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tolazoline

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tolazoline

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Also known as 2-benzyl-2-imidazoline, 2-benzyl-4,5-imidazoline, 2-benzylimidazoline, 4,5-dihydro-2-(phenylmethyl)-1H-imidazole

Tolazoline is a non-selective competitive α2-adrenergic receptor antagonist. It is a vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis). It has also been used (in conjunction with sodium nitroprusside) successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT2A receptor agonist drugs such as 25I-NBOMe, DOB, and Bromodragonfly. ==History== Tolazoline was first used in the 1980s as an alternative reversal agent for xylazine. ==Use== Tolazoline is used in large animal medicine to r

Chemical data

Formula
C10H12N2
Molecular weight
160.22 g/mol
IUPAC name
2-benzyl-4,5-dihydro-1H-imidazole
SMILES
C1CN=C(N1)CC2=CC=CC=C2
InChIKey
JIVZKJJQOZQXQB-UHFFFAOYSA-N
XLogP
2.6
Polar surface area
24.4 Ų
H-bond donors
1
H-bond acceptors
1
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
First approval
1985
Admin. routes
parenteral
Indications
cardiovascular disease, Arthralgia, Myalgia

via ChEMBL · EBI

Research

1,423 papers

via PubMed

Wikidata facts

Mass
160.1
Has use
medication
Show 7 more facts
Commons category
Tolazoline
chemical formula
C₁₀H₁₂N₂
World Health Organisation international non-proprietary name
tolazoline
medical condition treated
thromboangiitis obliterans
canonical SMILES
C1CN=C(N1)CC2=CC=CC=C2
subject has role
vasodilator agent
defined daily dose
75
Sources (4)

via Wikidata · CC0

~1 min read

Encyclopedic overview

4 sections
Contents
  • History
  • Use
  • Pharmacology
  • References

Tolazoline is a non-selective competitive α2-adrenergic receptor antagonist. It is a vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis). It has also been used (in conjunction with sodium nitroprusside) successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT2A receptor agonist drugs such as 25I-NBOMe, DOB, and Bromodragonfly. ==History== Tolazoline was first used in the 1980s as an alternative reversal agent for xylazine. ==Use== Tolazoline is used in large animal medicine to reverse the effects of α2-adrenergic receptor agonists, typically xylazine. Large doses of intravenous tolazoline in cattle can cause hyperesthesia and opisthotonos and other routes such as intramusucular are preferred. ==Pharmacology== Tolazoline binds to the a2 adrenergic receptor at a ratio of 4:1, the lowest of all a2 adrenergic receptor antagonists. Tolazoline activates the imidazoline receptor.

IV tolazoline has slow elimination and a large distribution in the horse. ==References==

Excerpted from Wikipedia’s “tolazoline” article, available under the CC BY-SA 4.0 licence.