Details
| Stereochemistry | RACEMIC |
| Molecular Formula | 2C9H11N.H2O4S |
| Molecular Weight | 364.459 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OS(O)(=O)=O.N[C@H]1C[C@@H]1C2=CC=CC=C2.N[C@H]3C[C@@H]3C4=CC=CC=C4
InChI
InChIKey=BKPRVQDIOGQWTG-KAVFMPKWSA-N
InChI=1S/2C9H11N.H2O4S/c2*10-9-6-8(9)7-4-2-1-3-5-7;1-5(2,3)4/h2*1-5,8-9H,6,10H2;(H2,1,2,3,4)/t2*8-,9+;/m11./s1
Tranylcypromine is a non-hydrazine monoamine oxidase inhibitor with a rapid onset of activity. Tranylcypromine has being marketed under original trade name Parnate, indicated for the treatment of major depressive episode without melancholia. Tranylcypromine irreversibly and nonselectively inhibits monoamine oxidase (MAO). Within neurons, MAO appears to regulate the levels of monoamines released upon synaptic firing. Since depression is associated with low levels of monoamines, the inhibition of MAO serves to ease depressive symptoms, as this results in an increase in the concentrations of these amines within the CNS.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 23.6 µM [IC50] | |||
| 4.02 µM [IC50] | |||
Target ID: CHEMBL6136 |
5.8 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | PARNATE Approved UseINDICATIONS For the treatment of Major Depressive Episode Without Melancholia. PARNATE should be used in adult patients who can be closely supervised. It should rarely be the first antidepressant drug given. Rather, the drug is suited for patients who have failed to respond to the drugs more commonly administered for depression. The effectiveness of PARNATE has been established in adult outpatients, most of whom had a depressive illness which would correspond to a diagnosis of Major Depressive Episode Without Melancholia. As described in the American Psychiatric Association’s Diagnostic and Statistical Manual, third edition (DSM III), Major Depressive Episode implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed or dysphoric mood that usually interferes with daily functioning and includes at least 4 of the following 8 symptoms: change in appetite, change in sleep, psychomotor agitation or retardation, loss of interest in usual activities or decrease in sexual drive, increased fatigability, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and suicidal ideation or attempts. The effectiveness of PARNATE in patients who meet the criteria for Major Depressive Episode with Melancholia (endogenous features) has not been established. Launch Date1961 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
112 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3757407 |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TRANYLCYPROMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
373 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3757407 |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TRANYLCYPROMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.45 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3757407 |
20 mg 2 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TRANYLCYPROMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
Disc. AE: Drowsiness, Restlessness... AEs leading to discontinuation/dose reduction: Drowsiness Sources: Page: p.64Restlessness Sweating Muscle contractions involuntary Cyanosed Cyanosis Dyspnea Spasms Acute renal failure Hyperpyrexia |
250 mg single, oral Overdose |
unhealthy, 35 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 35 Sex: F Population Size: 1 Sources: |
Disc. AE: Headache, Obtundation... AEs leading to discontinuation/dose reduction: Headache (severe) Sources: Obtundation Hypertension Electrocardiogram T wave peaked |
600 mg single, oral Overdose Dose: 600 mg Route: oral Route: single Dose: 600 mg Co-administed with:: trifluoperazine, p.o(60 mg; single) Sources: |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 42 Sex: M Population Size: 1 Sources: |
Disc. AE: Sweating, Nystagmus... AEs leading to discontinuation/dose reduction: Sweating Sources: Nystagmus Generalised spasm Tachycardia |
30 mg 2 times / day multiple, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 3 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 3 Sources: Page: p.1895 |
DLT: Asthenia, Weakness of limbs... Dose limiting toxicities: Asthenia (grade 2, 33.3%) Sources: Page: p.1895Weakness of limbs (grade 2, 33.3%) Nausea (grade 2, 33.3%) Vomiting (grade 2, 33.3%) |
20 mg 2 times / day multiple, oral MTD Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 6 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 6 Sources: Page: p.1895 |
DLT: Dizziness... Dose limiting toxicities: Dizziness (grade 2, 16.7%) Sources: Page: p.1895 |
4000 mg single, oral Overdose Dose: 4000 mg Route: oral Route: single Dose: 4000 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
Disc. AE: Hyperthermia, Delirium... AEs leading to discontinuation/dose reduction: Hyperthermia Sources: Delirium Thrombocytopenia |
30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
Disc. AE: Suicidal tendency, Suicidal behavior... AEs leading to discontinuation/dose reduction: Suicidal tendency Sources: Page: p.1Suicidal behavior Hypertensive crisis Serotonin syndrome Mania Hypomania Hypotension Hepatotoxicity |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Acute renal failure | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Cyanosed | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Cyanosis | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Drowsiness | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Dyspnea | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Hyperpyrexia | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Muscle contractions involuntary | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Restlessness | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Spasms | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Sweating | Disc. AE | 500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: Page: p.64 |
unhealthy, 27 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 27 Sex: F Population Size: 1 Sources: Page: p.64 |
| Electrocardiogram T wave peaked | Disc. AE | 250 mg single, oral Overdose |
unhealthy, 35 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 35 Sex: F Population Size: 1 Sources: |
| Hypertension | Disc. AE | 250 mg single, oral Overdose |
unhealthy, 35 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 35 Sex: F Population Size: 1 Sources: |
| Obtundation | Disc. AE | 250 mg single, oral Overdose |
unhealthy, 35 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 35 Sex: F Population Size: 1 Sources: |
| Headache | severe Disc. AE |
250 mg single, oral Overdose |
unhealthy, 35 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 35 Sex: F Population Size: 1 Sources: |
| Generalised spasm | Disc. AE | 600 mg single, oral Overdose Dose: 600 mg Route: oral Route: single Dose: 600 mg Co-administed with:: trifluoperazine, p.o(60 mg; single) Sources: |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 42 Sex: M Population Size: 1 Sources: |
| Nystagmus | Disc. AE | 600 mg single, oral Overdose Dose: 600 mg Route: oral Route: single Dose: 600 mg Co-administed with:: trifluoperazine, p.o(60 mg; single) Sources: |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 42 Sex: M Population Size: 1 Sources: |
| Sweating | Disc. AE | 600 mg single, oral Overdose Dose: 600 mg Route: oral Route: single Dose: 600 mg Co-administed with:: trifluoperazine, p.o(60 mg; single) Sources: |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 42 Sex: M Population Size: 1 Sources: |
| Tachycardia | Disc. AE | 600 mg single, oral Overdose Dose: 600 mg Route: oral Route: single Dose: 600 mg Co-administed with:: trifluoperazine, p.o(60 mg; single) Sources: |
unhealthy, 42 n = 1 Health Status: unhealthy Condition: Major depressive disorder Age Group: 42 Sex: M Population Size: 1 Sources: |
| Asthenia | grade 2, 33.3% DLT, Disc. AE |
30 mg 2 times / day multiple, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 3 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 3 Sources: Page: p.1895 |
| Nausea | grade 2, 33.3% DLT, Disc. AE |
30 mg 2 times / day multiple, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 3 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 3 Sources: Page: p.1895 |
| Vomiting | grade 2, 33.3% DLT, Disc. AE |
30 mg 2 times / day multiple, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 3 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 3 Sources: Page: p.1895 |
| Weakness of limbs | grade 2, 33.3% DLT, Disc. AE |
30 mg 2 times / day multiple, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 3 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 3 Sources: Page: p.1895 |
| Dizziness | grade 2, 16.7% DLT, Disc. AE |
20 mg 2 times / day multiple, oral MTD Dose: 20 mg, 2 times / day Route: oral Route: multiple Dose: 20 mg, 2 times / day Co-administed with:: all-trans retinoic acid, p.o(45 mg/m2; q.d) Sources: Page: p.1895 |
unhealthy, 47–82 n = 6 Health Status: unhealthy Condition: Acute myeloid leukemia|Myelodysplasia Age Group: 47–82 Sex: M+F Population Size: 6 Sources: Page: p.1895 |
| Delirium | Disc. AE | 4000 mg single, oral Overdose Dose: 4000 mg Route: oral Route: single Dose: 4000 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
| Hyperthermia | Disc. AE | 4000 mg single, oral Overdose Dose: 4000 mg Route: oral Route: single Dose: 4000 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
| Thrombocytopenia | Disc. AE | 4000 mg single, oral Overdose Dose: 4000 mg Route: oral Route: single Dose: 4000 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
| Hepatotoxicity | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Hypertensive crisis | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Hypomania | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Hypotension | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Mania | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Serotonin syndrome | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Suicidal behavior | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
| Suicidal tendency | Disc. AE | 30 mg 2 times / day multiple, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: multiple Dose: 30 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Major depressive disorder Sources: Page: p.1 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no [IC50 112 uM] | ||||
| no [IC50 >10 uM] | ||||
| no [IC50 >1000 uM] | ||||
| weak [IC50 >10 uM] | ||||
| weak | ||||
| yes [IC50 0.42 uM] | ||||
| yes [IC50 12.1 uM] | ||||
| yes [IC50 6.9 uM] | ||||
| yes [Ki 32 uM] | ||||
| yes [Ki 56 uM] | ||||
| yes | ||||
| yes | ||||
| yes |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Synthesis and antidepressant activities of some 3,5-diphenyl-2-pyrazolines. | 2001 Jun |
|
| [Protease inhibitors as an anesthetic component in ENT surgery]. | 2002 Jul-Aug |
|
| Successful treatment of recurrent brief depression with reboxetine -- a single case analysis. | 2002 Mar |
|
| Regulation of corticotropin-releasing factor neuronal systems and hypothalamic-pituitary-adrenal axis activity by stress and chronic antidepressant treatment. | 2002 Mar |
|
| Successful suppression of cataplectic attacks with tramadol. | 2003 Sep 23 |
|
| Purification and characterization of recombinant human prostacyclin synthase. | 2004 Apr |
|
| Evaluation of the effect of chronic antidepressant treatment on neurokinin-1 receptor expression in the rat brain. | 2004 Jun |
|
| Zinc treatment induces cortical brain-derived neurotrophic factor gene expression. | 2004 May 10 |
|
| Fluorinated phenylcyclopropylamines. Part 3: Inhibition of monoamine oxidase A and B. | 2004 May 15 |
|
| An extensive new literature concerning low-dose effects of bisphenol A shows the need for a new risk assessment. | 2005 Aug |
|
| Cyp2a6 is a principal enzyme involved in hydroxylation of 1,7-dimethylxanthine, a main caffeine metabolite, in humans. | 2005 Sep |
|
| Characterization of hepatic drug-metabolizing activities of Bama miniature pigs (Sus scrofa domestica): comparison with human enzyme analogs. | 2006 Aug |
|
| Running exercise- and antidepressant-induced increases in growth and survival-associated signaling molecules are IGF-dependent. | 2007 Apr |
|
| Venlafaxine in the treatment of panic disorder. | 2007 Feb |
|
| STAR*D: what have we learned? | 2007 Feb |
|
| Biological targets for isatin and its analogues: Implications for therapy. | 2007 Jun |
|
| Not all monoamine oxidase inhibitors are created equal. | 2007 Nov |
|
| A possible role for the endocannabinoid system in the neurobiology of depression. | 2007 Nov 19 |
|
| Cellular and molecular mechanisms in the long-term action of antidepressants. | 2008 |
|
| Pharmacological management of panic disorder. | 2008 Feb |
|
| Diverse antidepressants increase CDP-diacylglycerol production and phosphatidylinositide resynthesis in depression-relevant regions of the rat brain. | 2008 Jan 24 |
|
| Withdrawal from high-dose tranylcypromine. | 2008 Mar |
|
| Safety of high-intensity treatment with the irreversible monoamine oxidase inhibitor tranylcypromine in patients with treatment-resistant depression. | 2008 Nov |
|
| NF-Y substitutes H2A-H2B on active cell-cycle promoters: recruitment of CoREST-KDM1 and fine-tuning of H3 methylations. | 2008 Nov |
|
| Synthesis and studies on antidepressant and anticonvulsant activities of some 3-(2-thienyl)pyrazoline derivatives. | 2008 Nov |
|
| The neurotrophic and neuroprotective effects of psychotropic agents. | 2009 |
|
| Generation of human-induced pluripotent stem cells in the absence of exogenous Sox2. | 2009 Dec |
|
| TCP-FA4: a derivative of tranylcypromine showing improved blood-brain permeability. | 2009 Dec 1 |
|
| Effects of bisphenol-A and other endocrine disruptors compared with abnormalities of schizophrenia: an endocrine-disruption theory of schizophrenia. | 2009 Jan |
|
| Drugs associated with more suicidal ideations are also associated with more suicide attempts. | 2009 Oct 2 |
|
| Long-term portal hypertension increases the vasodilator response to acetylcholine in rat aorta: role of prostaglandin I2. | 2009 Sep 7 |
|
| Ziprasidone, monoamine oxidase inhibitors, and the serotonin syndrome. | 2010 Aug |
|
| α7 and β2 nicotinic receptors control monoamine-mediated locomotor response. | 2010 Dec 8 |
|
| Role of alpha-adrenoceptors and prostacyclin in the enhanced adrenergic reactivity of goat cerebral arteries after ischemia-reperfusion. | 2010 Jul 30 |
Patents
Sample Use Guides
The usual effective dosage is 30 mg per day, usually given in divided doses. If there are no
signs of improvement after a reasonable period (up to 2 weeks), then the dosage may be
increased in 10 mg per day increments at intervals of 1 to 3 weeks; the dosage range may be
extended to a maximum of 60 mg per day from the usual 30 mg per day.
Route of Administration:
Oral
In Vitro Use Guide
Curator's Comment: The release of [(3)H]5-hydroxytryptamine ([(3)H]5-HT) byL-5-hydroxytryptophan (L-5-HTP),α-methyl-m-tyramine (α-MMTA), and elevated levels of K(+) was studied using crude synaptosomal preparations (P2) isolated from the telencephalon of the rat and pigeon.
Studies were conducted in vitro in the presence of 2×10(-5) M tranylcypromine, which inhibited the MAO activity of both the extrasynaptosomal mitochondria and the mitochondria contained within the nerve endings (intrasynaptosomal mitochondria).
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| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C667
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757342
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91119
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m11004
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13614-18-1
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SUB04930MIG
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ACTIVE MOIETY
SUBSTANCE RECORD
