Molecular structure of PD 116,948, CAS Number: 102146-07-6
PD 116,948 (CAS 102146-07-6)
See product citations (6)
Alternate Names:
8-Cyclopentyl-1,3-dipropylxanthine
Application:
PD 116,948 is a very potent and selective Adenosine A1-R antagonist
CAS Number:
102146-07-6
Purity:
≥98%
Molecular Weight:
304.4
Molecular Formula:
C16H24N4O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PD 116,948, a xanthine derivative, is a very potent and selective adenosine A1 receptor antagonist. Exhibits negative chronotropic activity via A1 receptors in isolated rat heart and produces vasodilator effects via A2 receptors. Has been shown to block adenosine-inhibited excitatory post synaptic currents (EPSCs) recorded from subiculum neurons. This product was also observed to inhibit osteoclast formation in mice and stimulate Cl- efflux from delta F508 genotypic cells typically associated with cystic fibrosis.
PD 116,948 (CAS 102146-07-6) References
- Adenosine inhibits glutamate exocytosis largely without interfering with Ca2+ influx in rat cerebrocortical synaptosomes. | Zoccarato, F., et al. 2001. Neurosci Lett. 309: 181-4. PMID: 11514071
- Adenosine A1 receptors and the anticonvulsant potential of drugs effective in the model of 3-nitropropionic acid-induced seizures in mice. | Zuchora, B., et al. 2005. Eur Neuropsychopharmacol. 15: 85-93. PMID: 15572277
- Isoflurane preconditioning decreases glutamate receptor overactivation-induced Purkinje neuronal injury in rat cerebellar slices. | Zheng, S. and Zuo, Z. 2005. Brain Res. 1054: 143-51. PMID: 16081051
- Adenosine A1 receptor antagonist blunts urinary potassium excretion, but not renal hemodynamic effects, induced by carbonic anhydrase inhibitor in rats. | Zhou, X. and Kost, CK. 2006. J Pharmacol Exp Ther. 316: 530-8. PMID: 16278313
- Adenosine A1 receptors presynaptically modulate excitatory synaptic input onto subiculum neurons. | Hargus, NJ., et al. 2009. Brain Res. 1280: 60-8. PMID: 19450566
- Adenosine A1 receptors (A1Rs) play a critical role in osteoclast formation and function. | Kara, FM., et al. 2010. FASEB J. 24: 2325-33. PMID: 20181934
- Effects of adenosine A(1) receptor antagonism on insulin secretion from rat pancreatic islets. | Zywert, A., et al. 2011. Physiol Res. 60: 905-11. PMID: 21995904
- The Adenosine A1 Receptor Antagonist DPCPX Inhibits Tumor Progression via the ERK/JNK Pathway in Renal Cell Carcinoma. | Zhou, Y., et al. 2017. Cell Physiol Biochem. 43: 733-742. PMID: 28950257
- PD 116,948, a highly selective A1 adenosine receptor antagonist. | Haleen, SJ., et al. 1987. Life Sci. 40: 555-61. PMID: 3807648
- Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes. | Zocchi, C., et al. 1996. Br J Pharmacol. 117: 1381-6. PMID: 8730729
- Adenosine release mediates cyanide-induced suppression of CA1 neuronal activity. | Zhu, PJ. and Krnjević, K. 1997. J Neurosci. 17: 2355-64. PMID: 9065496
- 8-cyclopentyl-1,3-dipropylxanthine and other xanthines differentially bind to the wild-type and delta F508 first nucleotide binding fold (NBF-1) domains of the cystic fibrosis transmembrane conductance regulator. | Cohen, BE., et al. 1997. Biochemistry. 36: 6455-61. PMID: 9174362
- Decreased benzodiazepine binding with little effect on gamma-aminobutyric acid binding in rat brain after treatment with antisense oligodeoxynucleotide to the gamma-aminobutyric acidA receptor gamma-2 subunit. | Zhao, TJ., et al. 1998. J Pharmacol Exp Ther. 287: 752-9. PMID: 9808706
Inhibitor of:
A1, Adenosine A1-R, Adenosine A2A-R, Adenosine A3-R, Cdc35, GPR family (GPCR;G protein-coupled), GPR115, GPR128, LALP1, OR1L1, and Vmn2r96.Activator of:
GRK 6, Olfr566, and PDE1C.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PD 116,948, 25 mg | sc-200115 | 25 mg | $124.00 | |||
PD 116,948, 100 mg | sc-200115A | 100 mg | $228.00 |