PD 116,948A very potent and selective Adenosine A1-R antagonist

PD 116,948 (CAS 102146-07-6)

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Synonym: 8-Cyclopentyl-1,3-dipropylxanthine
Application: A very potent and selective Adenosine A1-R antagonist
CAS Number: 102146-07-6
Purity: ≥98%
Molecular Weight: 304.4
Molecular Formula: C16H24N4O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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PD 116,948, a xanthine derivative, is a very potent and selective Adenosine A1-R antagonist. It displays very modest efficacy against Adenosine A2A-R, Adenosine A2B-R and Adenosine A3-R. PD 116948 exhibits negative chronotropic activity via Adenosine A1-R in isolated rat heart and produces vasodilator effects via Adenosine A2-R. PD 116,948 is an inhibitor of Adenosine A2A-R.


References

1. Haleen, S.J., et al. 1987. Life Sci. 40: 555-561. PMID: 3807648
2. Cohen, B.E., et al. 1997. Biochemistry. 36: 6455-6461. PMID: 9174362
3. Hargus, N.J., et al. 2009. Brain Res. 1280: 60-68. PMID: 19450566
4. Kara, F.M., et al. 2010. FASEB J. PMID: 20181934

Physical State :
Solid
Solubility :
Soluble in water, DMSO (>10 mg/ml), 0.1 M NaOH (2 mg/ml), and ethanol (4 mg/ml).
Storage :
Store at -20° C
Melting Point :
175-179° C
Boiling Point :
535.09° C at 760 mmHg (Predicted)
Density :
1.20 g/cm3 (Predicted)
Refractive Index :
n20D 1.57 (Predicted)
IC50 :
Adenosine A1 receptor: IC50 = 1.31 nM (human); Adenosine A2a receptor: IC50 = 217 nM (human); Adenosine A2b receptor: IC50 = 656 nM (human)
Ki Data :
A1 receptor: Ki= 3.9 nM; A2A receptor: Ki= 130 nM; A2B receptor: Ki= 50 nM; A3 receptor: Ki= 4000 nM
pK Values :
pKa: 9.04 (Predicted), pKb: 2.50 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UO8184725
PubChem CID :
1329
MDL Number :
MFCD00055117
SMILES :
CCCN1C2=C(C(=O)N(C1=O)CCC)NC(=N2)C3CCCC3

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PD 116,948  Product Citations

See how others have used PD 116,948. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 8232234  Redman, RS. et al. 1993. Mol. Pharmacol. 44: 835-840.

PMID: # 8287913  Von Lubitz, DK. et al. 1993. Eur. J. Pharmacol. 249: 265-270.

PMID: # 8495243  Knight, RJ. et al. 1993. Br. J. Pharmacol. 109: 271-277.

PMID: # 3574492  Bruns, RF. et al. 1987. Naunyn Schmiedebergs Arch. Pharmacol. 335: 59-63.

Citations 1 to 4 of 4 total
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