Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C9H11N.ClH |
| Molecular Weight | 169.651 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.N[C@H]1C[C@@H]1C2=CC=CC=C2
InChI
InChIKey=ZPEFMSTTZXJOTM-RJUBDTSPSA-N
InChI=1S/C9H11N.ClH/c10-9-6-8(9)7-4-2-1-3-5-7;/h1-5,8-9H,6,10H2;1H/t8-,9+;/m1./s1
| Molecular Formula | C9H11N |
| Molecular Weight | 133.1903 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|---|---|---|
| Role of ETB and B2 receptors in the ex vivo platelet inhibitory properties of endothelin and bradykinin in the mouse. | 2001 Feb |
|
| Regulation of GFRalpha-1 and GFRalpha-2 mRNAs in rat brain by electroconvulsive seizure. | 2001 Jan |
|
| Synthesis and antidepressant activities of some 3,5-diphenyl-2-pyrazolines. | 2001 Jun |
|
| The N-demethylation of the doxepin isomers is mainly catalyzed by the polymorphic CYP2C19. | 2002 Jul |
|
| [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 |
|
| Noradrenergic and serotonergic blockade inhibits BDNF mRNA activation following exercise and antidepressant. | 2003 Apr |
|
| Treatment of seasonal affective disorders. | 2003 Dec |
|
| Regulation of GAP-43 expression by chronic desipramine treatment in rat cultured hippocampal cells. | 2003 Mar 15 |
|
| Differential regulation of brain derived neurotrophic factor transcripts by antidepressant treatments in the adult rat brain. | 2003 Sep |
|
| Purification and characterization of recombinant human prostacyclin synthase. | 2004 Apr |
|
| Utility of microtiter plate assays for human cytochrome P450 inhibition studies in drug discovery: application of simple method for detecting quasi-irreversible and irreversible inhibitors. | 2004 Feb |
|
| Evaluation of the effect of chronic antidepressant treatment on neurokinin-1 receptor expression in the rat brain. | 2004 Jun |
|
| Current perspectives in the management of treatment-resistant depression. | 2004 Mar |
|
| Zinc treatment induces cortical brain-derived neurotrophic factor gene expression. | 2004 May 10 |
|
| Effect of antidepressants on GABA(B) receptor function and subunit expression in rat hippocampus. | 2004 Oct 15 |
|
| An extensive new literature concerning low-dose effects of bisphenol A shows the need for a new risk assessment. | 2005 Aug |
|
| Potential of [11C]DASB for measuring endogenous serotonin with PET: binding studies. | 2005 Feb |
|
| Cyp2a6 is a principal enzyme involved in hydroxylation of 1,7-dimethylxanthine, a main caffeine metabolite, in humans. | 2005 Sep |
|
| Isatin interaction with glyceraldehyde-3-phosphate dehydrogenase, a putative target of neuroprotective drugs: partial agonism with deprenyl. | 2006 |
|
| Monoamine oxidase inhibitors allow locomotor and rewarding responses to nicotine. | 2006 Aug |
|
| Tyramine pressor sensitivity during treatment with the selegiline transdermal system 6 mg/24 h in healthy subjects. | 2006 Aug |
|
| New findings from the Bipolar Collaborative Network: clinical implications for therapeutics. | 2006 Dec |
|
| Combination rapid transcranial magnetic stimulation in treatment refractory depression. | 2006 Mar |
|
| Sustained effects of phenelzine and tranylcypromine on orthostatic challenge in antidepressant-refractory depression. | 2006 Oct |
|
| Motor cortex excitability after vagus nerve stimulation in major depression. | 2007 Apr |
|
| Venlafaxine in the treatment of panic disorder. | 2007 Feb |
|
| Honokiol up-regulates prostacyclin synthease protein expression and inhibits endothelial cell apoptosis. | 2007 Jan 5 |
|
| Tranylcypromine enhancement of nicotine self-administration. | 2007 May |
|
| Not all monoamine oxidase inhibitors are created equal. | 2007 Nov |
|
| The guinea pig forced swim test as a new behavioral despair model to characterize potential antidepressants. | 2007 Nov |
|
| A possible role for the endocannabinoid system in the neurobiology of depression. | 2007 Nov 19 |
|
| Receptor mediation of exaggerated responses to serotonin-enhancing drugs in serotonin transporter (SERT)-deficient mice. | 2007 Oct |
|
| Involvement of alpha1-adrenergic receptors in tranylcypromine enhancement of nicotine self-administration in rat. | 2007 Sep |
|
| Cellular and molecular mechanisms in the long-term action of antidepressants. | 2008 |
|
| Pharmacological management of panic disorder. | 2008 Feb |
|
| Rasagiline in treatment of Parkinson's disease. | 2008 Feb |
|
| Repeated unpredictable stress and antidepressants differentially regulate expression of the bcl-2 family of apoptotic genes in rat cortical, hippocampal, and limbic brain structures. | 2008 Jun |
|
| 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 |
|
| 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 |
|
| Inhibition of monoamine oxidases desensitizes 5-HT1A autoreceptors and allows nicotine to induce a neurochemical and behavioral sensitization. | 2009 Jan 28 |
|
| Drugs associated with more suicidal ideations are also associated with more suicide attempts. | 2009 Oct 2 |
|
| Ziprasidone, monoamine oxidase inhibitors, and the serotonin syndrome. | 2010 Aug |
|
| On the formation and nature of the imidazoline I2 binding site on human monoamine oxidase-B. | 2010 Dec |
|
| An overview of curcumin in neurological disorders. | 2010 Mar |
|
| Biochemical, structural, and biological evaluation of tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and LSD2. | 2010 May 19 |
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).
| Substance Class |
Chemical
Created
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admin
on
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| Record UNII |
7H4CZX4FYH
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| Record Status |
Validated (UNII)
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