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pipazethate

Structure via PubChem · Public domain (PubChem)

EntityQ7197205· pop 5· linked from 290 articles

pipazethate

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Also known as D-254, SO-15874, Pipazetate, SK&F-70230-A

Pipazetate () (brand names Dipect, Lenopect, Selvigon, Theratuss, Toraxan), or pipazethate (), is a 1-azaphenothiazine drug that was briefly marketed as a cough suppressant. It binds to the sigma-1 receptor with an IC50 value of 190 nM. It also has local anesthetic action, and in large doses can produce seizures.

Chemical data

Formula
C21H25N3O3S
Molecular weight
399.5 g/mol
IUPAC name
2-(2-piperidin-1-ylethoxy)ethyl pyrido[3,2-b][1,4]benzothiazine-10-carboxylate
SMILES
C1CCN(CC1)CCOCCOC(=O)N2C3=CC=CC=C3SC4=C2N=CC=C4
InChIKey
DTVJXCOMJLLMAK-UHFFFAOYSA-N
XLogP
3.4
Polar surface area
80.2 Ų
H-bond donors
0
H-bond acceptors
6
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Phase 2
Molecule type
Small molecule
Indications
Cough

via ChEMBL · EBI

Research

24 papers

via PubMed

Wikidata facts

Mass
399.161663
Has use
medication
Show 4 more facts
defined daily dose
80
chemical formula
C₂₁H₂₅N₃O₃S
canonical SMILES
C1CCN(CC1)CCOCCOC(=O)N2C3=CC=CC=C3SC4=C2N=CC=C4
subject has role
antitussive
Sources (3)

via Wikidata · CC0

~1 min read

Encyclopedic overview

2 sections
Contents
  • Synthesis
  • References

Pipazetate () (brand names Dipect, Lenopect, Selvigon, Theratuss, Toraxan), or pipazethate (), is a 1-azaphenothiazine drug that was briefly marketed as a cough suppressant. It binds to the sigma-1 receptor with an IC50 value of 190 nM. It also has local anesthetic action, and in large doses can produce seizures.

As the brand name Theratuss, it was approved by the FDA in 1962, on evidence of safety only. It was withdrawn from the US market in 1972 when the manufacturer, Bristol Myers Squibb, failed to produce evidence of efficacy. Clinical studies showed that it did not decrease cough frequency at recommended dosages.

Excerpted from Wikipedia’s “pipazethate” article, available under the CC BY-SA 4.0 licence.

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