product name Mirabegron
Description: Mirabegron, formerly known as YM-178, is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM. Mirabegron is a drug for the treatment of overactive bladder. Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.
References: J Pharmacol Exp Ther. 2007 May;321(2):642-7; Xenobiotica. 2012 Dec;42(12):1187-96.
396.51
Formula
C21H24N4O2S
CAS No.
223673-61-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 79 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (20.17 mM)
Solubility (In vivo)
Synonyms
YM 178
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397645
| In Vitro |
In vitro activity: Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron has little agonistic effect on 1- and 2-ARs. Mirabegron concentration-dependently relaxes rat and Human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol with EC50 values of 5.1 μM and 0.78 μM, respectively. The maximal relaxant effects of Mirabegron are 94.0 % and 89.4% that of carbachol, respectively. Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH as the IC50 value in human liver microsomes decreased from 13 to 4.3 μM after 30 min preincubation. Mirabegron acts partly as an irreversible or quasi-irreversible metabolism-dependent inhibitor of CYP2D6, Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Mirabegron produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. 3 mg/kg i.v. Mirabegron suppresses the frequency to 2 counts/10 min. Mirabegron does not decrease the amplitude of rhythmic bladder contraction. Mirabegron decreases primary bladder afferent activity and bladder microcontractions in rats. Mirabegron (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling. SAAs of C-fibers decrease only at 1 mg/kg Mirabegron treatment. Mirabegron administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder. Mirabegron is efficient on facilitation of bladder storage. Mirabegron dose-dependently decreases the resting intravesical pressure. Mirabegron dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. Mirabegron exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2007 May;321(2):642-7; Xenobiotica. 2012 Dec;42(12):1187-96. |
Related Posts
product name Mirabegron
Description: Mirabegron, formerly known as YM-178, is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM. Mirabegron is a drug for the treatment of overactive bladder. Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.
References: J Pharmacol Exp Ther. 2007 May;321(2):642-7; Xenobiotica. 2012 Dec;42(12):1187-96.
396.51
Formula
C21H24N4O2S
CAS No.
223673-61-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 79 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (20.17 mM)
Solubility (In vivo)
Synonyms
YM 178
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397645
| In Vitro |
In vitro activity: Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron has little agonistic effect on 1- and 2-ARs. Mirabegron concentration-dependently relaxes rat and Human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol with EC50 values of 5.1 μM and 0.78 μM, respectively. The maximal relaxant effects of Mirabegron are 94.0 % and 89.4% that of carbachol, respectively. Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH as the IC50 value in human liver microsomes decreased from 13 to 4.3 μM after 30 min preincubation. Mirabegron acts partly as an irreversible or quasi-irreversible metabolism-dependent inhibitor of CYP2D6, Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Mirabegron produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. 3 mg/kg i.v. Mirabegron suppresses the frequency to 2 counts/10 min. Mirabegron does not decrease the amplitude of rhythmic bladder contraction. Mirabegron decreases primary bladder afferent activity and bladder microcontractions in rats. Mirabegron (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling. SAAs of C-fibers decrease only at 1 mg/kg Mirabegron treatment. Mirabegron administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder. Mirabegron is efficient on facilitation of bladder storage. Mirabegron dose-dependently decreases the resting intravesical pressure. Mirabegron dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. Mirabegron exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2007 May;321(2):642-7; Xenobiotica. 2012 Dec;42(12):1187-96. |