Molecule Information

General Information of the Molecule (ID: Mol01014)

• Name: Multidrug resistance protein 1 (ABCB1) ,Sus scrofa
• Synonyms: ABCB1; Fragment
• Molecule Type: Protein
• Gene Name: ABCB1
• Sequence:
  GQKKELERYNKNLEEAKRIGIKKAITANISIGAAFLLIYASYALAFWYGTTLVLSNEYTI
  GQVLTVFFSVLIGAFSVGQASPSIEAFANARGAAYEIFKIIDSKPSIDSYSKNGHKPDNI
  KGNLEFRNVHFSYPSRNEVKILKGLNLKVESGQTVALVGNSGCGKSTTVQLMQRLYDPTE
  GVVSIDGQDIRTINVRYLREIIGVVSQEPVLFATTIAENIRYGRENVTMEEIEKAVKEAN
  AYDFIMKLPNKFDTLVGERGAQLSGGQKQRIAIARALVRNPKILLLDEATSALDTESEAV
  VQVALDKAREGRTTIVIAHRLSTVRNADVIAGFDDGVIVEKGSHDELMKEKGVYFKLVTM
  QTKGNEIELENTVGVSKGVVDALDMSPKDLESSLIRRGSTRKSIKGPQGQDRKLSTKEGL
  DENVPPVSFWRILKLNITEWPYFVVGIFCAIINGGLQPAFSIIFSRIIGVFTKVTDPETK
  RQDSNIFSLLFLILGIISFITFFLQGFTFGKAGEILTKRLRYMVFRSMLRQDVSWFDDPK
  NTTGALTTRLANDAAQVKGAIGSRLAVITQNIANLGTGIIISFIYGWQLTLLLLAIVPII
  AIAGVVEMKMLSGQALKDKKELEGAGKIATEAIENFRTVVSLTREEKFESMYDQSLQVPY
  SNSLRKAHIFGITFSITQAMMYFSYAACFRFGAYLVQHGHMDFQDVLLVFSAIVFGAMAV
  GQVSSFAPDYAKAKVSASHVIMIIEKTPQIDSYSTVGLKPNTVEGNLTFNEVMFNYPTRP
  DIPVLQGLSLEVKKGQTLALVGSSGCGKSTVVQLLERFYDPLAGKVLIDGREIKELNVQW
  LRAHMGIVSQEPILFDCSIAENIAYGDNSRVVSQEEIVQAAKEANIHPFIETLPDKYNTR
  VGDKGTQLSGGQKQRIAIARALVRRPRILLLDEATSALDTESEKVVQEALDKAR
• Uniprot ID: Q5MIZ9_PIG

Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Artiodactyla
Family: Suidae
Genus: Sus
Species: Sus scrofa

Type(s) of Resistant Mechanism of This Molecule

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Drug

Approved Drug(s) 3 drug(s) in total

Chlorpromazine

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Disease Class: Psychosis [1]

• Sensitive Disease: Psychosis [ICD-11: 6D8Z.0]
• Sensitive Drug: Chlorpromazine
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: L-MDR1 cells(Sus scrofa (Pig)); Kidney; Homo sapiens (Human); CVCL_0391
• In Vitro Model: LLC-Pk1 cells(Sus scrofa (Pig)); Kidney; Homo sapiens (Human); CVCL_0391
• Experiment for Drug Resistance: Flow cytometric assay
• Mechanism Description: The multidrug resistance transporter, P-glycoprotein (P-gp), is involved in efflux transport of several antipsychotics in the blood-brain barrier (BBB). All the antipsychotics showed various degrees of inhibitory effects on P-gp activity at concentrations ranging from 1 to 100 uM. However, risperidone and olanzapine are the most likely agents that may inhibit P-gp activity.

Clozapine

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Disease Class: Psychosis [1]

• Sensitive Disease: Psychosis [ICD-11: 6D8Z.0]
• Sensitive Drug: Clozapine
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: L-MDR1 cells(Sus scrofa (Pig)); Kidney; Homo sapiens (Human); CVCL_0391
• In Vitro Model: LLC-Pk1 cells(Sus scrofa (Pig)); Kidney; Homo sapiens (Human); CVCL_0391
• Experiment for Drug Resistance: Flow cytometric assay
• Mechanism Description: The multidrug resistance transporter, P-glycoprotein (P-gp), is involved in efflux transport of several antipsychotics in the blood-brain barrier (BBB). All the antipsychotics showed various degrees of inhibitory effects on P-gp activity at concentrations ranging from 1 to 100 uM. However, risperidone and olanzapine are the most likely agents that may inhibit P-gp activity.

Haloperidol

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Disease Class: Psychosis [1]

• Sensitive Disease: Psychosis [ICD-11: 6D8Z.0]
• Sensitive Drug: Haloperidol
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: L-MDR1 cells(Sus scrofa (Pig)); Kidney; Homo sapiens (Human); CVCL_0391
• In Vitro Model: LLC-Pk1 cells(Sus scrofa (Pig)); Kidney; Homo sapiens (Human); CVCL_0391
• Experiment for Drug Resistance: Flow cytometric assay
• Mechanism Description: The multidrug resistance transporter, P-glycoprotein (P-gp), is involved in efflux transport of several antipsychotics in the blood-brain barrier (BBB). All the antipsychotics showed various degrees of inhibitory effects on P-gp activity at concentrations ranging from 1 to 100 uM. However, risperidone and olanzapine are the most likely agents that may inhibit P-gp activity.

References

• Ref 1: Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.