General Information of Drug (ID: DMYH9SU)

Drug Name
batrachotoxin Drug Info
Synonyms
BATRACHOTOXIN; UNII-TSG6XHX09R; TSG6XHX09R; Batrachotoxinin A, 20-(2,4-dimethyl-1H-pyrrole-3-carboxylate); Betrachotoxinin A, 20-alpha-(2,4-dimethyl-1H-pyrrole-3-carboxylate); 23509-16-2; GTPL2619; LS-24727; Betrachotoxinin A, 20-alpha-(2,4-dimethyl-1H-pyrrole-3-carboxylate) (9CI)
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
6324647
CAS Number
CAS 23509-16-2
TTD Drug ID
DMYH9SU
VARIDT Drug ID
DR01019

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Patented Agent(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lanperisone DM4EGPN Musculoskeletal disorder FA00-FC0Z Phase 3 [10]
SIPATRIGINE DMMQ4GC Neurological disorder 6B60 Discontinued in Phase 2 [11]
V-102862 DMR2EUV N. A. N. A. Discontinued in Phase 1 [12]
veratridine DMUF8JZ Discovery agent N.A. Investigative [5]
BW-202W92 DMFKXMT Discovery agent N.A. Investigative [11]
CCNCSSKWCRDHSRCC DMBGHTW Discovery agent N.A. Investigative [13]
CCNCSSKWCRAHSRCC DM96YR2 Discovery agent N.A. Investigative [13]
CCACSSKWCRDHSRCC DMSE20Y Discovery agent N.A. Investigative [13]
CCNCASKWCRDHSRCC DMRFA5O Discovery agent N.A. Investigative [13]
ZNCCNCSSKWCRDHSRCC DMY2V37 Discovery agent N.A. Investigative [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
XEN-402 DMR69CG Osteoarthritis FA00-FA05 Phase 2 [14]
PF-05089771 DMD74BJ Chronic pain MG30 Phase 2 [15]
BIIB074 DMLV1ET Bipolar disorder 6A60 Phase 2 [16]
DSP-2230 DM0WTMD Neuropathic pain 8E43.0 Phase 1 [16]
BIIB095 DMUC6EP Pain MG30-MG3Z Phase 1 [16]
GDC0310 DMUNFEP Chronic pain MG30 Phase 1 [17]
DSP-3905 DMYHU24 Neuropathic pain 8E43.0 Phase 1 [16]
PF-05241328 DM2NTBL Pain MG30-MG3Z Phase 1 [18]
DWJ-208 DMQKDJZ Cancer related pain MG30 Phase 1 [16]
RG7893 DM1R4MQ Pain MG30-MG3Z Phase 1 [19]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
veratridine DMUF8JZ Discovery agent N.A. Investigative [20]
aconitine DMFOZ60 Discovery agent N.A. Investigative [20]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mephenytoin DM5UGDK Epilepsy 8A60-8A68 Approved [21]
Mexiletine DMCTE9R Ventricular tachycardia BC71 Approved [22]
Fosphenytoin DMOX3LB Epilepsy 8A60-8A68 Approved [21]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [22]
LOMERIZINE DME0TC8 Migraine 8A80 Approved [23]
Tetrodotoxin DMWMPRG Bacterial infection 1A00-1C4Z Approved [24]
Dyclonine DMU6OFP Pain MG30-MG3Z Approved [25]
Moricizine DMOMBJW Arrhythmia BC9Z Approved [26]
Ethotoin DMXWOCP Complex partial seizure 8A68.0 Approved [27]
Prilocaine DMI7DZ2 Pain MG30-MG3Z Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rilpivirine DMJ0QOW Human immunodeficiency virus infection 1C62 Approved [28]
Ropivacaine DMSPJG2 Anaesthesia 9A78.6 Approved [29]
Bupivacaine DM4PRFC Anaesthesia 9A78.6 Approved [29]
Tiapride DMN6CAG Alcohol dependence 6C40.2 Approved [30]
Tetracaine DM9J6C2 Spinal anesthesia MB40.3 Approved [31]
Proparacaine DMLS39E Anaesthesia 9A78.6 Approved [29]
Conatumumab DM2UOSN Colorectal cancer 2B91.Z Phase 2 [32]
VX-150 DMGDB21 Neuropathic pain 8E43.0 Phase 2 [17]
DSP-2230 DM0WTMD Neuropathic pain 8E43.0 Phase 1 [16]
PF-01247324 DM93LMS Pain MG30-MG3Z Phase 1 [33]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
US9694002, 495 DMV1OR0 N. A. N. A. Patented [34]
US9694002, 59 DM804T5 N. A. N. A. Patented [34]
US9694002, 129 DMMCNVO N. A. N. A. Patented [34]
veratridine DMUF8JZ Discovery agent N.A. Investigative [2]
Drug Name Drug ID Indication ICD 11 Highest Status REF
NBI-921352 DMTTW9V Epileptic encephalopathy 8A62 Phase 2 [35]
XEN901 DMRP9YF Epilepsy 8A60-8A68 Phase 1 [16]
PRAX-330 DMHIS3M Epilepsy 8A60-8A68 Phase 1 [17]
veratridine DMUF8JZ Discovery agent N.A. Investigative [7]
4,9-anhydro-tetrodotoxin DMEKI1B Discovery agent N.A. Investigative [36]
Drug Name Drug ID Indication ICD 11 Highest Status REF
LIDOFLAZINE DMV23GL Angina pectoris BA40 Approved [37]
Aryl carboxamide derivative 1 DMTZRCW N. A. N. A. Patented [38]
Aryl carboxamide derivative 2 DM146TA N. A. N. A. Patented [38]
Pyrimidine derivative 1 DMN9VQM N. A. N. A. Patented [38]
Pyrrolo-pyridinone derivative 6 DMXGNP8 N. A. N. A. Patented [38]
Pyrrolo-pyridinone derivative 5 DMK2FSY N. A. N. A. Patented [38]
SIPATRIGINE DMMQ4GC Neurological disorder 6B60 Discontinued in Phase 2 [39]
U-92032 DMTYO3P N. A. N. A. Terminated [40]
PD-85639 DMNUKB4 N. A. N. A. Terminated [37]
veratridine DMUF8JZ Discovery agent N.A. Investigative [4]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
SCN1A messenger RNA (SCN1A mRNA) TTANOZH SCN1A_HUMAN Activator [2]
Voltage-gated sodium channel alpha Nav1.2 (SCN2A) TTLJTUF SCN2A_HUMAN Activator [3]
Voltage-gated sodium channel alpha Nav1.3 (SCN3A) TTAXZ0K SCN3A_HUMAN Activator [4]
Voltage-gated sodium channel alpha Nav1.4 (SCN4A) TT84DRB SCN4A_HUMAN Activator [5]
Voltage-gated sodium channel alpha Nav1.5 (SCN5A) TTZOVE0 SCN5A_HUMAN Activator [6]
Voltage-gated sodium channel alpha Nav1.6 (SCN8A) TT54ERL SCN8A_HUMAN Activator [7]
Voltage-gated sodium channel alpha Nav1.7 (SCN9A) TT4G2JS SCN9A_HUMAN Activator [8]
Voltage-gated sodium channel alpha Nav1.8 (SCN10A) TT90XZ8 SCNAA_HUMAN Activator [9]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2619).
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 578).
3 Interaction of batrachotoxin with the local anesthetic receptor site in transmembrane segment IVS6 of the voltage-gated sodium channel. Proc Natl Acad Sci U S A. 1998 Nov 10;95(23):13947-52.
4 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 580).
5 Point mutations in segment I-S6 render voltage-gated Na+ channels resistant to batrachotoxin. Proc Natl Acad Sci U S A. 1998 Mar 3;95(5):2653-8.
6 Binding of [3H]batrachotoxinin A benzoate to specific sites on rat cardiac sodium channels. Mol Pharmacol. 1986 Dec;30(6):617-23.
7 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 583).
8 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 584).
9 The poison Dart frog's batrachotoxin modulates Nav1.8. FEBS Lett. 2004 Nov 5;577(1-2):245-8.
10 Tolperisone-type drugs inhibit spinal reflexes via blockade of voltage-gated sodium and calcium channels. J Pharmacol Exp Ther. 2005 Dec;315(3):1237-46.
11 Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. J Med Chem. 2009 May 14;52(9):2694-707.
12 3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers. J Med Chem. 2004 Mar 11;47(6):1547-52.
13 Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels. J Biol Chem. 2007 Oct 19;282(42):30699-706.
14 Treatment of Na(v)1.7-mediated pain in inherited erythromelalgia using a novel sodium channel blocker. Pain. 2012 Jan;153(1):80-5.
15 Primary erythromelalgia: a review. Orphanet J Rare Dis. 2015 Sep 30;10:127.
16 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
17 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
18 Recent progress in sodium channel modulators for pain. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9.
19 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800041740)
20 Binding of batrachotoxinin A 20-alpha-benzoate to a receptor site associated with sodium channels in synaptic nerve ending particles. J Biol Chem. 1981 Sep 10;256(17):8922-7.
21 Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68.
22 Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9.
23 Medicinal chemistry of neuronal voltage-gated sodium channel blockers. J Med Chem. 2001 Jan 18;44(2):115-37.
24 Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81.
25 Monoamine transporter and sodium channel mechanisms in the rapid pressor response to cocaine. Pharmacol Biochem Behav. 1998 Feb;59(2):305-12.
26 From first class to third class: recent upheaval in antiarrhythmic therapy--lessons from clinical trials. Am J Cardiol. 1996 Aug 29;78(4A):28-33.
27 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
28 Structures of muO-conotoxins from Conus marmoreus. I nhibitors of tetrodotoxin (TTX)-sensitive and TTX-resistant sodium channels in mammalian senso... J Biol Chem. 2004 Jun 11;279(24):25774-82.
29 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
30 Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
31 Heterologous expression and functional analysis of rat Nav1.8 (SNS) voltage-gated sodium channels in the dorsal root ganglion neuroblastoma cell line ND7-23. Neuropharmacology. 2004 Mar;46(3):425-38.
32 Pathobiology of visceral pain: molecular mechanisms and therapeutic implications. II. Genetic approaches to pain therapy. Am J Physiol Gastrointest Liver Physiol. 2000 Apr;278(4):G507-12.
33 Oral Administration of PF-01247324, a Subtype-Selective Nav1.8 Blocker, Reverses Cerebellar Deficits in a Mouse Model of Multiple Sclerosis. PLoS One. 2015; 10(3): e0119067.
34 Substituted benzamides and methods of use thereof. US9694002.
35 Clinical pipeline report, company report or official report of Neurocrine Biosciences
36 The TTX metabolite 4,9-anhydro-TTX is a highly specific blocker of the Na(v1.6) voltage-dependent sodium channel. Am J Physiol Cell Physiol. 2007 Aug;293(2):C783-9.
37 Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. J Med Chem. 1994 Jan 21;37(2):268-74.
38 Sodium channel blockers: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015 Mar;25(3):279-90.
39 Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. J Med Chem. 2002 Aug 15;45(17):3755-64.
40 Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a ... J Med Chem. 2000 Sep 7;43(18):3372-6.