RACLOPRIDE TARTRATE

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C15H20Cl2N2O3.C4H6O6
Molecular Weight	497.324
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@H]([C@@H](O)C(O)=O)C(O)=O.CCN1CCC[C@H]1CNC(=O)C2=C(OC)C(Cl)=CC(Cl)=C2O

InChI

InChIKey=QULBVRZTKPQGCR-NDAAPVSOSA-N

InChI=1S/C15H20Cl2N2O3.C4H6O6/c1-3-19-6-4-5-9(19)8-18-15(21)12-13(20)10(16)7-11(17)14(12)22-2;5-1(3(7)8)2(6)4(9)10/h7,9,20H,3-6,8H2,1-2H3,(H,18,21);1-2,5-6H,(H,7,8)(H,9,10)/t9-;1-,2-/m01/s1

HIDE SMILES / InChI

Molecular Formula	C4H6O6
Molecular Weight	150.0868
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	C15H20Cl2N2O3
Molecular Weight	347.237
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3131792 | https://www.ncbi.nlm.nih.gov/pubmed/3873656 | https://www.ncbi.nlm.nih.gov/pubmed/27286237 | https://www.ncbi.nlm.nih.gov/pubmed/21678422https://www.ncbi.nlm.nih.gov/pubmed/2975809
Curator's Comment: the description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24848155 | https://www.ncbi.nlm.nih.gov/pubmed/17765546 | https://www.drugs.com/mmx/raclopride-c-11.html

Raclopride is a salicylamide neuroleptic, that acts as a selective antagonist of D2 dopamine receptors both in vitro and in vivo. Tritium-labelled raclopride has properties that demonstrate its usefulness as a radioligand for the labelling of dopamine-D2 receptors : 3H-Raclopride has a high affinity for the rat and human dopamine-D2 receptors, the non-specific binding of 3H-raclopride is very low, not exceeding 5% of the total binding and the distribution of the 3H-raclopride binding sites in the brain closely correlates with the dopaminergic innervation. The binding of 3H-raclopride is blocked by dopamine-D2 agonists and antagonists, while the D1 agonist SKF 38393 and the Dl antagonist SCH 23390 have much less potency. The interaction of dopamine with 3H-raclopride binding results in a shallow competition curve, which suggests that 3H-raclopride, similar to other dopamine-D2 radioligands, labels both high and low agonist affinity states of the dopamine-D2 receptor. The in vivo receptor binding studies performed with 3H-raclopride also demonstrate its favorable properties as a dopamine-D2 receptor marker in vivo In contrast to some other compounds used as radioligands, raclopride enters the brain readily and binds with a low component of non-specific binding in all dopamine-rich brain areas. A saturation curve may be achieved in vivo binding studies since injections of increasing concentrations of 3H-raclopride appears to be saturated at concentrations above 25 mkCi (corresponding to approximately 5 nmol/kg). Raclopride antagonizes apomorphine-induced hyperactivity in the rat at low doses (ED50 = 130 nM/kg i.p.) but induces catalepsy only at much higher doses (ED50 = 27 mkM/kg i.p.). Radiolabelled raclopride has been used as a ligand for in vitro and in vivo autoradiography in rat and primate brains. Raclopride C 11 is used with positron emission tomography (PET) as a clinical research tool to determine dopamine type 2 (D 2) receptor density in the human brain under normal and pathological conditions. For example, raclopride C 11 used in PET studies has served to confirm the age-related decrease in striatal dopamine D2 receptor density, which may be associated with a decline in the motor as well as cognitive functions. In patients with Alzheimer's disease, raclopride C 11 may be used to examine neuroreceptor distribution and quantities, which may help in the analysis of degenerative alterations of neuron populations and neuroreceptor systems in patients with this disease. In Huntington's disease, in which degeneration of neostriatal interneurons occurs (postsynaptic to the dopaminergic input), specific binding of raclopride C 11 to D 2 receptors may serve as one of the parameters in predicting performance in cognitive tasks.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 311 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24848155	Antagonist 2849	12.7 nM [Ki]
Dopamine D3 receptor 97 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24848155	Antagonist 2849	13.4 nM [Ki]
Dopamine D4 receptor 76 Target ID: CHEMBL219 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17765546	Antagonist 2849	3100.0 nM [Ki]
Dopamine receptor 60 Target ID: CHEMBL2096905 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2391685	Antagonist 2849	8.7 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Alzheimer’s disease 278 Sources: https://www.drugs.com/mmx/raclopride-c-11.html	Diagnostic	Approved 8583	Unknown Approved Use Unknown
Huntington's disease 28 Sources: https://www.drugs.com/mmx/raclopride-c-11.html	Diagnostic	Approved 8583	Unknown Approved Use Unknown
Parkinson's disease 232 Sources: https://www.drugs.com/mmx/raclopride-c-11.html	Diagnostic	Approved 8583	Unknown Approved Use Unknown
Depression 240 Sources: https://clinicaltrials.gov/ct2/show/NCT00832221	Diagnostic	Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
92.5 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
158.8 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	8 mg 2 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
288.25 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	12 mg 2 times / day steady-state, oral dose: 12 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
448.75 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	16 mg 2 times / day steady-state, oral dose: 16 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1949 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
1597 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	8 mg 2 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
2648 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	12 mg 2 times / day steady-state, oral dose: 12 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
4025 nM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	16 mg 2 times / day steady-state, oral dose: 16 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
7.38 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
27.56 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	8 mg 2 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
9.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	12 mg 2 times / day steady-state, oral dose: 12 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
13.29 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7647082/	16 mg 2 times / day steady-state, oral dose: 16 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	RACLOPRIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
16 mg 2 times / day multiple, oral Highest recorded dose Dose: 16 mg, 2 times / day Route: oral Route: multiple Dose: 16 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7871044/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/7871044/	Disc. AE: Drug-induced extrapyramidal side effects... AEs leading to discontinuation/dose reduction: Drug-induced extrapyramidal side effects (16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/7871044/
8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/	Disc. AE: Bilirubin increased, Hypotension postural... AEs leading to discontinuation/dose reduction: Bilirubin increased (2.3%) Hypotension postural (2.3%) Neutrophils (2.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/
8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2531773/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2531773/	Disc. AE: Aggressiveness... AEs leading to discontinuation/dose reduction: Aggressiveness (13.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/2531773/
16 mg single, oral Studied dose Dose: 16 mg Route: oral Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2526172/	healthy Health Status: healthy Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/2526172/	Other AEs: Akathisia... Other AEs: Akathisia (100%) Sources: https://pubmed.ncbi.nlm.nih.gov/2526172/

AEs

AE	Significance	Dose	Population
Drug-induced extrapyramidal side effects	16.7% Disc. AE	16 mg 2 times / day multiple, oral Highest recorded dose Dose: 16 mg, 2 times / day Route: oral Route: multiple Dose: 16 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/7871044/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/7871044/
Bilirubin increased	2.3% Disc. AE	8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/
Hypotension postural	2.3% Disc. AE	8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/
Neutrophils	2.3% Disc. AE	8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/1485530/
Aggressiveness	13.3% Disc. AE	8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2531773/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2531773/
Akathisia	100%	16 mg single, oral Studied dose Dose: 16 mg Route: oral Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2526172/	healthy Health Status: healthy Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/2526172/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2C19 2057 BCRP 910	P-gp 2052 BCRP 697

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDg4MDkifX0=	inconclusive [IC50 31.6228 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDg4MDkifX0=	inconclusive [IC50 7.9433 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMODgwOSJ9fQ==	no [IC50 >10 uM]
BCRP 985	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/3033769#section=Biological-Test-Results Page: 39.0	no
CYP3A4 2633	inducer 1966 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/3033769#section=Biological-Test-Results Page: 247.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDg4MDkifX0=	yes [IC50 1.2589 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMODgwOSJ9fQ==	yes [IC50 12.5893 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
BCRP 697	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21321274/	no
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21321274/ Page: 244 \| 246	no

PubMed

Title	Date	PubMed
Demonstration of competition between endogenous dopamine and [11C]raclopride binding in in vitro brain slices using a dynamic autoradiography technique.	2002-04	11842445
In vivo assessment of adenoviral vector-mediated gene expression of dopamine D(2) receptors in the rat striatum by positron emission tomography.	2002-03-01	11793425
Relationship between blockade of dopamine transporters by oral methylphenidate and the increases in extracellular dopamine: therapeutic implications.	2002-03-01	11793423
Amphetamine-induced dopamine release and post-synaptic specific binding in patients with mild tardive dyskinesia.	2002-03	11850144
Clozapine can induce high dopamine D(2) receptor occupancy in vivo.	2002-02	11862380
SIC, an intracerebral beta(+)-range-sensitive probe for radiopharmacology investigations in small laboratory animals: binding studies with (11)C-raclopride.	2002-02	11850489
Atropine reduces raclopride-induced muscle rigidity by acting in the ventral region of the striatum.	2002-01-11	11779574
NMDA antagonist effects on striatal dopamine release: positron emission tomography studies in humans.	2002-01	11746730
Facilitation of dopaminergic neural transmission does not affect [(11)C]SCH23390 binding to the striatal D(1) dopamine receptors, but the facilitation enhances phosphodiesterase type-IV activity through D(1) receptors: PET studies in the conscious monkey brain.	2001-12-15	11746724
Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT(1A) receptors expressed in HeLa cells.	2001-12-14	11755134
Differential effects of dopamine antagonists on locomotor activity, conditioned activity and conditioned place preference induced by cocaine in rats.	2001-12	11856897
Combined alpha 2-adrenergic/D2 dopamine receptor blockade fails to reproduce the ability of clozapine to reverse phencyclidine-induced deficits in prepulse inhibition of startle.	2001-12	11797077
Neurons and neuronal systems involved in the pathophysiologies of Rett syndrome.	2001-12	11738851
Dopamine D2 receptor-mediated G-protein activation in rat striatum: functional autoradiography and influence of unilateral 6-hydroxydopamine lesions of the substantia nigra.	2001-11-30	11716810
Pharmacodynamic modeling of oral levodopa in Parkinson's disease.	2001-11	11706980
Antagonism of the discriminative stimulus effects of cocaine at two training doses by dopamine D2-like receptor antagonists.	2001-11	11702088
Hypothermia reduces the rate of dissociation of specific ligands from dopamine-D2 and 5-hydroxytryptamine1A receptors in the mouse brain in vivo.	2001-11	11692232
Potent inhibitory effect of selective D2 and D3 agonists on dopamine-responsive dorsomedial arcuate neurons in brain slices of estrogen-primed rats.	2001-10-19	11712668
Aberrant behavioral effects of a dopamine D1 receptor antagonist and agonist in monkeys: evidence of uncharted dopamine D1 receptor actions.	2001-10-01	11600103
Catecholamines in murine bone marrow derived mast cells.	2001-10-01	11585626
Catalepsy induced by a blockade of dopamine D1 or D2 receptors was reversed by a concomitant blockade of adenosine A(2A) receptors in the caudate-putamen of rats.	2001-10	11703457
Effects of raclopride in the nucleus accumbens on ethanol seeking and consumption.	2001-10	11696662
Apomorphine-induced changes in synaptic dopamine levels: positron emission tomography evidence for presynaptic inhibition.	2001-10	11598492
[11C]Raclopride binding was reduced in vivo by sigma(1) receptor ligand SA4503 in the mouse brain, while [11C]SA4503 binding was not by raclopride.	2001-10	11578899
Potentials and pitfalls using high affinity radioligands in PET and SPET determinations on regional drug induced D2 receptor occupancy--a simulation study based on experimental data.	2001-10	11554812
Age-related changes of dopamine D1-like and D2-like receptor binding in the F344/N rat striatum revealed by positron emission tomography and in vitro receptor autoradiography.	2001-09-15	11494399
[Th effect of D2-dopamine receptor blockade on glutamate release into extracellular space of Nucleus accumbens during food reinforcement].	2001-09-11	11548610
A role for dopamine D1 receptors of the nucleus accumbens shell in conditioned taste aversion learning.	2001-09-01	11517277
Drug-induced receptor occupancy: substantial differences in measurements made in vivo vs ex vivo.	2001-09	11594441
Expression and localization of human dopamine D2 and D4 receptor mRNA in the adrenal gland, aldosterone-producing adenoma, and pheochromocytoma.	2001-09	11549694
Imaging human mesolimbic dopamine transmission with positron emission tomography: I. Accuracy and precision of D(2) receptor parameter measurements in ventral striatum.	2001-09	11524609
Dopamine inhibits vasopressin action in the rat inner medullary collecting duct via alpha(2)-adrenoceptors.	2001-09	11504796
The effect of dopamine receptor blockade on motor behavior in Aplysia californica.	2001-08-18	11509200
Iron deficiency decreases dopamine D1 and D2 receptors in rat brain.	2001-08-18	11509198
D1 or D2 antagonism in nucleus accumbens core or dorsomedial shell suppresses lever pressing for food but leads to compensatory increases in chow consumption.	2001-08-18	11509194
Functional neuroanatomy of the ventral striopallidal GABA pathway. New sites of intervention in the treatment of schizophrenia.	2001-08-15	11489297
Expectation and dopamine release: mechanism of the placebo effect in Parkinson's disease.	2001-08-10	11498597
Atropine acts in the ventral striatum to reduce raclopride-induced catalepsy.	2001-07-27	11672560
Delta 9-tetrahydrocannabinol-induced MAPK/ERK and Elk-1 activation in vivo depends on dopaminergic transmission.	2001-07	11553284
An investigation of the mechanisms responsible for acute fluoxetine-induced anxiogenic-like effects in mice.	2001-06	11485052
Vulnerability of positron emission tomography radiotracers to endogenous competition. New insights.	2001-06	11476162
Aging and caloric restriction in nonhuman primates: behavioral and in vivo brain imaging studies.	2001-04	11795523
D1 but not D2 dopamine receptor antagonism blocks the acquisition of a flavor preference conditioned by intragastric carbohydrate infusions.	2001-04	11526968
A PET study with [11-C]raclopride in Parkinson's disease: preliminary results on the effect of amantadine on the dopaminergic system.	2001-02	11487182
Effects of single and repeated administration of 1,2,3,4-tetrahydroisoquinoline analogs on the binding of [11C]raclopride to dopamine D2 receptors in the mouse brain.	2001	11725814
Dopamine and glutamate release in the nucleus accumbens and ventral tegmental area of rat following lateral hypothalamic self-stimulation.	2001	11720786
Effects of the atypical neuroleptic clozapine on micturition parameters in anesthetized rats.	2001	11574938
Caudate nucleus dopamine D(2) receptors in depressed suicide victims.	2001	11490173
Scopolamine does not restore normal conditioned avoidance performance in raclopride-treated rats.	2001	11475009
Stereoselective binding of 11C-raclopride in living human brain--a search for extrastriatal central D2-dopamine receptors by PET.	1988	3131792

Patents

Sample Use Guides

In Vivo Use Guide

3.3 MBq/kg

Route of Administration: Intravenous

In Vitro Use Guide

Primary cultures of rat neonatal ventricular cardiac myocytes were prepared by enzymatic digestion of ventricle tissue with 0.25% trypsin. The cardiomyocytes were first plated for 2 h to reduce non-myocyte contamination. The cells were then washed to remove erythrocytes, replated at a density of 2.0x10^6 cells in culture flasks and incubated at 37C in the presence of 5% CO2 in a humidified incubator. 2.0x10^6 neonatal rat ventricular myocytes were treated with 40 mkM of Raclopride for 24 h.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:01:18 GMT 2025` Edited by `admin` on `Mon Mar 31 18:01:18 GMT 2025`
Record UNII	EXZ5FGZ55J
Record Status	`Validated (UNII)`
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Name

Type

Language

RACLOPRIDE TARTRATE

Common Name

English

BENZAMIDE, 3,5-DICHLORO-N-(((2S)-1-ETHYL-2-PYRROLIDINYL)METHYL)-2-HYDROXY-6-METHOXY-, (2R,3R)-2,3-DIHYDROXYBUTANEDIOATE (1:1)

Preferred Name

English

Code System Code Type Description

FDA UNII

EXZ5FGZ55J

Created by admin on Mon Mar 31 18:01:18 GMT 2025 , Edited by admin on Mon Mar 31 18:01:18 GMT 2025

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EPA CompTox

DTXSID00913404

Created by admin on Mon Mar 31 18:01:18 GMT 2025 , Edited by admin on Mon Mar 31 18:01:18 GMT 2025

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PUBCHEM

57346

Created by admin on Mon Mar 31 18:01:18 GMT 2025 , Edited by admin on Mon Mar 31 18:01:18 GMT 2025

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CAS

98185-20-7

Created by admin on Mon Mar 31 18:01:18 GMT 2025 , Edited by admin on Mon Mar 31 18:01:18 GMT 2025

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					430K3SOZ7G

RACLOPRIDE

PARENT -> SALT/SOLVATE

Related Record Type Details


					430K3SOZ7G

RACLOPRIDE

ACTIVE MOIETY

Details

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Approved Use

Approved Use

Approved Use

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

PubMed

Patents

Sample Use Guides

C_max

T_1/2

Drug as perpetrator