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Urapidil hydrochloride

Urapidil hydrochloride structure

CAS No:
64887-14-5
Formula:
C20H30ClN5O3
Chemical Name:
Urapidil hydrochloride
Synonyms:
6[[3-[4-(O-METHOXYPHENYL)-1-PIPERAZINYL]PROPYL]AMINO]-1,3-DIMETHYLURACIL HYDROCHLORIDE;6-[[3-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]PROPYL]AMINO]-1,3-DIMETHYL-2,4(1H,3H)-PYRIMIDINEDIONE;6-[[3-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]PROPYL]AMINO]-1,3-DIMETHYL-2,4(1H,3H)-PYRIMIDINEDIONE HYDROCHLORIDE;URAPIDIL HCL;URAPIDIL HYDROCHLORIDE;URAPIDIL HYDROCHLORIDE A1 ADRENOCEPTOR A NTAG;6-[[3-[4-(2-Methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyluracil hydrochloride;6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propylamino]-1,3-dimethyl-pyrimidine-2,4-dione hydrochloride
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist.Target: α1-adrenoceptor; 5-HT1A receptorUrapidil hydrochloride is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT1A receptors in the central nervous system [1]. Urapidil

Urapidil hydrochloride Basic Attributes

Molecular Weight：

423.94

Exact Mass：

423.203705

UNII：

PVU92PZO12

NSC Number：

758226

DSSTox ID：

DTXSID2045812

HScode：

3004909090

Characteristics

PSA：

68.4

XLogP3：

1.59470

Appearance：

white solid

Melting Point：

156-1580C

Boiling Point：

549°C at 760 mmHg

Flash Point：

285.8ºC

Water Solubility：

H2O: soluble

Storage Conditions：

Desiccate at RT

Collision Cross Section：

192.1 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

22-36/37/38

safety instructions：

26-36

RTECS Number：

YQ9862000

Marks：

Precautionary statement(s)：

P264, P270, P301+P312, P330, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 39 companies from 1 notifications to the ECHA C&L Inventory.

Urapidil hydrochloride Use and Manufacturing

a1-Adrenergic antagonist; derivative of Uracil. Antihypertensive

Computed Properties

Molecular Weight:423.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:7
Exact Mass:423.2037175
Monoisotopic Mass:423.2037175
Topological Polar Surface Area:68.4
Heavy Atom Count:29
Complexity:588
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is quickly absorbed orally, and the blood concentration reaches the peak in 4 to 6 hours. It is extensively metabolized in the liver, mainly hydroxylation, and the para-hydroxy compound (M1) produced accounts for 50%, which is inactive. The aromatic ring ortho-demethylated compound (M2) and uracil ring N-demethylated compound (M3) are trace amounts and have biological activity like the original drug. After oral absorption, 80% of this product is bound to protein, and most of the metabolites and 10% to 20% of the original drug are excreted through the kidneys, and the rest is excreted through the feces. Oral T1/2 is 4.7 hours, and intravenous T1/2 is 2.7 hours.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Urapidil Hydrochloride Injection
Ingredients	Ingredients: Urapidil hydrochloride. Chemical name: 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione hydrochloride.
Indication	1 Urapidil injection cannot be mixed with alkaline liquids, as its acidic nature may cause solution turbidity or floc formation. 2 The antihypertensive effect of this product can be enhanced when used with antihypertensive drugs or drinking alcohol. 3 The blood concentration of this product can be increased by 15% when used with cimetidine. 4 There is currently insufficient information to indicate that this product can be used with angiotensin-converting enzyme inhibitors, so it is not recommended to use it with angiotensin-converting enzyme inhibitors. If other antihypertensive drugs are used at the same time, drinking alcohol or the patient has hypovolemia, such as diarrhea and vomiting, the antihypertensive effect of urapidil injection can be enhanced.
Specifications	10ml: 50mg (based on urapidil)
Manufacturer	Xi'an Lijun Pharmaceutical Co.Limited

Urapidil Hydrochloride
Manufacturer	Xi'an Lijun Pharmaceutical Co.Limited

Urapidil Hydrochloride Injection

See More Related Drugs

Registered Holders

Yuanda Medical Nutrition Science (Wuhan) Co., Ltd.

China
Active
Shandong Chenghuishuangda Pharmaceutical Co., Ltd.

China
Active
Hanrui Pharmaceutical (Jingmen) Co., Ltd.

China
Active

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