Octaverine
Octaverine is a synthetic isoquinoline alkaloid with oral activity and adrenergic lytic activity. Octaverine antagonizes the pressor effect of adrenaline, elevates the toxicity threshold of adrenaline, and reduces blood pressure. Octaverine increases respiratory depth, respiratory frequency, ventilation rate, and coronary blood flow. Octaverine inhibits spontaneous uterine contractions, antagonizes induced intestinal spasms, alleviates histamine-induced bronchospasm, and exhibits favorable biosafety. Octaverine can be used in research related to intestinal spasms and bronchospasm.
For research use only. We do not sell to patients.
- CAS No.: 549-68-8
- Formula: C23H27NO5
- Molecular Weight:397.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Octaverine (2-4 mg/l; 2 min) inhibits spontaneous contractions of isolated rat uterus, with its minimum effective concentration being 4 mg/l[2].
Octaverine (5-52 mg/l) abolishes the isolated guinea pig ileum spasms induced by Acetylcholine bromide (HY-B0282A) (52 mg/l), Histamine (HY-B1204) (5 mg/l), Barium chloride (HY-Y0527) (10 mg/l), and Pilocarpine (HY-B0726A) (26 mg/l)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Octaverine (0.5-2 mg/kg; intravenous injection; single administration; administered 15 seconds after epinephrine administration) dose-dependently reverses epinephrine-induced hypertension in urethane-anesthetized rabbits and effectively reverses epinephrine-induced respiratory slowing[1].
Octaverine (50 mg/kg; i.p.; single administration) provides 75% and 100% protection against lethal adrenaline toxicity in mice when administered 5 minutes and 10 minutes prior to adrenaline injection, respectively[1].
The LD50 of Octaverine (50-240 mg/kg; intraperitoneal injection; single administration) in mice is approximately 200 mg/kg, with a 100% survival rate at doses up to 190 mg/kg and a 0% survival rate at 240 mg/kg[2].
Octaverine (25-50 mg/kg; p.o.; single administration) exerts partial protective effects against histamine-induced bronchospasm in guinea pigs at the dose of 50 mg/kg, while no protective effect is observed at the dose of 25 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rabbit (weighing 1.75-2.0 kg; urethane-anesthetized, heparinized)[1]
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Dosage:1 mg/kg; 2 mg/kg; 4 mg/kg
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Administration:i.v.; single dose
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Result:Caused rapid 30% decrease in blood pressure (from 85 to 60 mm Hg), sustained for 15 seconds, returning to normal over 15 minutes; slight increase in respiratory depth, normal respiratory rate.
Caused immediate 30% decrease in blood pressure (from 85 to 60 mm Hg), with pressure remaining 10% below normal (75 mm Hg) after 30 minutes; noticeable increase in respiratory depth and rate, which returned to baseline after 15 minutes.
Caused 40% reduction in blood pressure (from 85 to 52 mm Hg), with pressure still 10% below normal (75 mm Hg) after 30 minutes and returning to normal after 60 minutes; increased respiratory rate by 27% (from 45 to 65 p.m.), respiratory depth by 40%, with these levels maintained throughout the hypotensive period; increased ventilation rate by about 50% from baseline.
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Animal Model:Rabbit (weighing 1.75-2.0 kg; urethane-anesthetized, heparinized; adrenaline-induced hypertension model)[1]
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Dosage:0.5 mg/kg; 1.0 mg/kg; 2 mg/kg
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Administration:i.v.; single dose; administered 15 seconds post-adrenaline
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Result:Reduced adrenaline-induced elevated blood pressure by 38-44%, resulting in blood pressure levels at or below baseline; counteracted adrenaline-induced hypopnoea, increasing respiratory depth to 160% of normal (60% increase) and respiratory rate to 50 p.m.
Reduced adrenaline-induced elevated blood pressure by 57%, resulting in blood pressure below baseline.
Increased respiratory depth to 160% of normal (60% increase) and respiratory rate to 41 p.m., counteracting adrenaline-induced hypopnoea; exhibited about 3 times and twice as active as papaverine, respectively, in counteracting adrenaline's pressor effect at 1 mg/kg and 2 mg/kg.
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Animal Model:Mice (weighing 20 g; adrenaline toxicity model)[1]
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Dosage:50 mg/kg (5 minutes pre-adrenaline); 50 mg/kg (10 minutes pre-adrenaline)
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Administration:i.p.; single dose; 5 minutes pre-adrenaline; 10 minutes pre-adrenaline
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Result:Provided 75% protection (1/4 mice died within 4 hours; no apnea or convulsions observed in survivors, with fast breathing noted).
Provided 100% protection (0/4 mice died; fast breathing noted but no apnea or convulsions).
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Animal Model:Mice (mixed sex, 18-22 g)[2]
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Dosage:50 mg/kg; 100 mg/kg; 160 mg/kg; 180 mg/kg; 190 mg/kg; 200 mg/kg; 210 mg/kg; 240 mg/kg
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Administration:i.p.; single dose
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Result:Achieved 100% survival at 50 mg/kg, 100 mg/kg, 160 mg/kg, 180 mg/kg, and 190 mg/kg.
Caused diminished reflexes and drowsiness at 160 mg/kg and 180 mg/kg.
Induced lateral decubitus and sleeping behavior at 190 mg/kg.
Resulted in 50% survival with lateral decubitus and sleeping behavior at 200 mg/kg.
Led to 50% survival with lateral decubitus, sleeping behavior, and convulsions at 210 mg/kg.
Produced 0% survival with lateral decubitus, sleeping behavior, and convulsions at 240 mg/kg.
Yielded an approximate LD50 of 200 mg/kg, with the minimum convulsive dose equal to 100% of the LD50.
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Animal Model:Guinea pigs[2]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Failed to protect any guinea pigs against histamine-induced bronchospasm at 30, 60, or 90 minutes post-dose at 25 mg/kg.
Protected 25 to 50% of guinea pigs at 50 mg/kg, though protected animals showed intermittent neck muscle spasm and respiratory distress during the observation period.
Chemical Information
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CAS No. 549-68-8
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Molecular Weight 397.46
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Formula C23H27NO5
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SMILES
N=1C=CC=2C=C(OC)C(OC)=CC2C1C=3C=C(OCC)C(OCC)=C(OCC)C3
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. GOLDBERG AA, SHAPERO M. A comparative study of the action of octaverine perparine and papaverine on the circulatory and respiratory systems. J Pharm Pharmacol. 1954 Apr;6(4):236-45. [Content Brief]
[2]. GOLDBERG AA, SHAPERO M. A comparative study of the spasmolytic activities of octaverine, perparine and papaverine. J Pharm Pharmacol. 1954 Mar;6(3):171-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Octaverine Related Classifications
HY-W277805 Related Classifications
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