ESERIDINE SALICYLATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C15H21N3O3.C7H6O3
Molecular Weight	429.4663
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)C1=CC=CC=C1O.CNC(=O)OC2=CC3=C(C=C2)N(C)[C@H]4ON(C)CC[C@@]34C

InChI

InChIKey=ANZYOGDQEPQZOI-SLHAJLBXSA-N

InChI=1S/C15H21N3O3.C7H6O3/c1-15-7-8-17(3)21-13(15)18(4)12-6-5-10(9-11(12)15)20-14(19)16-2;8-6-4-2-1-3-5(6)7(9)10/h5-6,9,13H,7-8H2,1-4H3,(H,16,19);1-4,8H,(H,9,10)/t13-,15-;/m0./s1

HIDE SMILES / InChI

Description
Sources: http://jpet.aspetjournals.org/content/46/4/375 | https://www.google.co.ug/patents/WO1993003041A1 | https://www.fda.gov/ohrms/dockets/dockets/98n0182/nom004a.pdf

Eseridine (Geneserine) has been known for many years as an anticholinergic agent and used in therapy as a gastrointestinal antispastic. Eseridine salicylate is an inhibitor of cholinesterase activity that has been given by mouth in preparations for dyspepsia and other gastric disorders. It has also been studied for the treatment of Alzheimer’s disease.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Acetylcholinesterase 209 Target ID: CHEMBL220 Sources: https://www.fda.gov/ohrms/dockets/dockets/98n0182/nom004a.pdf \| https://www.drugs.com/international/eseridine.html \| https://www.google.co.ug/patents/WO1993003041A1	Inhibitor 8504		100.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Dyspepsia 11 Sources: http://www.doctissimo.fr/medicament-GENESERINE-3.htm http://en.pharmacodia.com/web/drug/1_11986.html	Primary		Approved 8583	GENESERINE Approved Use Dyspepsia

Doses

Dose	Population	Adverse events
4.5 mg 3 times / day multiple, oral Recommended Dose: 4.5 mg, 3 times / day Route: oral Route: multiple Dose: 4.5 mg, 3 times / day Sources: https://sante.lefigaro.fr/medicaments/3555951-geneserine-4-5mg-cpr-30	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: https://sante.lefigaro.fr/medicaments/3555951-geneserine-4-5mg-cpr-30	Sources: https://sante.lefigaro.fr/medicaments/3555951-geneserine-4-5mg-cpr-30

PubMed

Title	Date	PubMed
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.	2002-08-15	12166941
Geneserine and geneseroline revisited: acid-base catalyzed equilibria of hexahydropyrrolo-[2,3-b]-indole N-oxides with hexahydro-1,2-oxazino-[5,6-b]-indoles.	1989-03-01	2746259
[Studies of the effect of geneserine, carbamoyl-choline and acetyl-beta-methyl-choline and other related substances on the thyroid gland of the guinea pig].	1959	13663363
[Determination of geneserine in pharmaceutical solutions].	1958-03-01	13550058

Patents

Sample Use Guides

In Vivo Use Guide

Adult: 30 to 45 drops, 3 times a day, preferably taken 1/2 hour before main meals.

Route of Administration: Oral

In Vitro Use Guide

Geneserine hydrochloride inhibited human Acetylcholinesterase with IC50 value of 100 nM.

Name

Type

Language

ESERIDINE SALICYLATE

Common Name

English

1,2-OXAZINO(6,5-B)INDOL-6-OL, 2,3,4,4A,9,9A-HEXAHYDRO-2,4A,9-TRIMETHYL-, METHYLCARBAMATE (ESTER), (4AS,9AS)-, MONO(2-HYDROXYBENZOATE) (SALT)

Preferred Name

English

BENZOIC ACID, 2-HYDROXY-, COMPD. WITH (4AS,9AS)-2,3,4,4A,9,9A-HEXAHYDRO-2,4A,9-TRIMETHYL-1,2-OXAZINO(6,5-B)INDOL-6-YL METHYLCARBAMATE (1:1)

Systematic Name

English

GENESERINE SALICYLATE

Common Name

English

GENESERINE, SALICYLATE

Common Name

English

BENZOIC ACID, 2-HYDROXY-, COMPD. WITH (4AS-CIS)-2,3,4,4A,9,9A-HEXAHYDRO-2,4A,9-TRIMETHYL-1,2-OXAZINO(6,5-B)INDOL-6-YL METHYLCARBAMATE (1:1)

Common Name

English

Eseridine salicylate [WHO-DD]

Common Name

English

GENESERINE, SALICYLATE (1:1)

Common Name

English

Code System Code Type Description

CAS

5995-96-0