METHYPRYLON

Details

Stereochemistry	RACEMIC
Molecular Formula	C10H17NO2
Molecular Weight	183.2475
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCC1(CC)C(=O)NCC(C)C1=O

InChI

InChIKey=SIDLZWOQUZRBRU-UHFFFAOYSA-N

InChI=1S/C10H17NO2/c1-4-10(5-2)8(12)7(3)6-11-9(10)13/h7H,4-6H2,1-3H3,(H,11,13)

HIDE SMILES / InChI

Description
Sources: https://www.drugs.com/mmx/methyprylon.html

Methyprylon (brand name Noludar) is a sedative agent, which used to treat insomnia. But then the drug was replaced in the market by another drugs with less side effects. The precise mechanism of action is not known, but was made suggestion, that methyprylon increases the effects of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the brain.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; anion channel 202 Target ID: CHEMBL2093872 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16792	Positive Allosteric Modulator 179

Conditions

Condition	Modality	Targets	Highest Phase	Product
Insomnia 108 Sources: https://www.drugs.com/mmx/methyprylon.html	Primary		Approved 8429	NOLUDAR Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
5.62 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2866242	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		METHYPRYLON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
74.75 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2866242	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		METHYPRYLON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
9.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2866242	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		METHYPRYLON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
30 g single, oral Overdose Dose: 30 g Route: oral Route: single Dose: 30 g Co-administed with:: dimenhydrinate(one hundred 50-mg capsules) Sources: https://pubmed.ncbi.nlm.nih.gov/5897795	unhealthy, 36 years n = 1 Health Status: unhealthy Age Group: 36 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/5897795	Other AEs: Comatose... Other AEs: Comatose (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/5897795

AEs

AE	Significance	Dose	Population
Comatose	1 patient	30 g single, oral Overdose Dose: 30 g Route: oral Route: single Dose: 30 g Co-administed with:: dimenhydrinate(one hundred 50-mg capsules) Sources: https://pubmed.ncbi.nlm.nih.gov/5897795	unhealthy, 36 years n = 1 Health Status: unhealthy Age Group: 36 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/5897795

Sourcing

Vendor/Aggregator	ID	URL
ABI Chem	AC1L1HJV
Alfa Chemistry	125-64-4	https://www.alfa-chemistry.com/cas_125-64-4.htm
Ambinter	Amb17594728	http://www.ambinter.com/reference/17594728
Aurora Fine Chemicals LLC	A06.787.840	http://online.aurorafinechemicals.com/info?ID=A06.787.840
Chemieliva Pharmaceutical Co., Ltd	PBCM0178614
Compound Cloud	4162
Enamine	BBV-38270220
Enamine	BBV-77645600
Enamine	BBV-77665348
MuseChem	I007969	https://www.musechem.com/product/I007969.html
NovoSeek	4162
Smolecule	S535265	http://www.smolecule.com/products/s535265
THE BioTek	bt-275775	https://www.thebiotek.com/product/inhibitors/bt-275775
Toronto Research Chemicals	KIT8630
Toronto Research Chemicals	M338670
ZINC	ZINC000003831106	http://zinc15.docking.org/substances/ZINC000003831106
ZINC	ZINC000003831107	http://zinc15.docking.org/substances/ZINC000003831107
mcule	MCULE-5210305552

PubMed

Title	Date	PubMed
Pharmacokinetics of methyprylon following a single oral dose.	1985 Sep	2866242

Patents

Sample Use Guides

In Vivo Use Guide

300 mg once a day before bedtime.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

METHYPRYLON

Official Name

English

methyprylon [INN]

Common Name

English

METHYPRYLON [HSDB]

Common Name

English

METHYPRYLON [ORANGE BOOK]

Common Name

English

METHYPRYLON [JAN]

Common Name

English

NOLUDAR

Brand Name

English

NSC-30442

Code

English

METHYPRYLON [MI]

Common Name

English

METHYPRYLONE

Common Name

English

Methyprylon [WHO-DD]

Common Name

English

METHYPRYLON [MART.]

Common Name

English

3,3-Diethyl-5-methyl-2,4-piperidinedione

Systematic Name

English

METHYPRYLON [VANDF]

Common Name

English

2,4-PIPERIDINEDIONE, 3,3-DIETHYL-5-METHYL-

Systematic Name

English

Classification Tree Code System Code

WHO-VATC

QN05CE02