U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C5H7N3
Molecular Weight 109.1294
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMIFAMPRIDINE

SMILES

c1c[nH]cc(c1=N)N

InChI

InChIKey=OYTKINVCDFNREN-UHFFFAOYSA-N
InChI=1S/C5H7N3/c6-4-1-2-8-3-5(4)7/h1-3H,7H2,(H2,6,8)

HIDE SMILES / InChI

Description

vesicles, which in turn enhances neuromuscular transmission. Amifampridine phosphate has been granted Orphan Drug Designation and Breakthrough Therapy designation by the FDA for the treatment of Lambert-Eaton Myasthenic Syndrome (LEMS).

CNS Activity

CNS Penetrant
2415
Curator's Comment:: Amifampridine (3,4-DAP) displays toxicity largely due to blood-brain-barrier (BBB) penetration.

Originator

Approval Year

2018
97
Targets

Targets

Primary TargetPharmacologyConditionPotency
Blocker
504
Lambert-Eaton myasthenic syndrome
 2 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
voltage-gated potassium channel activity
Approved
7997
Firdapse

Approved Use

Symptomatic treatment of Lambert-Eaton myasthenic syndrome (LEMS) in adults.

Launch Date

1261526400000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
59.1 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
40.6 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
189 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
3-N-ACETYL-AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
268 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
3-N-ACETYL-AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
117 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
109 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
1220 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
3-N-ACETYL-AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
1444 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
3-N-ACETYL-AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.5 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.28 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
4.03 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
3-N-ACETYL-AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
4.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26101174/
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
3-N-ACETYL-AMIFAMPRIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
100 mg 1 times / day multiple, oral
Highest studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Other AEs: Paresthesia, Dysesthesia...
Other AEs:
Paresthesia (69%)
Dysesthesia (69%)
Oral dysesthesia (69%)
Abdominal pain (25%)
Upper abdominal pain (25%)
Dyspepsia (17%)
Dizziness (12%)
Nausea (10%)
Back pain (8%)
Hypoesthesia (6%)
Muscle spasms (6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Other AEs: Convulsion, Head titubation...
Other AEs:
Convulsion (0.6%)
Head titubation (0.6%)
Tremor (0.6%)
Unresponsive to stimuli (0.6%)
Small cell lung cancer (0.6%)
Metastases to central nervous system (0.6%)
Lung cancer metastatic (0.6%)
Pulmonary mass (0.6%)
Bradycardia (0.6%)
Pneumonia (0.6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Nausea 10%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Dizziness 12%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Dyspepsia 17%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Abdominal pain 25%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Upper abdominal pain 25%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Hypoesthesia 6%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Muscle spasms 6%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Dysesthesia 69%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Oral dysesthesia 69%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Paresthesia 69%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Back pain 8%
10 mg 3 times / day multiple, oral
Recommended
Dose: 10 mg, 3 times / day
Route: oral
Route: multiple
Dose: 10 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209321s000lbl.pdf
Bradycardia 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Convulsion 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Head titubation 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Lung cancer metastatic 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Metastases to central nervous system 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Pneumonia 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Pulmonary mass 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Small cell lung cancer 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Tremor 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Unresponsive to stimuli 0.6%
75 mg 1 times / day multiple, oral
Studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209321Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1172

inducer
657
inhibitor
1318
inhibitor
1421
inhibitor
1360

OverviewOther

Other InhibitorOther SubstrateOther Inducer
Kv1.3
16

Kv1.5
25

P-gp
1089

OATP1B3
613

CYP1A2
1268

CYP2A6
594

CYP2B6
679

CYP2C8
761

CYP2C19
1215

CYP2E1
761
P-gp
1223

CYP450
58

FMO
29
CYP1A2
618

CYP2B6
486
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OATP1B3
622
 no [Inhibition 30 uM]
CYP1A2
1406
 no
3-N-acetyl-BMN125
2
CYP1A2
1406
 no
CYP2A6
625
 no
CYP2B6
845
 no
3-N-acetyl-BMN125
2
CYP2B6
845
 no
CYP2C19
1277
 no
CYP2C8
810
 no
CYP2C9
1362
 no
CYP2D6
1455
 no
CYP2E1
841
 no
CYP3A4
1462
 no
3-N-acetyl-BMN125
2
CYP3A4
1462
 no
Kv1.3
31
 no
3-N-acetyl-BMN125
2
Kv1.5
40
 no
3-N-acetyl-BMN125
2
P-gp
1255
 no
Kv1.5
40
 yes [IC50 490.9 uM]
Kv1.3
31
 yes [IC50 524.8 uM]
CYP1A2
1406
 yes
CYP2B6
845
 yes
CYP3A4
1462
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP450
58
 no
FMO
29
 no
P-gp
1223
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1392
hERG
1392
3-N-acetyl-BMN125
2
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
NO22778
1PlusChem LLC
1P003IW5
A2B Chem
AB63653
AA Blocks
AA003ICP
AK Scientific
L421
AbovChem LLC
AC290039
AbovChem LLC
HY-14946
Aceschem
ACS010096
Achemo BB
AC-11438
Acros Organics
11239
Alfa Chemistry
A12465
Alinda
ALBB-005969
Ambeed
A101083
Ampyridine
AM11000
Apollo Scientific
OR6459
Aromalake
LS00018
AstaTech
CL0116
BLDpharm
BD9613
BOC Sciences
54-96-6
Beijing Acemol Technology
AMPD00217
Bide Pharmatech
BD9613
BioSynth
J-610017
BioSynth
W-105592
BlocksMatrix Scientific
11183
Bosche Scientific
D5650
Capot Chemical
1295
Chem Scene
CS-2778
ChemDiv
BB01-6065
ChemShuttle
107211
Chemik
CHHZ03300
Combi-Blocks
OR-1325
Compound Cloud
5918
Compound Cloud
9920716
Coresyn
CM14022
Debye Scientific
DB-011105
Enamine
BBV-42303146
Enamine
EN300-69695
Fluorochem
212979
Fluorochem
43674
Hairui
HR1295
Hangzhou Yuhao Chemical Technology
LQ0029
Heteroz
9425
IBScreen
BB_SC-03135
Indofine
CS-251
Innovapharm
BBS-00025688
Innovapharm
BBV-00004732
KeyOrganics
PS-9273
Lab Network
LN00007606
Lab Seeker
SC-05267
Lan Pharmatech
LQT-B01192
Life Chemicals
F0001-1409
MedChem Express
HY-14946
MolPort
MolPort-000-139-949
Molcore
CS22778
Molnova
M18788
MuseChem
I002172
MuseChem
I002177
NCI Plated 2007
521760
Nanjing Pope Bio-tech
NSTH-D10707
Norris Pharm
NSTH-D10707
Oakwood
43674
PI Chemicals
PI-16569
Pharmeks
PHBB_SC-03315
Selleck Chemicals
S4622
Sigma Aldrich
D7148
Sigma Aldrich
D7148|ALDRICH
Specs
AC-907/34116043
SpiroChem
SPC-g158
StruChem
SC-05267
SynQuest
53179
SynQuest
G311-A-33
Synthonix
P24217
TargetMol
T4497
Tetrahedron
TS02530
TimTec
SBB004341
TimTec
ST50946583
Vitas-M Laboratory
BBL013269
Vitas-M Laboratory
STK503647
W&J PharmaChem
50A146595
Wonderchem
WD03OU5
ZINC
ZINC000000164000
http://zinc15.docking.org/substances/ZINC000000164000
eMolecules
498389
eNovation Chemicals
D497406
mcule
MCULE-5478459845
PubMed

PubMed

TitleDatePubMed
[Lambert-Eaton myasthenic syndrome: diagnosis and treatment].
2001 Nov
Effect of 3,4-diaminopyridine on the gravity dependence of ocular drift in downbeat nystagmus.
2004 Aug 24
Electrophysiological and pharmacological characterization of K+-currents in muscle fibres isolated from the ventral sucker of Fasciola hepatica.
2004 Dec
Visceral periadventitial adipose tissue regulates arterial tone of mesenteric arteries.
2004 Sep
Effect of 3,4-diaminopyridine on the postural control in patients with downbeat nystagmus.
2005 Apr
NCAM 180 acting via a conserved C-terminal domain and MLCK is essential for effective transmission with repetitive stimulation.
2005 Jun 16
Cognitive deficits in aged rats correlate with levels of L-arginine, not with nNOS expression or 3,4-DAP-evoked transmitter release in the frontoparietal cortex.
2005 Mar
Taicatoxin inhibits the calcium-dependent slow motility of mammalian outer hair cells.
2005 May
Fetal exposure to 3,4-diaminopyridine in a pregnant woman with congenital myasthenia syndrome.
2006 Apr
Pre- and post-synaptic abnormalities associated with impaired neuromuscular transmission in a group of patients with 'limb-girdle myasthenia'.
2006 Aug
Inotropic effects of the K+ channel blocker 3,4-diaminopyridine: differential responses of rat soleus and extensor digitorum longus.
2006 Dec
Guidelines for the treatment of autoimmune neuromuscular transmission disorders.
2006 Jul
Available treatment options for the management of Lambert-Eaton myasthenic syndrome.
2006 Jul
Potassium channel blockers in multiple sclerosis: neuronal Kv channels and effects of symptomatic treatment.
2006 Jul
The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction.
2006 Jun
No benefit of 3,4-diaminopyridine in essential tremor: a placebo-controlled crossover study.
2006 Jun 13
[Fatigue and episodic exhaustion as a feature of multiple sclerosis].
2006 Mar
Treatment of the gravity dependence of downbeat nystagmus with 3,4-diaminopyridine.
2006 Sep 12
Altered diaphragm muscle action potentials in Zucker diabetic fatty (ZDF) rats.
2006 Sep 28
The therapy of congenital myasthenic syndromes.
2007 Apr
Childhood myasthenia: clinical subtypes and practical management.
2007 Aug
Beneficial effects of 3,4-diaminopyridine on positioning downbeat nystagmus in a circumscribed uvulo-nodular lesion.
2007 Aug
[Successful treatment of a Lambert-Eaton myasthenic syndrome patient with 3,4-diaminopyridine].
2007 Aug 10
Stability studies of ionised and non-ionised 3,4-diaminopyridine: hypothesis of degradation pathways and chemical structure of degradation products.
2007 Jan 4
Myasthenia gravis and Lambert-Eaton myasthenic syndrome in the same patient.
2007 Jul
[Treatment of Lambert-Eaton syndrome with 3,4- diaminopyridine and pyridostigmine].
2007 Jul-Aug
Potassium initiates vasodilatation induced by a single skeletal muscle contraction in hamster cremaster muscle.
2007 Jun 1
Neuromuscular paralysis and recovery in mice injected with botulinum neurotoxins A and C.
2007 May
Molecular docking study of the binding of aminopyridines within the K+ channel.
2007 May
Long-lasting in vivo inotropic effects of the K(+) channel blocker 3,4-diaminopyridine during fatigue-inducing stimulation.
2008 Dec
[Pharmacotherapy of central oculomotor disorders].
2008 Dec
[Lambert-Eaton Myasthenic Syndrome associated with vocal cord carcinoma].
2008 Jan
Inotropic effects of the K+ channel blocker 3,4-diaminopyridine on fatigued diaphragm muscle.
2008 Jan 1
Autoantibodies in neuromuscular transmission disorders.
2008 Jul
Onset dynamics of type A botulinum neurotoxin-induced paralysis.
2008 Jun
Mechanisms of neuromodulation as dissected using Sr2+ at motor nerve endings.
2008 Jun
L-type Ca2+ channel function is linked to dystrophin expression in mammalian muscle.
2008 Mar 12
Therapeutic strategies in congenital myasthenic syndromes.
2008 Oct
Brain structural and functional abnormalities in mood disorders: implications for neurocircuitry models of depression.
2008 Sep
Lambert-Eaton myasthenic syndrome: search for alternative autoimmune targets and possible compensatory mechanisms based on presynaptic calcium homeostasis.
2008 Sep 15
[A case of Lambert-Eaton myasthenic syndrome with small cell lung cancer, treated with 3,4-diaminopyridine].
2009 Jan
[Treatment approach to congenital myasthenic syndrome in a patient with acetylcholine receptor deficiency].
2009 Jan
Skeletal muscle contraction-induced vasodilator complement production is dependent on stimulus and contraction frequency.
2009 Jul
Efficacy of 3,4-diaminopyridine and pyridostigmine in the treatment of Lambert-Eaton myasthenic syndrome: a randomized, double-blind, placebo-controlled, crossover study.
2009 Jul
Mutations in LAMB2 causing a severe form of synaptic congenital myasthenic syndrome.
2009 Mar
3,4-Diaminopyridine is more effective than placebo in a randomized, double-blind, cross-over drug study in LEMS.
2009 Nov
Gold and silver nanoparticles conjugated with heparin derivative possess anti-angiogenesis properties.
2009 Nov 11
Management of myasthenic conditions: nonimmune issues.
2009 Oct
Quantification of 4-aminopyridine in plasma by capillary electrophoresis with electrokinetic injection.
2010 Feb 1
3,4-diaminopyridine safety in clinical practice: an observational, retrospective cohort study.
2010 Jun
Patents

Patents

04692443
2
04888426
4
05151424
3
05332744
2
06953790
7
07648998
2

Sample Use Guides

In Vivo Use Guide
Amifampridine (Firdapse) should be given in divided doses, three or four times a day. The recommended starting dose is
Route of Administration: Oral
In Vitro Use Guide
In nerve terminal regions of axons in rat olfactory cortex in the presence of tetraethylammonium (TEA, 5 mM) and Cd2+ (100 uM), the K(+)-component was depressed by Amifampridine (3,4-DAP; 1 to 20 uM; IC50 2.0 +/- 0.4 uM).
Name Type Language
AMIFAMPRIDINE
DASH   EMA EPAR   INN   MART.   MI   USAN   WHO-DD  
INN   USAN  
Official Name English
AMIFAMPRIDINE [MI]
Common Name English
3,4 DIAMINOPYRIDINE
VANDF  
Systematic Name English
AMIFAMPRIDINE [ORANGE BOOK]
Common Name English
NSC-521760
Code English
AMIFAMPRIDINE [INN]
Common Name English
PYRIDINE, 3,4-DIAMINO-
Systematic Name English
DAP
Common Name English
AMIFAMPRIDINE [MART.]
Common Name English
3,4-DIAMINOPYRIDINE
Systematic Name English
AMIFAMPRIDINE [USAN]
Common Name English
3,4 DIAMINOPYRIDINE [VANDF]
Common Name English
3,4-DAP
Code English
DYNAMINE
Brand Name English
AMIFAMPRIDINE [WHO-DD]
Common Name English
RUZURGI
Brand Name English
AMIFAMPRIDINE [EMA EPAR]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 56090
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
WHO-ATC N07XX05
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
WHO-VATC QN07XX05
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
NDF-RT N0000192795
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
FDA ORPHAN DRUG 299909
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
NCI_THESAURUS C93038
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
FDA ORPHAN DRUG 43189
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
FDA ORPHAN DRUG 556516
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
EMA ASSESSMENT REPORTS FIRDAPSE (AUTHORIZED: LAMBERT-EATON MYASTHENIC SYNDROME)
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
FDA ORPHAN DRUG 51590
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
Code System Code Type Description
ChEMBL
CHEMBL354077
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
RXCUI
2106338
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
ECHA (EC/EINECS)
200-220-9
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
FDA UNII
RU4S6E2G0J
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
NCI_THESAURUS
C82687
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
WIKIPEDIA
3,4-DIAMINOPYRIDINE
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
IUPHAR
8032
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
EVMPD
SUB28846
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
LACTMED
Amifampridine
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
MESH
C016361
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
MERCK INDEX
M1668
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY Merck Index
CAS
54-96-6
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
INN
8804
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
EPA CompTox
54-96-6
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
PUBCHEM
5918
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
DRUG CENTRAL
4336
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
DRUG BANK
DB11640
Created by admin on Sat Jun 26 06:11:22 UTC 2021 , Edited by admin on Sat Jun 26 06:11:22 UTC 2021
PRIMARY
ACTIVE MOIETY
Structure of AMIFAMPRIDINE
METABOLITE INACTIVE (PARENT)
Structure of 3-N-ACETYL-AMIFAMPRIDINE
SALT/SOLVATE (PARENT)
Structure of AMIFAMPRIDINE PHOSPHATE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
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