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

Stem definitionDrug idCAS RN
1688 60-89-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • mepazine
  • mepazin
  • mepazine base
  • meprazine
  • mesapin
  • nothiazine
  • pecazine
  • mepazine acetate
major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd
  • Molecular weight: 310.46
  • Formula: C19H22N2S
  • CLOGP: 5.27
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -4.69
  • ROTB: 2

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

None

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Dermatographic urticaria indication 7632005 DOID:743
Angioedema indication 41291007 DOID:1558
General anesthesia indication 50697003
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Sneezing indication 76067001
Urticaria indication 126485001
Itching of skin indication 418363000
Allergic conjunctivitis indication 473460002 DOID:11204
Alcoholism contraindication 7200002
Organophosphate poisoning contraindication 8260003
Weight gain finding contraindication 8943002
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Chronic disease of respiratory system contraindication 17097001
Myocardial infarction contraindication 22298006 DOID:5844
Glaucoma contraindication 23986001 DOID:1686
Orthostatic hypotension contraindication 28651003
Torsades de pointes contraindication 31722008
Parkinsonism contraindication 32798002
Conduction disorder of the heart contraindication 44808001
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Extrapyramidal disease contraindication 76349003
Hyperglycemia contraindication 80394007 DOID:4195
Epilepsy contraindication 84757009 DOID:1826
Leukopenia contraindication 84828003 DOID:615
Stupor contraindication 89458003
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Acute disease of cardiovascular system contraindication 128487001
Angina pectoris contraindication 194828000
Disease of liver contraindication 235856003 DOID:409
Metabolic syndrome X contraindication 237602007 DOID:14221
Hyperprolactinemia contraindication 237662005 DOID:12700
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Coma contraindication 371632003
At risk for aspiration contraindication 371736008
Visual impairment contraindication 397540003
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.07 Basic
pKa2 3.55 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
Alpha-2A adrenergic receptor GPCR Ki 6.26 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.12 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.73 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.96 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 6.49 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.59 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 6.07 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.74 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.17 DRUG MATRIX
Histamine H1 receptor GPCR Ki 8.50 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 7.72 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 6.70 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 7.40 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 7.72 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 7.55 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 7.24 DRUG MATRIX
FAD-linked sulfhydryl oxidase ALR Enzyme AC50 7.01 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 7.47 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 6.41 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 6.84 CHEMBL

External reference:

IDSource
D02607 KEGG_DRUG
9663002 SNOMEDCT_US
001484 NDDF
CHEMBL395110 ChEMBL_ID
PH34873A38 UNII
523 INN_ID
CHEBI:135324 CHEBI
6075 PUBCHEM_CID
CHEMBL1712842 ChEMBL_ID
9782 IUPHAR_LIGAND_ID
C100190 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None