methapyrilene

Small moleculeexperimental

Methapyrilene is an antihistamine and anticholinergic of the pyridine chemical class which was developed in the early 1950s. It was sold under the trade names Co-Pyronil and Histadyl EC. It has relatively strong sedative effects, to the extent that its primary use was as a medication for insomnia rather than for its antihistamine action. Together with scopolamine, it was the main ingredient in Sominex, Nytol, and Sleep-Eze. It also provided the sedative component of Excedrin PM. Manufacturers voluntarily withdrew methapyrilineb drug products from the market in May and June 1979, when methapyrilene was demonstrated to cause liver cancer in rats when given chronically. — NCATS

Clinical trial activity

1 trials · 1 clinical orgs · 0 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jan 1, 2017 (NCT02982642)

Timeline

No events for the selected filters.

Indications

Approved for

Hypersensitivity

Studied for

Cognitive Dysfunction · Phase 4

Mechanism of action

Histamine H1 receptorANTAGONIST
HRH1 antagonist
- Histamine H1 receptor (HRH1) ↗

Chemistry & pharmacology

Loading structure…

SMILES

Cl.CN(C)CCN(CC1=CC=CS1)C2=CC=CC=N2

Mol. weight: 297.847 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No

Oral

Parenteral

Topical

Sources

Also known as

1612
1612
2-[[2-(dimethylamino)ethyl]-2-thenylamino]pyridine
2-[[2-(dimethylamino)ethyl]-2-thenylamino]pyridine
metapyrilene
methapyrilene
methapyrilene
methapyrilene
methapyrilene
methapyrilene
methapyrilene
methapyrilene
methapyrilene
methapyrilene hcl
methapyrilene hcl
methapyrilene hcl
methapyrilene hydrochloride
methapyrilene hydrochloride
methapyrilene hydrochloride
methypyrilene
methypyrilene
n,n-dimethyl-n'-pyrid-2-yl-n'-2-thenylethylenediamine
n,n-dimethyl-n'-pyrid-2-yl-n'-2-thenylethylenediamine
paradormalene
pyrinistab
pyrinistol
thenylene
thenylene hcl
thenylpyramine
thenylpyramine
thenylpyramine
thenylpyramine hcl
thenylpyramine hcl

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT02982642	Phase 4	Jan 1, 2017	Peking University

Showing 1 of 1 trials

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Organizations

Research & Development (1)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Peking University	Academic/Hospital	1	1	1	2017

1 organizations

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