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Chemical Structure| 102146-07-6 Chemical Structure| 102146-07-6

Structure of DPCPX
CAS No.: 102146-07-6

Chemical Structure| 102146-07-6

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DPCPX is a potent and selective A1 adenosine receptor antagonist, both in vitro and in vivo, with Ki of 3.9 nM for human A1.

Synonyms: PD 116948

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Product Details of DPCPX

CAS No. :102146-07-6
Formula : C16H24N4O2
M.W : 304.39
SMILES Code : O=C(N1CCC)N(CCC)C2=C(NC(C3CCCC3)=N2)C1=O
Synonyms :
PD 116948
MDL No. :MFCD00055117

Safety of DPCPX

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of DPCPX

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
rat spinal cord neurons 50 μM 30 minutes DPCPX significantly augmented the C-fiber-evoked spinal local field potential (C-LFP) and increased the amplitude of A-LFP in nerve-injured rats, indicating that A1R activation exerts tonic inhibition on spinal nociceptive transmission. Br J Anaesth. 2024 Apr;132(4):746-757
PFC pyramidal neurons 0.3 μM Blocked the inhibitory effect of 40 Hz light flicker on excitatory transmission, increased sEPSC frequency and amplitude Mol Psychiatry. 2024 Nov;29(11):3381-3394
rat mesenteric vascular bed 1 μmol/L DPCPX significantly inhibited norepinephrine-induced mesenteric vasoconstriction, indicating that A1 receptor signaling plays an important role in α1-adrenoceptor-mediated vasoconstriction. Hypertension. 2020 Oct;76(4):1308-1318

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Tibial-spared nerve injury (SNI-t) model Spinal topical application 50 μM Single administration, 30 minutes exposure DPCPX significantly augmented the C-fiber-evoked spinal local field potential (C-LFP) and increased the amplitude of A-LFP in nerve-injured rats by blocking A1R activation, indicating that A1R activation exerts tonic inhibition on spinal nociceptive transmission. Additionally, DPCPX blocked the inhibition of C-LFP by spinal cord stimulation (SCS). Br J Anaesth. 2024 Apr;132(4):746-757
Sprague-Dawley rats Transient middle cerebral artery occlusion (MCAO) model Intraperitoneal (i.p.) administration 1.25 mg/kg Once daily for 6 consecutive days To evaluate the effect of DPCPX on neuroinflammation after cerebral ischemia, results showed that DPCPX treatment group had improved brain lesion volume and neurological scores. Theranostics. 2021 Jan 1;11(1):410-425
Female 16p11.2 deletion mice 16p11.2 deletion mouse model Intragastric 4 mg/kg Once daily for 14 days Blocked the ameliorative effect of 40 Hz light flicker on social novelty deficits, increased anxiety levels Mol Psychiatry. 2024 Nov;29(11):3381-3394
Mice Wild type mice Epidural application or intracortical injection 0.7–1 mM (epidural application) or 30 μM (intracortical injection) DPCPX induced spontaneous CSDs but only small-DC shifts along with suppression of EEG spikes during photic stimulation, suggesting that the inhibition co-activated with sensory stimulation could limit CSD ignition when K+ uptake was not sufficiently suppressed as with ouabain. J Headache Pain. 2022 Aug 19;23(1):107
Sprague–Dawley rats Parkinson's disease model Intraperitoneal injection 3 mg/kg Once daily for 7 consecutive days To investigate the inhibitory effect of DPCPX on CPA-induced α-synuclein expression/aggregation and neurodegeneration. Results showed that DPCPX and 1-aminoindan attenuated CPA-induced α-synuclein expression/aggregation and neurodegeneration in the substantia nigra and hippocampus. Transl Neurodegener. 2022 Feb 10;11(1):9

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3.29mL

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32.85mL

6.57mL

3.29mL

 

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