IBMX is a phosphodiesterase inhibitor (IC50 values are 13, 18, 19, 32 and 50 μM for PDE4, PDE3, PDE1, PDE5 and PDE2 respectively). IBMX suppresses α-adrenoceptor-mediated 5-HT release from neuroendocrine epithelial cells (IC50 = 1.3 μM). IBMX (100 μM) activates renal outer medullary K+ (ROMK) channels (n=6, P<0.05) and prevents further channel activation by ANG II (n=6, P=NS) or cGMP.
Treatments with IBMX and Apocynin significantly decrease cold-induced elevation of right ventricular (RV) systolic pressure (23.5±1.8 and 24.2±0.6 mmHg, respectively) although they do not decrease RV pressure to the warm control levels. IBMX or Apocynin significantly reduces medial layer thickness (19.0±0.9, and 16.9±0.8 μm, respectively) and increases lumen diameter (62.7±4.2, and 59.5±4.3 μm, respectively) of small PAs in cold-exposed rats.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO: ≥ 32 mg/mL|
The phosphodiesterase inhibitor isobutylmethylxanthine attenuates behavioral sensitization to cocaine.
Schroeder JA, et al. Behav Pharmacol. 2012 Jun;23(3):310-4. PMID: 22495185.
KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels.
Wu BN, et al. Br J Pharmacol. 2004 Aug;142(7):1105-14. PMID: 15237094.
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ITI-214 phosphate is an orally active, potent and selective inhibitors of PDE1, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
GLPG1690 (Ziritaxestat) is a first-in-class autotaxin (ATX) inhibitor, with IC50 of 131 nM and Ki of 15 nM.
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