Drug Information

Drug (ID: DG00898) and It's Reported Resistant Information

• Name: Picrotoxin
• Synonyms: PICROTOXIN; Cocculin; Cocculus; Oriental berry; Indian berry; Fish berry; Coques du levant; Picrotoxinum; 124-87-8; Picrotoxine; Picrotox; Picrotin, compd. with picrotoxinin (1:1); UNII-ZLT174DL7U; Coques du levant [French]; Caswell No. 663A; Picrotoxinin - picrotin; Picrotoxin [NF]; HSDB 6385; Picrotoxinin, compd. with picrotin (1:1); Picrotin, compound with picrotoxinin (1:1); ZLT174DL7U; EINECS 204-716-6; EPA Pesticide Chemical Code 002301; NSC 403139; AI3-17689; GTPL4051; SCHEMBL16319990; DB00466; BP166191; Q416602; 3,6-Methano-8H-1,5,7-trioxacyclopenta(ij)cycloprop(a)azulene-4,8(3H)-dione, hexahydro-2a-hydroxy-9-(1-hydroxy-1-methylethyl)-8b-methyl-, (1aR,2aR,3S,6R,6aS,8aS,8bR,9S)-, compd. with (1aR,2aR,3S,6R,6aS,8aS,8bR,9R)-hexahydro-2a-hydroxy-8b-methyl-9-(1-methylethenyl)-3,6-methano-8H-1,5,7-trioxacyclopenta(ij)cycloprop(a)azulene-4,8(3H)-dione (1:1)
• Indication:
  In total 1 Indication(s)
  Respiratory distress syndrome [ICD-11: CB00]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Brain cancer [ICD-11: 2A00]; [1]
• Target: GABA(A) receptor alpha-1 (GABRA1); GBRA1_HUMAN; [1]
• Formula: C30H34O13
• IsoSMILES: CC(=C)[C@@H]1C2[C@@H]3[C@@]4([C@](C1C(=O)O2)(CC5[C@]4(O5)C(=O)O3)O)C.C[C@@]12[C@H]3C4[C@H](C([C@@]1(C[C@@H]5[C@]2(O5)C(=O)O3)O)C(=O)O4)C(C)(C)O
• InChI: 1S/C15H18O7.C15H16O6/c1-12(2,18)6-7-10(16)20-8(6)9-13(3)14(7,19)4-5-15(13,22-5)11(17)21-9;1-5(2)7-8-11(16)19-9(7)10-13(3)14(8,18)4-6-15(13,21-6)12(17)20-10/h5-9,18-19H,4H2,1-3H3;6-10,18H,1,4H2,2-3H3/t5-,6+,7 ,8 ,9-,13-,14-,15+;6 ,7-,8 ,9 ,10+,13+,14+,15-/m10/s1
• InChIKey: VJKUPQSHOVKBCO-ZTYBEOBUSA-N
• PubChem CID: 31304
• TTD Drug ID: D0KR9U
• VARIDT ID: DR00640
• DrugBank ID: DB00466

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Brain cancer [ICD-11: 2A00]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Gamma-aminobutyric acid receptor subunit alpha-1 (GABAARs) [1]

• Molecule Alteration: Function; Inhibition
• Resistant Disease: Neuroblastoma [ICD-11: 2A00.11]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: SH-1-V7 cells; Esophagus; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: Whole-cell patch-clamp recording assay
• Experiment for Drug Resistance: Slice whole-cell recording
• Mechanism Description: Receptors containing Delta T6'Y had marginally weaker sensitivity to positive allosteric modulators, likely a secondary consequence of differing GABA sensitivity. Overexpression of DeltaT6'Y in neurons resulted in robust PTX-insensitive IPSCs, suggesting that Delta-containing receptors are readily recruited by synaptically released GABA.

References

• Ref 1: Pharmacological and Biophysical Characteristics of Picrotoxin-Resistant, Delta Subunit-Containing GABA(A) Receptors .Front Synaptic Neurosci. 2021 Nov 18;13:763411. doi: 10.3389/fnsyn.2021.763411. eCollection 2021. 10.3389/fnsyn.2021.763411