product name Loperamide HCl
Description: Loperamide HCl (also known as ADL 2-1294) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, it is used to treat diarrhea resulting from gastroenteritis or inflammatory bowel disease. The specificity for μ-opioid receptors and limited penetrability into the brain prevent Loperamide from demonstrating central systemic effects generally associated with opiates.
References: J Pharmacol Exp Ther. 1999 Apr;289(1):494-502; Pharmacol Biochem Behav. 2005 May;81(1):114-21.
513.5
Formula
C29H33ClN2O2.HCl
CAS No.
34552-83-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (42.8 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.8 mM)
Solubility (In vivo)
Synonyms
ADL 2-1294
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396159
| In Vitro |
In vitro activity: Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [35S]guanosine-5-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1999 Apr;289(1):494-502; J Pharmacol Exp Ther. 2005 Jun;313(3):1011-6; Pharmacol Biochem Behav. 2005 May;81(1):114-21. |
Related Posts
product name Loperamide HCl
Description: Loperamide HCl (also known as ADL 2-1294) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, it is used to treat diarrhea resulting from gastroenteritis or inflammatory bowel disease. The specificity for μ-opioid receptors and limited penetrability into the brain prevent Loperamide from demonstrating central systemic effects generally associated with opiates.
References: J Pharmacol Exp Ther. 1999 Apr;289(1):494-502; Pharmacol Biochem Behav. 2005 May;81(1):114-21.
513.5
Formula
C29H33ClN2O2.HCl
CAS No.
34552-83-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (42.8 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.8 mM)
Solubility (In vivo)
Synonyms
ADL 2-1294
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19396159
| In Vitro |
In vitro activity: Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [35S]guanosine-5-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1999 Apr;289(1):494-502; J Pharmacol Exp Ther. 2005 Jun;313(3):1011-6; Pharmacol Biochem Behav. 2005 May;81(1):114-21. |