Isoaminile
Isoaminile is an antitussive agent and an anticholinergic compound with antimuscarinic and antinicotinic properties. Isoaminile blocks the effects of acetylcholine and McN-A-343 at ganglionic sites, inhibits responses to preganglionic sympathetic and splanchnic nerve stimulation, and does not affect postganglionic nerve- or adrenergic-mediated responses. Isoaminile inhibits nictitating membrane contraction and induced hypertension, suppresses isolated guinea pig atrial activity, and stimulates central vagal nerve activity to trigger bradycardia. Isoaminile exerts effects of antitussive action, respiratory inhibition, central nervous system excitation, and cardiovascular function regulation.
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- No. CAS: 77-51-0
- Fòrmula: C16H24N2
- Peso molecular:244.38
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Descripciòn
In Vivo
Isoaminile (10-30 mg/kg; i.v.) reduces or abolishes splanchnic nerve stimulation-induced hypertension in dogs, while leaving adrenaline-induced pressor effects unaltered or potentiated[1].
Isoaminile (s.c.) suppresses ammonia-induced cough in guinea pigs with an ED50 of 0.5 mg/kg s.c.[3].
Isoaminile (i.v.) has an acute intravenous LD50 of 55 mg/kg in male mice, with central nervous system stimulation and convulsions observed with toxic doses[3].
Isoaminile (i.v.) has an acute intravenous LD50 of 20 mg/kg in male rats, with central nervous system stimulation and convulsions observed with toxic doses[3].
Isoaminile (i.v.) has an acute intravenous LD50 of 20 mg/kg in rabbits, with central nervous system stimulation and convulsions observed with toxic doses, and anesthesia plus artificial respiration able to reduce mortality[3].
Isoaminile (i.v.; p.o.) has an acute intravenous LD50 of 20 mg/kg in dogs, with central nervous system stimulation, cardiovascular failure as a primary cause of death, and oral administration causing salivation and vomiting[3].
Isoaminile citrate (22 mg/kg; p.o.; daily six days/week; six weeks) causes transient restlessness and tremor but no lasting adverse effects on growth, organ histology, urine, or blood electrolytes in adult mice[3].
Isoaminile (6 mg/kg; s.c.; daily six days/week; six weeks) causes transient restlessness and tremor, absolute lymphocytosis, but no adverse effects on growth, organ histology, urine, or blood electrolytes in growing rats[3].
Isoaminile (26 mg/kg; p.o.; daily six days/week; six weeks) causes transient restlessness, tremor, and occasional vomiting; one dog developed anemia and porphyrinuria, while others showed no adverse effects on growth, organ histology, urine, or blood electrolytes[3].
Isoaminile (3 mg/kg; p.o.; daily six days/week; 14 weeks) causes no adverse gastrointestinal, behavioral, or hematological effects in mongrel bitches or adult rats[3].
Isoaminile (0.5-10 mg/kg; i.v.) rapid intravenous administration of 10 mg/kg causes diastolic hypotension and bradycardia in anesthetized dogs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cat (anesthetized)[1]
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Dosage:10 mg/kg; 15 mg/kg; 20 mg/kg
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Administration:i.v.
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Result:Reduced pre-ganglionic stimulation-induced nictitating membrane contraction from 40 mm to 12 mm, while post-ganglionic stimulation-induced contraction remained unchanged (26 mm before vs. 27 mm after).
Reduced pre-ganglionic stimulation-induced contraction from 46 mm to 6 mm, with post-ganglionic contraction remaining nearly unchanged (30 mm before vs. 27 mm after), and reduced another pre-ganglionic contraction from 38 mm to 6 mm.
Reduced pre-ganglionic stimulation-induced contraction from 52 mm to 4 mm, with post-ganglionic contraction remaining nearly unchanged (25 mm before vs. 23 mm after), and reduced another pre-ganglionic contraction from 37 mm to 2 mm.
Left post-ganglionic stimulation-induced contractions and adrenaline (50 μg)-induced nictitating membrane contractions unaffected.
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Animal Model:Dog (anesthetized)[1]
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Dosage:10 mg/kg; 15 mg/kg; 20 mg/kg; 30 mg/kg
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Administration:i.v.
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Result:Reduced splanchnic nerve stimulation-induced hypertension from 40 mm Hg to 22 mm Hg.
Reduced splanchnic nerve stimulation-induced hypertension from 36 mm Hg to 2 mm Hg.
Abolished splanchnic nerve stimulation-induced hypertension (from 42 mm Hg to 0 mm Hg in one dog, and from 30 mm Hg to 0 mm Hg in another).
Abolished splanchnic nerve stimulation-induced hypertension from 48 mm Hg to 0 mm Hg.
Left adrenaline (50 μg)-induced pressor effect unaltered or potentiated.
Chemical Information
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No. CAS 77-51-0
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Peso molecular 244.38
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Fòrmula C16H24N2
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SMILES
N#CC(C(C)C)(CC(N(C)C)C)C1=CC=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Isoaminile Related Classifications
HY-105642 Related Classifications
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Keywords
- Isoaminile
- 77-51-0
- Cholinesterase (ChE)
- mAChR
- nAChR
- Muscarinic acetylcholine receptor
- Nicotinic acetylcholine receptors
- muscarinic ganglionic receptor
- acetylcholine
- urethane-anesthetized rabbits
- guinea pig atria
- McN-A-343
- central vagus nerve
- chronic bronchitis
- rat diaphragm-sciatic nerve preparation
- nicotinic ganglionic receptor
- mongrel bitches
- Inhibitor
- inhibitor
- inhibit