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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Intravenous |
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| ECHA InfoCard | 100.000.408 |
| Chemical and physical data | |
| Formula | C10H12N2 |
| Molar mass | 160.220 g·mol−1 |
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Tolazoline is a non-selectivecompetitiveα2-adrenergic receptor antagonist.[1] It is avasodilator that is used to treat spasms of peripheral blood vessels (as inacrocyanosis). It has also been used (in conjunction with sodium nitroprusside) successfully as an antidote to reverse the severeperipheral vasoconstriction which can occur as a result ofoverdose with certain5-HT2A receptoragonist drugs such as25I-NBOMe,[2]DOB, andBromodragonfly.[3][4]
Tolazoline was first used in the 1980s as an alternative reversal agent forxylazine.[5]
Tolazoline is used in large animal medicine to reverse the effects of α2-adrenergic receptor agonists, typicallyxylazine. Large doses ofintravenous tolazoline in cattle can causehyperesthesia andopisthotonos and other routes such asintramusucular are preferred.[5]
Tolazoline binds to the a2 adrenergic receptor at a ratio of 4:1, the lowest of all a2 adrenergic receptor antagonists. Tolazoline activates theimidazoline receptor.[5]
IV tolazoline has slow elimination and a large distribution in the horse.[6][5]
Tolazoline is an α2 adrenoceptor antagonist that increases skin blood flow in healthy subjects and has been used to relieve acute vasospasm.
