Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H12N2 |
Molecular Weight | 160.2161 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
c1ccc(cc1)CC2=NCCN2
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 | 160.2161 |
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 |
---|---|---|---|---|
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 |
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DDT-induced myoclonus: serotonin and alpha noradrenergic interaction. | 1979 Feb |
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Hypochloremic metabolic alkalosis following tolazoline-induced gastric hypersecretion. | 1980 Feb |
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Tolazoline and acute renal failure in the newborn. | 1981 May 30 |
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[Tolazoline and dopamine in the treatment of the persistent fetal circulation syndrome]. | 1983 Oct |
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[Renal disorders in the newborn infant]. | 1984 Jan-Feb |
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Bolus and continuous infusion of tolazoline in neonates with hypoxemia. | 1986 |
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Blood flow distribution and brain metabolism during tolazoline-induced hypotension in newborn dogs. | 1990 Aug |
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Spasms of the hepatic artery following percutaneous transluminal angioplasty and tolazoline administration in a liver transplant patient. | 1996 May-Jun |
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Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding. | 1998 Apr 1 |
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Inhaled nitric oxide applications in paediatric practice. | 2002 Jan |
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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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Re: Nonlocalized lower gastrointestinal bleeding: provocative bleeding studies with intraarterial tPA, heparin, and tolazoline. | 2002 May |
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Is nebulised tolazoline an effective treatment for persistent pulmonary hypertension of the newborn? | 2003 Jan |
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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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The effect of different combinations of lignocaine, ketoprofen, xylazine and tolazoline on the acute cortisol response to dehorning in calves. | 2003 Oct |
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Pharmacokinetics of xylazine, 2,6-dimethylaniline, and tolazoline in tissues from yearling cattle and milk from mature dairy cows after sedation with xylazine hydrochloride and reversal with tolazoline hydrochloride. | 2003 Summer |
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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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An in vitro study of the effects of Cassia podocarpa fruit on the intestinal motility of rats. | 2004 Feb |
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Effectiveness of antagonists for tiletamine-zolazepam/xylazine immobilization in female white-tailed deer. | 2004 Jul |
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Characterisation of some pharmacological effects of the venom from Vipera lebetina. | 2004 Mar 15 |
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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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Bench-to-bedside review: Ventilator strategies to reduce lung injury -- lessons from pediatric and neonatal intensive care. | 2005 Apr |
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Clinical assessment of epidural analgesia induced by xylazine-lidocaine combination accompanied by xylazine sedation in calves. | 2005 Oct 1 |
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Persistent pulmonary hypertension of the newborn: pathogenesis, etiology, and management. | 2006 |
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Comparative effects of tolazoline and nitroprusside on human isolated radial artery. | 2006 Jan |
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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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Antagonism of detomidine sedation in the horse using intravenous tolazoline or atipamezole. | 2006 May |
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Impaired cognition and attention in adults: pharmacological management strategies. | 2007 Feb |
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Castration of lambs: a welfare comparison of different castration techniques in lambs over 10 weeks of age. | 2007 May |
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A diazonium ion cascade from the nitrosation of tolazoline, an imidazoline-containing drug. | 2008 Feb |
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Nucleoside and DNA adducts from N-nitrosotolazoline. | 2008 Feb |
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N-nitrosotolazoline: decomposition studies of a typical N-nitrosoimidazoline. | 2008 Feb |
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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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Effect of vasoactive agents on the dermatopharmacokinetics and systemic disposition of model compounds, salicylate and FITC-dextran 4 kDa, following intracutaneous injection of the compounds. | 2008 May 22 |
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A novel high-throughput screening assay for putative antidiabetic agents through PPARalpha interactions. | 2008 Oct |
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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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Butorphanol-azaperone-medetomidine for immobilization of captive white-tailed deer. | 2009 Apr |
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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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The clinical outcomes of transcatheter microcoil embolization in patients with active lower gastrointestinal bleeding in the small bowel. | 2009 Jul-Aug |
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Adenosine and adenosine receptors: Newer therapeutic perspective. | 2009 Jun |
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Physiologic effects of nasal oxygen or medical air administered prior to and during carfentanil-xylazine anesthesia in North American elk (Cervus canadensis manitobensis). | 2009 Mar |
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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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Effect of sildenafil on digital ulcers in systemic sclerosis: analysis from a single centre pilot study. | 2010 Aug |
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Pharmacological characterization of a Bombyx mori alpha-adrenergic-like octopamine receptor stably expressed in a mammalian cell line. | 2010 Feb |
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Functional and pharmacological characterization of a beta-adrenergic-like octopamine receptor from the silkworm Bombyx mori. | 2010 Jun |
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Cardiovascular effects of sub-daily levels of ambient fine particles: a systematic review. | 2010 Jun 15 |
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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
Sat Jun 26 10:25:20 UTC 2021
by
admin
on
Sat Jun 26 10:25:20 UTC 2021
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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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59-98-3
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DB00797
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200-448-9
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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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5504
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10634
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2695
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TARGET -> AGONIST |
SHORT-ACTING
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TARGET -> AGONIST | |||
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |