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Penfluridol

Penfluridol structure

CAS No:
26864-56-2
Formula:
C28H27ClF5NO
Chemical Name:
Penfluridol
Synonyms:
4-Piperidinol,1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-;4-Piperidinol,1-[4,4-bis(p-fluorophenyl)butyl]-4-(4-chloro-α,α,α-trifluoro-m-tolyl)-;1-[4,4-Bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol;Penfluridol;1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-α,α,α-trifluoro-m-tolyl)-4-piperidinol;R 16341;McN-JR 16341;Semap
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

Penfluridol is a highly potent, first generation diphenylbutylpiperidine antipsychotic.

1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol is a diarylmethane.|One of the long-acting ANTIPSYCHOTIC AGENTS used for maintenance or long-term therapy of SCHIZOPHRENIA and other PSYCHOTIC DISORDERS.

Penfluridol Basic Attributes

Molecular Weight：

523.97

Exact Mass：

523.97

EC Number：

248-074-5

UNII：

25TLU22Q8H

NSC Number：

759179

DSSTox ID：

DTXSID5049021

ATC Code：

N05AG03|N - Nervous system

HScode：

2942000000

Characteristics

PSA：

23.5

XLogP3：

7.3

Appearance：

white powder

Density：

1.3±0.1 g/cm3

Melting Point：

106 °C

Boiling Point：

587.7°C at 760 mmHg

Flash Point：

309.2±30.1 °C

Refractive Index：

1.553

Water Solubility：

H2O: insoluble

Storage Conditions：

2-8°C

Toxicity：

LD50 orally in mice (day 7): 86.8 mg/kg (Janssen)

Collision Cross Section：

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

Safety Information

Hazard category：

6.1

Transport codes：

UN 2811 6.1/PG 3

wgk germany：

hazard class code：

safety instructions：

RTECS Number：

TN6957000

Marks：

Precautionary statement(s)：

P301 + P310

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P321, P330, P405, and P501|Aggregated GHS information provided by 39 companies from 1 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)|Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)

MeSH Entry Terms：

Penfluridol

Penfluridol Use and Manufacturing

Methods of Manufacturing

In a 500 ml three-necked reaction flask equipped with a mechanical stirrer, a condenser, a thermometer and a calcium chloride drying tube, Add 250ml of anhydrous ether, 2.4g (0.0631mol) of lithium aluminum tetrahydrate, start stirring, 20 g (0.0372 mol) of amide (6) was added, and the reaction was completed at 38 ° C for 6 hours.After completion of the reaction, 4.2 ml of water was added for 25 minutes, And then 5.4 ml of a 20percent by weight solution of sodium hydroxide was added for 20 minutes, In 15.2 minutes with 14.2 ml of water;The decomposition product was filtered and the filtrate (ether) was dried over anhydrous potassium carbonate. The filter cake was washed with a small amount of ether.The filtrate and lotion added to the distillation flask, atmospheric pressure distillation recovery ether, vacuum dry, 100 ml of a mixed solvent [chloroform: petroleum ether (60-90 ° C) = 1: 4, weight ratio, Hot filtration, the filtrate at about 10 ° C static crystallization, to be natural precipitation crystallization frozen at -5 ° C overnight, filtration, The filter cake is washed with the mixed solvent, drained and dried at 70 DEG C under normal pressure to constant weight, (I), m.p 105-107 ° C, yield 81.5percent.

Uses

antineoplastic

Use Classification：

Pharmaceuticals

Computed Properties

Molecular Weight:524.0
XLogP3:7.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:7
Exact Mass:523.1701330
Monoisotopic Mass:523.1701330
Topological Polar Surface Area:23.5
Heavy Atom Count:36
Complexity:647
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

The antipsychotic effect is related to its blocking of dopamine receptors in the brain. It can also block the α-adrenaline receptors in the nervous system. The antipsychotic effect is strong and long-lasting, and can last for several days to a week after a single oral dose. It also has an antiemetic effect, but the sedative effect is weak and the effect on cardiovascular function is relatively mild.

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

Penfluridol Tablets
Ingredients	The main ingredient of this product is pentafluridol, whose chemical name is 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol
Indication	When this product is used in combination with ethanol or other central nervous system depressants, the central depressant effect is enhanced. When this product is used in combination with antihypertensive drugs, there is an increased risk of orthostatic hypotension.
Specifications	20mg
Manufacturer	Longhui Phamaceufical Co., Ltd.

Penfluridol Tablets
Ingredients	The main ingredient of this product is pentafluridol, whose chemical name is 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol
Indication	When this product is used in combination with ethanol or other central nervous system depressants, the central depressant effect is enhanced. When this product is used in combination with antihypertensive drugs, there is an increased risk of orthostatic hypotension.
Specifications	20mg
Manufacturer	Renhetang Pharmaceutical Co., Ltd.

Penfluridol Tablets
Ingredients	The main ingredient of this product is penfluridol. Its chemical name is 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol.
Indication	1. When this product is used in combination with ethanol or other central nervous system depressants, the central depressant effect is enhanced. 2. When this product is used in combination with antihypertensive drugs, there is a risk of increased orthostatic hypotension. 3. When this product is used in combination with other antipsychotic drugs, there is a risk of extrapyramidal reactions.
Specifications	20 mg
Manufacturer	Jiangsu Nhwa Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

Hunan Middle-South Pharmaceutical Co., Ltd.

China
Active
Jiangsu Nhwa-Sede Pharm. Co., Ltd.

China
Active
AMPHASTAR NANJING PHARMACEUTICALS INC (ANP) AN AMPHASTAR CO

United States
Active

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