Details
Stereochemistry | MIXED |
Molecular Formula | C21H33NO3 |
Molecular Weight | 347.4916 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 0 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1(O)CC2N(CCC3=C2C=C(OC)C(OC)=C3)CC1CC(C)C
InChI
InChIKey=TUNMGCULOKMBNJ-UHFFFAOYSA-N
InChI=1S/C21H33NO3/c1-6-21(23)12-18-17-11-20(25-5)19(24-4)10-15(17)7-8-22(18)13-16(21)9-14(2)3/h10-11,14,16,18,23H,6-9,12-13H2,1-5H3
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/9988119Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9988119 |
https://www.ncbi.nlm.nih.gov/pubmed/10773000
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9988119
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/9988119 |
https://www.ncbi.nlm.nih.gov/pubmed/10773000
Ro 4-1284 is a VMAT2 inhibitor. Compond exhibits reserpine-like effect and is used as a tool compound in preclinical studies, its chronic administration lead to such symptoms as deterioration of learning, decrease in locomotion in rearing, intense hypothermia
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1893 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16905316 |
28.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
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Monoamine-depleting drugs. | 1975 |
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An evaluation of the use of intraventricularly administered [3H]5-hydroxytryptamine as a marker for endogenous brain 5-hydroxytryptamine. | 1975 Jul 25 |
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Influence of a benzoquinolizinyl derivative on serum and hepatic alkaline phosphatase activity in the dog and rat. | 1975 May |
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A subchronic study of the toxicity of an orally administered benzoquinolizinyl derivative in the rat and dog. | 1975 May |
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Interaction of psychotropic agents with central neurotransmitters as revealed by their effects on PGO waves in the cat. | 1976 |
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On the role of storage granules in the functional utilization of newly synthesized dopamine. | 1976 |
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Uptake and liberation of mepacrine in blood platelets. | 1976 |
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[Studies on the synthesis of isocarbostyril derivatives. (1). A novel synthesis of isocarbostyril derivatives and synthesis of protoberberine and dibenzoquinolizine derivatives (author's transl)]. | 1976 Feb |
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Drugs and PGO waves in the lateral geniculate body of the curarized cat. IV. The effects of acetylcholine, GABA and benzodiazepines on PGO wave activity. | 1976 Feb |
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[Effects of methamphetamine and a reserpine-like drug on norepinephrine and dopamine metabolism in the rat brain]. | 1976 May |
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[Effect of lithium on the central serotonin- and adrenergic processes after its chronic administration]. | 1976 May-Jun |
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[Effects of lithium chloride administered in combination with methamphetamine or a reserpine- like drug on brain norepinephrine and dopamine metabolism in rats]. | 1976 Sep |
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Dopamine content and synthesis in retina and n. accumbens septi: pharmacological and light-induced modifications. | 1977 |
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Effects of Ro 4-1284 on electrically-induced spinal cord seizures and on spinal cord norepinephrine and 5-hydroxytryptamine levels. | 1977 Dec |
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Mechanisms underlying modifications in the severity of audiogenic convulsions. | 1977 Jun 15 |
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Possible physiological significance of the initial step in the catabolism of noradrenaline in the central nervous system of the rat. | 1977 Mar |
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Effect of neuroleptics and other drugs on monoamine uptake by membranes of adrenal chromaffin granules. | 1977 Mar |
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[Ways of increasing resistance of renal transplant to thermal ischemia]. | 1977 Sep-Oct |
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Enhancement of 5-hydroxytryptamine synthesis in brain by monamine-depleting drugs. | 1978 Feb |
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Effects of L-dopa, GPA 1734 and other agents on basement membrane biosynthesis. | 1978 Feb |
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Choline acetyltransferase and acetylcholinesterase activities in mice brain during the antagonistic action of antidepressant drugs and Ro 4--1284. | 1978 Jan-Feb |
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Forced swimming in rats: hypothermia, immobility and the effects of imipramine. | 1979 Aug 15 |
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A comparison of cochlear microphonics and N1 in audiogenic-seizure-susceptible and control rats. | 1980 |
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In vivo monoamine oxidase inhibition by d-amphetamine. | 1980 May 15 |
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Depletion of epinephrine in rat hypothalamus by Ro 4-1284: influence of pargyline and harmaline. | 1980 Sep-Oct |
|
An improved pharmacological procedure for depletion of noradrenaline: pharmacology and assessment of noradrenaline-associated behaviors. | 1982 Feb 5 |
|
Drug-induced release of biogenic amines from synaptosomes and blood platelets of guinea-pigs. | 1982 Sep |
|
The role of norepinephrine in feeding behavior. | 1982 Summer |
|
Comparison of the effects of beta-phenylethylamine and d-amphetamine on rat isolated atria. | 1983 Oct |
|
Synthesis and antihypertensive activity of a series of spiro[1,3,4,6,7,11b-hexahydro-2H-benzo[a]quinolizine-2,5'-oxazolidin-2'-one]s. | 1983 Oct |
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Studies of the alpha 2-adrenoceptor affinity and the alpha 2- to alpha 1-adrenoceptor selectivity of some substituted benzoquinolizines using receptor-binding techniques. | 1984 May 1 |
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Alpha 2-adrenoceptor antagonism and other pharmacological antagonist properties of some substituted benzoquinolizines and yohimbine in vitro. | 1984 Oct |
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The outward transport of axoplasmic noradrenaline induced by a rise of the sodium concentration in the adrenergic nerve endings of the rat vas deferens. | 1984 Sep |
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Errors introduced by a tritium label in position 8 of catecholamines. | 1986 Jan |
|
The mechanism of the 3H-noradrenaline releasing effect of various substrates of uptake1: role of monoamine oxidase and of vesicularly stored 3H-noradrenaline. | 1987 Dec |
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Rate of basement membrane biosynthesis as an index to angiogenesis. | 1988 |
|
[Electrophysiological study of tianeptine, a new enhancer of serotonin uptake with antidepressant activity]. | 1988 Aug |
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Mechanisms of effects of d-fenfluramine on brain serotonin metabolism in rats: uptake inhibition versus release. | 1988 Jul |
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Neuropeptide Y differentiates between exocytotic and nonexocytotic noradrenaline release in guinea-pig heart. | 1989 Nov |
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Pharmacological inactivation of the vesicular monoamine transporter can enhance 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurodegeneration of midbrain dopaminergic neurons, but not locus coeruleus noradrenergic neurons. | 2000 |
|
The control of blepharospasm by essential fatty acids. | 2000 |
|
Role for dopamine in malonate-induced damage in vivo in striatum and in vitro in mesencephalic cultures. | 2000 Apr |
|
Vesicular monoamine transporter 2 and the acute and long-term response to 3,4-(±)-methylenedioxymethamphetamine. | 2015 Jan |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10773000
In neurotoxicity experiments Ro4-1284 was administered to rats at doses 10 mg/kg i.p.
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16905316
Inhibition of [3H]DTBZ binding (probing VMAT2) on rat synaptic vesicle membranes was measured. Ro 4-1284 inhibits binding of [3H]DTBZ with Ki of 28 nM.
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9345
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303-75-3
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DTXSID90952665
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H2S3M5M720
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SUBSTANCE RECORD