PICAMILON

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H12N2O3
Molecular Weight	208.2139
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)CCCNC(=O)C1=CC=CN=C1

InChI

InChIKey=NAJVRARAUNYNDX-UHFFFAOYSA-N

InChI=1S/C10H12N2O3/c13-9(14)4-2-6-12-10(15)8-3-1-5-11-7-8/h1,3,5,7H,2,4,6H2,(H,12,15)(H,13,14)

HIDE SMILES / InChI

Molecular Formula	C10H12N2O3
Molecular Weight	208.2139
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.rlsnet.ru/tn_index_id_5545.htm

Picamilon (also known as N-nicotinoyl-GABA, Pycamilon, and Pikamilon) is a drug formed by a synthetic combination of niacin and GABA. It was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA. Picamilon permeated the blood-brain barrier and then is hydrolyzed into GABA and niacin. The released GABA, in theory, would activate GABA receptors potentially producing an anxiolytic response. The second released component, niacin, is a vasodilator. Today picamilon is sold in Russia as a prescription drug and is used for the treatment of a variety of illnesses and disorders, ranging from depression to a migraine, neuro infections, senile psychosis, certain types of glaucoma, and even acute alcohol intoxication. As of 2015, the FDA classified picamilon as a substance that does not meet the requirements of a dietary supplement and is therefore no longer permitted to be sold in the United States.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; anion channel 203 Target ID: CHEMBL2093872 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6529802	Agonist 2752

Conditions

Condition	Modality	Highest Phase	Product
Ischemic stroke 35 Sources: https://www.rlsnet.ru/tn_index_id_5545.htm	Primary	Approved 8583	Пикамилон Approved Use Indication of the drug Picamylon Violations of cerebral circulation (acute ischemic, subacute and recovery periods of ischemic stroke, chronic cerebral circulatory failure), vegetovascular dystonia, asthenia, depression, senile psychosis; alcoholism (the period of withdrawal), acute alcohol intoxication, migraine, craniocerebral trauma, neuroinfections, primary open-angle glaucoma (for stabilization of visual function).
Vegetovascular dystonia 2 Sources: https://www.rlsnet.ru/tn_index_id_5545.htm	Primary	Approved 8583	Пикамилон Approved Use Indication of the drug Picamylon Violations of cerebral circulation (acute ischemic, subacute and recovery periods of ischemic stroke, chronic cerebral circulatory failure), vegetovascular dystonia, asthenia, depression, senile psychosis; alcoholism (the period of withdrawal), acute alcohol intoxication, migraine, craniocerebral trauma, neuroinfections, primary open-angle glaucoma (for stabilization of visual function).
Depression 240 Sources: https://www.rlsnet.ru/tn_index_id_5545.htm	Primary	Approved 8583	Пикамилон Approved Use Indication of the drug Picamylon Violations of cerebral circulation (acute ischemic, subacute and recovery periods of ischemic stroke, chronic cerebral circulatory failure), vegetovascular dystonia, asthenia, depression, senile psychosis; alcoholism (the period of withdrawal), acute alcohol intoxication, migraine, craniocerebral trauma, neuroinfections, primary open-angle glaucoma (for stabilization of visual function).
Alcoholism 20 Sources: https://www.rlsnet.ru/tn_index_id_5545.htm	Primary	Approved 8583	Пикамилон Approved Use Indication of the drug Picamylon Violations of cerebral circulation (acute ischemic, subacute and recovery periods of ischemic stroke, chronic cerebral circulatory failure), vegetovascular dystonia, asthenia, depression, senile psychosis; alcoholism (the period of withdrawal), acute alcohol intoxication, migraine, craniocerebral trauma, neuroinfections, primary open-angle glaucoma (for stabilization of visual function).

C_max

Value	Dose	Analyte	Population
667 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1551 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2971 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1106 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2230 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4284 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1.46 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.46 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.46 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20359966/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	PICAMILON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

PubMed

Title	Date	PubMed
Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States.	2016 Mar-Apr	26426301

Patents

Sample Use Guides

In Vivo Use Guide

cerebrovascular diseases - 0,02-0,05 g 2-3 times for 1-2 months; depression - on 0,04-0,2 g in 2-3 receptions in day within 1,5-3 months; as an anti-asthenic and tranquilizing agent - 0,04-0,08 g per day, in some cases - up to 0,2-0,3 g per day for 1-1,5 months; alcoholism: 0.1-0.15 g per day (course - 6-7 days)

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:54:06 GMT 2025` Edited by `admin` on `Mon Mar 31 19:54:06 GMT 2025`
Record UNII	0S5N9SEK4N
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

PICAMILON

Common Name

English

NICOTINOYL-GABA

Preferred Name

English

PIKATROPIN

Common Name

English

PIKAMILONE

Common Name

English

PYCAMILON

Common Name

English

NICOTINOYL-.GAMMA.-AMINOBUTYRIC ACID

Systematic Name

English

4-(PYRIDINE-3-CARBONYLAMINO)BUTANOIC ACID

Systematic Name

English

BUTANOIC ACID, 4-((3-PYRIDINYLCARBONYL)AMINO)-

Systematic Name

English

PIKAMILON

Common Name

English

Classification Tree Code System Code

DSLD

2497 (Number of products:99)