protirelin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
thyrotropin releasing hormone analogues 2316 24305-27-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • protirelin tartrate
  • protirelin
  • lopremone
  • rifathyroin
  • rifotironin
  • TRH
  • Molecular weight: 362.39
  • Formula: C16H22N6O4
  • CLOGP: -2.79
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 4
  • TPSA: 150.28
  • ALOGS: -1.95
  • ROTB: 6

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 2 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Nov. 5, 1976 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC V04CJ02 VARIOUS
DIAGNOSTIC AGENTS
OTHER DIAGNOSTIC AGENTS
Tests for thyreoidea function
CHEBI has role CHEBI:77746 h. sapiens metabolites

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diagnostic Test for Thyroid Dysfunction indication
Pituitary Function Studies indication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.66 acidic
pKa2 13.44 acidic
pKa3 6.3 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Thyrotropin-releasing hormone receptor GPCR AGONIST Ki 7.70 CHEMBL CHEMBL
Thyrotropin-releasing hormone receptor GPCR Ki 8 CHEMBL
Protein Trhr2; Thyrotropin releasing hormone receptor 2; Thyrotropin-releasing hormone receptor 2 GPCR Ki 8 CHEMBL
Thyrotropin-releasing hormone receptor GPCR Ki 7.70 CHEMBL
Thyrotropin-releasing hormone receptor 2 Unclassified IC50 8.15 CHEMBL

External reference:

IDSource
4018469 VUID
N0000170390 NUI
D00176 KEGG_DRUG
53935-32-3 SECONDARY_CAS_RN
4018469 VANDF
C0040162 UMLSCUI
CHEBI:35940 CHEBI
CHEMBL1472 ChEMBL_ID
DB09421 DRUGBANK_ID
3335 INN_ID
5Y5F15120W UNII
638678 PUBCHEM_CID
2139 IUPHAR_LIGAND_ID
10580 RXNORM
5380 MMSL
d03679 MMSL
002111 NDDF
10534002 SNOMEDCT_US
412495007 SNOMEDCT_US
412496008 SNOMEDCT_US
73805002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Thyrotropin Releasing HormoneTRH HUMAN PRESCRIPTION DRUG LABEL 1 51808-209 SOLUTION 500 ug INTRAVENOUS Unapproved drug other 9 sections