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 Date-6.8774402E11 |
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 |
---|---|---|---|---|
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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Blood flow distribution and brain metabolism during tolazoline-induced hypotension in newborn dogs. | 1990 Aug |
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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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Nonlocalized lower gastrointestinal bleeding: provocative bleeding studies with intraarterial tPA, heparin, and tolazoline. | 2001 Nov |
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Inhaled nitric oxide applications in paediatric practice. | 2002 Jan |
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Re: Nonlocalized lower gastrointestinal bleeding: provocative bleeding studies with intraarterial tPA, heparin, and tolazoline. | 2002 May |
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Efficacy and safety of tolazoline for treatment of severe hypoxemia in extremely preterm infants. | 2002 May |
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Comparison of the vasodilating effect of nitroglycerin, verapamil, and tolazoline in hand angiography. | 2003 Jun |
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A comparison of two intramuscular doses of xylazine-ketamine combination and tolazoline reversal in llamas. | 2004 Apr |
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Effectiveness of antagonists for tiletamine-zolazepam/xylazine immobilization in female white-tailed deer. | 2004 Jul |
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Persistent pulmonary hypertension of the newborn. | 2004 Jun |
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2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. | 2004 Sep 20 |
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Ergotamine-induced upper extremity ischemia: a case report. | 2005 Apr-Jun |
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Antagonism by imidazoline-type drugs of muscarinic and other receptors in the guinea-pig ileum. | 2006 Jul |
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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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Impaired cognition and attention in adults: pharmacological management strategies. | 2007 Feb |
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A diazonium ion cascade from the nitrosation of tolazoline, an imidazoline-containing drug. | 2008 Feb |
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N-nitrosotolazoline: decomposition studies of a typical N-nitrosoimidazoline. | 2008 Feb |
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Evaluation of intramuscular butorphanol, azaperone, and medetomidine and nasal oxygen insufflation for the chemical immobilization of white-tailed deer, Odocoileus virginianus. | 2008 Sep |
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A novel approach for percutaneous treatment of massive nonocclusive mesenteric ischemia: tolazoline and glycerol trinitrate as effective local vasodilators. | 2009 Feb 1 |
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Accurate localization of life threatening colonic hemorrhage during nuclear medicine bleeding scan as an aid to selective angiography. | 2009 May 27 |
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Adverse drug effects in hospitalized elderly: data from the healthcare cost and utilization project. | 2010 |
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Bench-to-bedside review: carbon dioxide. | 2010 |
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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 UTC 2023
by
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on
Fri Dec 15 16:38:36 UTC 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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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 |
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ACTIVE MOIETY |