Homatropine Methylbromide 80-49-9
Product Description
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Molecular Weight: 370.28 Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
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.
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Chemical Information
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Contact us if you need more details on 80-49-9. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about Homatropine Methylbromide 80-49-9、80-49-9 Homatropine Methylbromide. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight: 370.28 Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
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.
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 370.28 |
---|---|
Formula | C17H24NO3.Br |
CAS No. | 80-49-9 |
Storage | 3 years -20℃Powder |
---|---|
6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | |
Solubility (25°C) * | In vitro | DMSO | 74 mg/mL (199.84 mM) |
---|---|---|---|
Water | 74 mg/mL (199.84 mM) | ||
Ethanol | 10 mg/mL (27 mM) | ||
In vivo | Saline | 30 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name | 8-Azoniabicyclo[3.2.1]octane, 3-[(2-hydroxy-2-phenylacetyl)oxy]-8,8-dimethyl-, bromide (1:1), (3-endo)- |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 80-49-9. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about Homatropine Methylbromide 80-49-9、80-49-9 Homatropine Methylbromide. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Neuronal Signaling > AChR Inhibitor
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