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

Details

Stereochemistry ABSOLUTE
Molecular Formula C17H17NO2
Molecular Weight 267.3224
Optical Activity ( - )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of APOMORPHINE

SMILES

CN1CCC2=C3[C@H]1CC4=CC=C(O)C(O)=C4C3=CC=C2

InChI

InChIKey=VMWNQDUVQKEIOC-CYBMUJFWSA-N
InChI=1S/C17H17NO2/c1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12/h2-6,13,19-20H,7-9H2,1H3/t13-/m1/s1

HIDE SMILES / InChI
Molecular Formula C17H17NO2
Molecular Weight 267.3224
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Apomorphine (brand names: Apokyn, Ixense, Spontane, Uprima) is indicated for the acute, intermittent treatment of hypomobility, “off” episodes (“end-of-dose wearing off” and unpredictable “on/off” episodes) in patients with advanced Parkinson’s disease. Apomorphine has been studied as an adjunct to other medications. It is a non-ergoline dopamine agonist with high in vitro binding affinity for the dopamine D4 receptor, and moderate affinity for the dopamine D2, D3, and D5, and adrenergic α1D, α2B, α2C receptors. The precise mechanism of action as a treatment for Parkinson’s disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D2-type receptors within the caudate-putamen in the brain.

CNS Activity

CNS Active
4002
Curator's Comment: Apomorphine quickly passes the nasal and intestinal mucosa as well as the blood-brain barrier (depending on the administration route)

Approval Year

1880
8
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2752
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8583
APOKYN

Approved Use

APOKYN (apomorphine hydrochloride injection) is indicated for the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) in patients with advanced Parkinson's disease. APOKYN has been studied as an adjunct to other medications [see Clinical Studies (14)

Launch Date

2004
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
47.5 pmol/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2774511/
30 μg/kg bw single, subcutaneous
dose: 30 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
APOMORPHINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
41.7 pmol × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2774511/
30 μg/kg bw single, subcutaneous
dose: 30 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
APOMORPHINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
33.6 min
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/2774511/
30 μg/kg bw single, subcutaneous
dose: 30 μg/kg bw
route of administration: Subcutaneous
experiment type: SINGLE
co-administered:
APOMORPHINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
4 mg single, respiratory
Highest studied dose
Dose: 4 mg
Route: respiratory
Route: single
Dose: 4 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Other AEs: Somnolence, Dysgeusia...
Other AEs:
Somnolence (1 patient)
Dysgeusia (1 patient)
Dizziness (1 patient)
Orthostatic hypotension (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
2.3 mg single, respiratory
Recommended
Dose: 2.3 mg
Route: respiratory
Route: single
Dose: 2.3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Other AEs: Somnolence, Yawning...
Other AEs:
Somnolence (1 patient)
Yawning (1 patient)
Flushing (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Disc. AE: Cognitive impairment, Skin reaction...
AEs leading to
discontinuation/dose reduction:
Cognitive impairment (16 patients)
Skin reaction (14 patients)
Posture abnormal (12 patients)
Psychosis (11 patient)
Anxiety/depression (11 patient)
Hypotension (3 patients)
Gastrointestinal disorder (NOS) (1 patient)
Cardiovascular disorder (1 patient)
Weight loss (1 patient)
Excessive daytime sleepiness (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
4 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 4 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
unhealthy, 65.21 years
Health Status: unhealthy
Age Group: 65.21 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
Disc. AE: Nausea and vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea and vomiting (187 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Disc. AE: Hallucination...
AEs leading to
discontinuation/dose reduction:
Hallucination (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (3%)
Vomiting (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
35 mg 1 times / day steady, sublingual
Recommended
Dose: 35 mg, 1 times / day
Route: sublingual
Route: steady
Dose: 35 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
unhealthy, mean 62.9 years
Health Status: unhealthy
Age Group: mean 62.9 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
Disc. AE: Respiratory tract signs and symptoms...
AEs leading to
discontinuation/dose reduction:
Respiratory tract signs and symptoms (9 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
AEs

AEs

AESignificanceDosePopulation
Dizziness 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Dysgeusia 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Orthostatic hypotension 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Somnolence 1 patient
1.5 mg single, respiratory
Recommended
Dose: 1.5 mg
Route: respiratory
Route: single
Dose: 1.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Flushing 1 patient
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Somnolence 1 patient
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Yawning 1 patient
3 mg single, respiratory
Recommended
Dose: 3 mg
Route: respiratory
Route: single
Dose: 3 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
unhealthy, 30 - 90 years
Health Status: unhealthy
Age Group: 30 - 90 years
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/23527823/
Cardiovascular disorder 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Excessive daytime sleepiness 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Gastrointestinal disorder (NOS) 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Weight loss 1 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Anxiety/depression 11 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Psychosis 11 patient
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Posture abnormal 12 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Skin reaction 14 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Cognitive impairment 16 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Hypotension 3 patients
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
unhealthy, 44 - 87 years
Health Status: unhealthy
Age Group: 44 - 87 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31111272/
Nausea and vomiting 187 patients
Disc. AE
4 mg 1 times / day multiple, subcutaneous
Highest studied dose
Dose: 4 mg, 1 times / day
Route: subcutaneous
Route: multiple
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
unhealthy, 65.21 years
Health Status: unhealthy
Age Group: 65.21 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/18978491/
Hallucination 1%
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Vomiting 2%
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Nausea 3%
Disc. AE
10 mg 1 times / day steady, subcutaneous
Recommended
Dose: 10 mg, 1 times / day
Route: subcutaneous
Route: steady
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021264s010lbl.pdf
Respiratory tract signs and symptoms 9 patients
Disc. AE
35 mg 1 times / day steady, sublingual
Recommended
Dose: 35 mg, 1 times / day
Route: sublingual
Route: steady
Dose: 35 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
unhealthy, mean 62.9 years
Health Status: unhealthy
Age Group: mean 62.9 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31818699/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
1087
inhibitor
2438
inhibitor
2507

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2B6
926

CYP2C8
1057

CYP2C19
2057

CYP3A4/5
296

BCRP
910

BSEP
550

P-gp
1741

MRP2
499

MRP3
246

MRP4
290

MATE1
415

MATE2
267

OATP1B1
1079

OATP1B3
961

OAT1
725

OAT3
747

OCT1
620

OCT2
779
UGT
219

sulfotransferases
39

CYP2B6
776

CYP2C8
810

CYP3A4/5
91
CYP1A2
832

CYP2B6
669

OCT1
39

P-gp
301

MRP2
146

MRP3
83

OATP1B1
29

BCRP
101
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no
BSEP
554
 no
apomorphine glucuronide
3
CYP1A2
2333
 no
apomorphine glucuronide
3
CYP1A2
2333
 no
apomorphine glucuronide
3
CYP2B6
1160
 no
CYP2B6
1160
 no
apomorphine glucuronide
3
CYP2B6
1160
 no
apomorphine glucuronide
3
CYP2C19
2141
 no
apomorphine glucuronide
3
CYP2C8
1117
 no
apomorphine glucuronide
3
CYP2C9
2497
 no
apomorphine glucuronide
3
CYP2D6
2546
 no
apomorphine glucuronide
3
CYP3A4
2633
 no
CYP3A4
2633
 no
apomorphine glucuronide
3
CYP3A4/5
357
 no
apomorphine glucuronide
3
MATE2
267
 no
apomorphine glucuronide
3
MRP2
625
 no
MRP2
625
 no
apomorphine glucuronide
3
MRP3
326
 no
MRP4
345
 no
apomorphine glucuronide
3
OATP1B1
1095
 no
OATP1B1
1095
 no
apomorphine glucuronide
3
OATP1B3
970
 no
apomorphine glucuronide
3
OCT1
656
 no
OCT1
656
 no
apomorphine glucuronide
3
OCT2
782
 no
apomorphine glucuronide
3
P-gp
1932
 no
P-gp
1932
 no
apomorphine glucuronide
3
BCRP
985
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
MATE1
416
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
OAT1
730
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
OAT3
749
 weak [Inhibition 50 uM]
apomorphine glucuronide
3
MRP3
326
 yes [IC50 50 uM]
apomorphine glucuronide
3
CYP1A2
2333
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2B6
776
 yes
CYP2C8
810
 yes
CYP3A4/5
91
 yes
UGT
219
 yes
sulfotransferases
39
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:48538
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:48538
eMolecules
901400
https://www.emolecules.com/cgi-bin/more?vid=901400
ZINC
ZINC000000009073
http://zinc15.docking.org/substances/ZINC000000009073
PubMed

PubMed

TitleDatePubMed
Forced limb-use effects on the behavioral and neurochemical effects of 6-hydroxydopamine.
2001-06-15
Clinical and electrophysiological effects of apomorphine in Parkinson's disease patients are not paralleled by amino acid release changes: a microdialysis study.
2001-06-09
Additive effect of clonidine and fluoxetine on apomorphine-induced aggressive behavior in adult male Wistar rats.
2001-06-08
Dopamine attenuates prefrontal cortical suppression of sensory inputs to the basolateral amygdala of rats.
2001-06-01
Entopeduncular lesions facilitate and thalamic lesions depress spontaneous and drug-evoked motor behavior in the hemiparkinsonian rat.
2001-06-01
Erectile dysfunction.
2001-06
Startle and sensorimotor gating in rats lacking CCK-A receptors.
2001-06
Oral drug therapy for erectile dysfunction.
2001-05
Pharmacology of erectile function and dysfunction.
2001-05
Apomorphine and the dopamine hypothesis of schizophrenia: a dilemma?
2001-05
The broad-spectrum anti-emetic activity of AS-8112, a novel dopamine D2, D3 and 5-HT3 receptors antagonist.
2001-05
Control of serotonergic neurons in rat brain by dopaminergic receptors outside the dorsal raphe nucleus.
2001-05
Interaction between D2 dopaminergic and glutamatergic excitatory influences on lower urinary tract function in normal and cerebral-infarcted rats.
2001-05
Cannabinoid CB(1) receptor agonists produce cerebellar dysfunction in mice.
2001-05
Central dopaminergic function in anorexia and bulimia nervosa: a psychoneuroendocrine approach.
2001-05
Intrasubthalamic injection of 6-hydroxydopamine induces changes in the firing rate and pattern of subthalamic nucleus neurons in the rat.
2001-05
Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents implications for cholinergic involvement in parkinsonism.
2001-04-27
Generation and pharmacological analysis of M2 and M4 muscarinic receptor knockout mice.
2001-04-27
Growth and functional efficacy of intrastriatal nigral transplants depend on the extent of nigrostriatal degeneration.
2001-04-15
Dose-dependent protective effects of apomorphine against methamphetamine-induced nigrostriatal damage.
2001-04-13
NMDA glutamate receptor stimulation is required for the expression of D2 dopamine mediated responses in apomorphine primed 6-hydroxydopamine lesioned rats.
2001-04-06
Attenuation of paraquat-induced dopaminergic toxicity on the substantia nigra by (-)-deprenyl in vivo.
2001-04-01
Acute trazodone and quipazine treatment attenuates apomorphine-induced aggressive behaviour in male rats without major impact on emotional behaviour or monoamine content post mortem.
2001-04
Inhibition of baclofen on morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity.
2001-04
The effects of apomorphine and haloperidol on memory consolidation in the day-old chick.
2001-04
Mechanisms of inverse agonism of antipsychotic drugs at the D(2) dopamine receptor: use of a mutant D(2) dopamine receptor that adopts the activated conformation.
2001-04
Resolution of stroke deficits following contralateral grafts of conditionally immortal neuroepithelial stem cells.
2001-04
Effects of R- and S-apomorphine on MPTP-induced nigro-striatal dopamine neuronal loss.
2001-04
A nitric oxide-dopamine link pathway in organum vasculosum laminae terminalis of rat brain exerts control over blood pressure.
2001-04
Potent, hydroxyl radical-scavenging effect of apomorphine with iron and dopamine perfusion in rat striatum.
2001-03-30
Corticosterone selectively attenuates 8-OH-DPAT-mediated hypothermia in mice.
2001-03
Reproductive experience modulates dopamine-related behavioral responses.
2001-03
Increased sensitivity of dopamine systems following reproductive experience in rats.
2001-03
Stimulus properties of 7-OH-DPAT versus auto- and postsynaptic receptor-specific doses of quinpirole.
2001-03
Differential effects of 7-OH-DPAT on the development of behavioral sensitization to apomorphine and cocaine.
2001-03
Psychopathological correlates of reduced dopamine receptor sensitivity in depression, schizophrenia, and opiate and alcohol dependence.
2001-03
Consensus statement on the role of acute dopaminergic challenge in Parkinson's disease.
2001-03
Orphanin FQ/nociceptin attenuates motor stimulation and changes in nucleus accumbens extracellular dopamine induced by cocaine in rats.
2001-02
Key issues from the clinical trials of apomorphine SL.
2001-02
[Motor impairment, in patients with severe Parkinson's disease, associated with dopaminergic hyperstimulation (entacapone)].
2001-02
Comparison of the effects of infant handling, isolation, and nonhandling on acoustic startle, prepulse inhibition, locomotion, and HPA activity in the adult rat.
2001-02
Microencapsulated bovine chromaffin cell xenografts into hemiparkinsonian rats: a drug-induced rotational behavior and histological changes analysis.
2001-02
The role of neurochemical mechanisms of ventromedial hypothalamus in various models of anxiety in rats.
2001-01
The Posturo-Locomotion-Manual Test. A simple method for the characterization of neurological movement disturbances.
2001
Dopamine agonists.
2001
A risk-benefit assessment of sildenafil in the treatment of erectile dysfunction.
2001
Compulsive checking behavior of quinpirole-sensitized rats as an animal model of Obsessive-Compulsive Disorder(OCD): form and control.
2001
Intrapallidal dopamine restores motor deficits induced by 6-hydroxydopamine in the rat.
2001
Dopaminergic mRNA expression in the intact substantia nigra of unilaterally 6-OHDA-lesioned and grafted rats: an in situ hybridization study.
2001
Involvement of GABAergic neurotransmission in the neurobiology of the apomorphine-induced aggressive behavior paradigm, a model of psychotic behavior in rats.
2000-10
Patents

Patents

05939094
3
JP2009526755A
475
JP2011526596A
7
JP4800219B2
66
JPH083043A
3

Sample Use Guides

In Vivo Use Guide
The recommended starting dose of is 0.2 mL (2 mg). Titrate on the basis of effectiveness and tolerance, up to a maximum recommended dose of 0.6 mL (6 mg)
Route of Administration: Other
In Vitro Use Guide
Apomorphine at concentrations of higher than 2 x 10(-5) M dramatically reduced the growth-stimulatory effect of retinal pigment epithelium (RPE) cells on the scleral chondrocytes, whereas the inhibitory effect of apomorphine on the proliferation of scleral chondrocytes without RPE cells was very little
Substance Class Chemical
Created
by admin
on Mon Mar 31 17:54:46 GMT 2025
Edited
by admin
on Mon Mar 31 17:54:46 GMT 2025
Record UNII
N21FAR7B4S
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
APOMORPHINUM
HPUS  
Preferred Name English
APOMORPHINE
HSDB   MI   VANDF   WHO-DD  
Common Name English
APOMORPHINE [HSDB]
Common Name English
APOMORPHINE [VANDF]
Common Name English
VR-040
Code English
APL-130277
Code English
Apomorphine [WHO-DD]
Common Name English
VR040
Code English
4H-DIBENZO(DE,G)QUINOLINE-10,11-DIOL, 5,6,6A,7-TETRAHYDRO-6-METHYL-, (R)-
Common Name English
6A.BETA.-APORPHINE-10,11-DIOL
Common Name English
APOMORPHINUM [HPUS]
Common Name English
APOMORPHINE [MI]
Common Name English
(6AR)-5,6,6A,7-TETRAHYDRO-6-METHYL-4H-DIBENZO(DE,G)QUINOLINE-10,11-DIOL
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C66884
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
WHO-ATC G04BE07
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
WHO-VATC QG04BE07
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
NDF-RT N0000175580
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
NCI_THESAURUS C38149
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
LIVERTOX NBK548143
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
EU-Orphan Drug EU/3/01/072
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
FDA ORPHAN DRUG 89295
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
WHO-ATC N04BC07
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
NDF-RT N0000000117
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
FDA ORPHAN DRUG 107997
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
WHO-VATC QN04BC07
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
Code System Code Type Description
DRUG BANK
DB00714
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
MESH
D001058
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
PUBCHEM
6005
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
EPA CompTox
DTXSID8022614
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
EVMPD
SUB12923MIG
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
ChEMBL
CHEMBL53
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
IUPHAR
33
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
ECHA (EC/EINECS)
200-360-0
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
CAS
58-00-4
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
MERCK INDEX
m2003
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY Merck Index
NCI_THESAURUS
C61639
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
FDA UNII
N21FAR7B4S
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
LACTMED
Apomorphine
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
HSDB
3289
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
CHEBI
48538
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
DRUG CENTRAL
228
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
RXCUI
1043
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY RxNorm
SMS_ID
100000090486
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
DAILYMED
N21FAR7B4S
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
WIKIPEDIA
APOMORPHINE
Created by admin on Mon Mar 31 17:54:46 GMT 2025 , Edited by admin on Mon Mar 31 17:54:46 GMT 2025
PRIMARY
Related Record Type Details
D(3) DOPAMINE RECEPTOR
TARGET -> AGONIST
Emax 82% Transfected CHO cells
EC50
D(4) DOPAMINE RECEPTOR
TARGET -> AGONIST
Emax 45% Emax 82% Transfected CHO cells
EC50
Structure of APOMORPHINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
CYTOCHROME P450 2D6
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 1A2
METABOLIC ENZYME -> INDUCER
MAXIMUM FOLD INCREASE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of APOMORPHINE HYDROCHLORIDE ANHYDROUS
SALT/SOLVATE -> PARENT
POTASSIUM VOLTAGE-GATED CHANNEL SUBFAMILY H MEMBER 2
OFF-TARGET->INHIBITOR
BINDING
IC50
D(2) DOPAMINE RECEPTOR
TARGET -> AGONIST
D2S Primary receptor interaction.. Emax 79%
EC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Structure of APOMORPHINE
EXCRETED UNCHANGED
INTRAVENOUS ADMINISTRATION
URINE
Related Record Type Details
Structure of APOMORPHINE PALMITATE
PRODRUG -> METABOLITE ACTIVE
Structure of APOMORPHINE DIACETATE
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
Structure of APOMORPHINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC SUBCUTANEOUS ADMINISTRATION

CSF/PLASMA RATIO PHARMACOKINETIC Tmax
PHARMACOKINETIC
Route of Adminstration
PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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