Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H12N2 |
Molecular Weight | 160.2157 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C(C1=NCCN1)C2=CC=CC=C2
InChI
InChIKey=JIVZKJJQOZQXQB-UHFFFAOYSA-N
InChI=1S/C10H12N2/c1-2-4-9(5-3-1)8-10-11-6-7-12-10/h1-5H,6-8H2,(H,11,12)
Molecular Formula | C10H12N2 |
Molecular Weight | 160.2157 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Tolazoline, also known as priscoline, was used in treatment of persistent pulmonary hypertension of the newborn. But that prescription was discontinued. Priscoline given intravenously produces vasodilatation, primarily due to a direct effect on vascular smooth muscle, and cardiac stimulation; the blood pressure response depends on the relative contributions of the two effects. Priscoline usually reduces pulmonary arterial pressure and vascular resistance. The mechanisms of its therapeutic effects are not clear, but is known, that tolazoline is a non-selective competitive α-adrenergic receptor antagonist and it possesses histamine agonist activity.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11938943 |
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Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8487790 |
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Target ID: CHEMBL1941 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8487790 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | PRISCOLINE Approved UseUnknown Launch Date1948 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
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3.8 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3576663 |
3.2 mg single, intravenous dose: 3.2 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
TOLAZOLINE blood | Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
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0.15 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3576663 |
3.2 mg single, intravenous dose: 3.2 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
TOLAZOLINE blood | Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Other AEs: Erythema, Thrombocytopenia... Other AEs: Erythema (60%) Sources: Thrombocytopenia (45%) Hyponatremia (40%) Gastric acid increased (36%) Seizures (30%) Hematuria (23%) Hypotension (19%) Oliguria (11%) Abdominal distension (9%) Activity motor exaggerated (6%) Tracheal bleeding (6%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Oliguria | 11% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Hypotension | 19% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Hematuria | 23% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Seizures | 30% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Gastric acid increased | 36% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Hyponatremia | 40% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Thrombocytopenia | 45% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Activity motor exaggerated | 6% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Tracheal bleeding | 6% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Erythema | 60% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Abdominal distension | 9% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Hypochloremic metabolic alkalosis following tolazoline-induced gastric hypersecretion. | 1980 Feb |
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Indirect atomic absorption determination of atropine, diphenhydramine, tolazoline, and levamisole based on formation of ion-associates with potassium tetraiodometrcurate. | 2001 Apr |
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Pharmacologic therapy of persistent pulmonary hypertension of the newborn. | 2001 Jan |
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[Indication for lung biopsy and usefulness of lung biopsy]. | 2001 Jun |
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Questionnaire on practices and priorities in neonatal care in Ireland. | 2001 Mar |
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Persistent pulmonary hypertension of the newborn: experience in a single institution. | 2001 Mar-Apr |
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[A case of Down syndrome with ventricular septal defect and hemodynamical Eisenmenger syndrome]. | 2001 May |
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Use of azaperone and zuclopenthixol acetate to facilitate translocation of white-tailed deer (Odocoileus virginianus). | 2002 Jun |
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Anesthesia of polar bears using xylazine-zolazepam-tiletamine or zolazepam-tiletamine. | 2003 Jul |
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Octopaminergic modulation of synaptic transmission between an identified sensory afferent and flight motoneuron in the locust. | 2003 Jul 14 |
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Comparison of the vasodilating effect of nitroglycerin, verapamil, and tolazoline in hand angiography. | 2003 Jun |
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An in vitro study of the effects of Cassia podocarpa fruit on the intestinal motility of rats. | 2004 Feb |
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Characterisation of some pharmacological effects of the venom from Vipera lebetina. | 2004 Mar 15 |
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Ergotamine-induced upper extremity ischemia: a case report. | 2005 Apr-Jun |
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Reported medication use in the neonatal intensive care unit: data from a large national data set. | 2006 Jun |
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A comparison of two combinations of xylazine-ketamine administered intramuscularly to alpacas and of reversal with tolazoline. | 2008 May |
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Adenosine and adenosine receptors: Newer therapeutic perspective. | 2009 Jun |
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Bench-to-bedside review: carbon dioxide. | 2010 |
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Effect of sildenafil on digital ulcers in systemic sclerosis: analysis from a single centre pilot study. | 2010 Aug |
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Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/priscoline.html
An initial dose of 1 to 2 mg/kg, via scalp vein, followed by an infusion of 1 to 2 mg/kg per hour have usually resulted in significant increases in arterial oxygen. There is very little experience with infusions lasting beyond 36 to 48 hours. Response, if it occurs, can be expected within 30 minutes after the initial dose.
Route of Administration:
Intravenous
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:38:36 GMT 2023
by
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on
Fri Dec 15 16:38:36 GMT 2023
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Record UNII |
CHH9H12AQ3
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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WHO-VATC |
QM02AX02
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WHO-VATC |
QV03AB94
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WHO-ATC |
M02AX02
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WHO-VATC |
QC04AB02
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NCI_THESAURUS |
C29713
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WHO-ATC |
C04AB02
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Code System | Code | Type | Description | ||
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TOLAZOLINE
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SUB11148MIG
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59-98-3
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DTXSID3023683
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35110
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DB00797
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200-448-9
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100000077751
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D014043
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m10936
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C66608
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7310
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4213
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CHEMBL770
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CHH9H12AQ3
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CHH9H12AQ3
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5504
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10634
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2695
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28502
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Related Record | Type | Details | ||
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TARGET -> AGONIST | |||
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TARGET -> AGONIST |
SHORT-ACTING
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |