2-binding sites in brown adipose tissue with Ki of 97 nM . 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 .|Product information|CAS Number: 23113-43-1|Molecular Weight: 267.54|Formula: C8H9Cl3N4|Chemical Name: N-[(E)-[(2,6-dichlorophenyl)methylidene]amino]guanidine hydrochloride|Smiles: Cl.NC(=N)N/N=C/C1C(Cl)=CC=CC=1Cl|InChiKey: UNWWUUPHJRAOMZ-GAYQJXMFSA-N|InChi: InChI=1S/C8H8Cl2N4.ClH/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12;/h1-4H,(H4,11,12,14);1H/b13-4+;|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|