product name Homatropine Methylbromide
Description: Homatropine Methylbromide is muscarinic AChR antagonist which inhibits endothelial and smooth muscle muscarinic receptors. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
References: Eur J Pharmacol. 1982 May 7;80(1):11-7; J Med Toxicol. 2006 Dec;2(4):156-9.
370.28
Formula
C17H24NO3.Br
CAS No.
80-49-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (199.8 mM)
Water: 74 mg/mL (199.8 mM)
Ethanol: 10 mg/mL (27.0 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1939282
| In Vitro |
In vitro activity: Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Homatropine (20 mg/kg) prevents lethality in rats with dichlorvos poisoning with survive rate of 30% and time of death ranged between 4 and 12 minutes, while Homatropine (10 mg/kg) has no effect on preventing lethality. Homatropine [14C]methylbromide administrated rectal achieves higher and rapid peak plasma concentrations than by the other routes in rats whether HMB-14C is administered in a water-soluble suppository base or in aqueous solution, retained 28% of the 14C has been excreted in the urine while 56% remained in the large intestine after 12 hours. Unlabelled Homatropine methylbromide, given in rectal suppositories to anaesthetized rats, causes prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in saline; 20 mg/kg; Intramuscular (IM) injections |
| References | Eur J Pharmacol. 1982 May 7;80(1):11-7; J Med Toxicol. 2006 Dec;2(4):156-9. |
Related Posts
product name Homatropine Methylbromide
Description: Homatropine Methylbromide is muscarinic AChR antagonist which inhibits endothelial and smooth muscle muscarinic receptors. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
References: Eur J Pharmacol. 1982 May 7;80(1):11-7; J Med Toxicol. 2006 Dec;2(4):156-9.
370.28
Formula
C17H24NO3.Br
CAS No.
80-49-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (199.8 mM)
Water: 74 mg/mL (199.8 mM)
Ethanol: 10 mg/mL (27.0 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1939282
| In Vitro |
In vitro activity: Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Homatropine (20 mg/kg) prevents lethality in rats with dichlorvos poisoning with survive rate of 30% and time of death ranged between 4 and 12 minutes, while Homatropine (10 mg/kg) has no effect on preventing lethality. Homatropine [14C]methylbromide administrated rectal achieves higher and rapid peak plasma concentrations than by the other routes in rats whether HMB-14C is administered in a water-soluble suppository base or in aqueous solution, retained 28% of the 14C has been excreted in the urine while 56% remained in the large intestine after 12 hours. Unlabelled Homatropine methylbromide, given in rectal suppositories to anaesthetized rats, causes prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in saline; 20 mg/kg; Intramuscular (IM) injections |
| References | Eur J Pharmacol. 1982 May 7;80(1):11-7; J Med Toxicol. 2006 Dec;2(4):156-9. |