Purinergic P1 Receptor Antagonists

Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.

Also Known As:

Adenosine Receptor Antagonists; P1 Purinoceptor Antagonists; Antagonist, Adenosine Receptor; Antagonist, P1 Purinoceptor; Antagonists, Adenosine Receptor; Antagonists, P1 Purinoceptor; Purinoceptor Antagonist, P1; Purinoceptor Antagonists, P1; Receptor Antagonist, Adenosine; Receptor Antagonists, Adenosine; Adenosine Receptor Antagonist; P1 Purinoceptor Antagonist; Purinergic P1 Receptor Antagonist

Networked: 374 relevant articles (22 outcomes, 56 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160
  - Molecular Mechanisms of Pharmacological Action: 24
    - Neurotransmitter Agents: 13181
      - Purinergic Agents: 10
        Purinergic Antagonists: 16
        Purinergic P1 Receptor Antagonists: 374
        Adenosine A2 Receptor Antagonists: 64
        Adenosine A1 Receptor Antagonists: 13
        Adenosine A3 Receptor Antagonists: 1
  - Physiological Effects of Drugs: 1
    - Neurotransmitter Agents: 13181
      - Purinergic Agents: 10
        Purinergic Antagonists: 16
        Purinergic P1 Receptor Antagonists: 374
        Adenosine A2 Receptor Antagonists: 64
        Adenosine A1 Receptor Antagonists: 13
        Adenosine A3 Receptor Antagonists: 1

Experts

1.	Givertz, Michael M: 10 articles (11/2019 - 02/2009)
2.	Metra, Marco: 10 articles (11/2019 - 01/2010)
3.	O'Connor, Christopher M: 10 articles (11/2019 - 01/2010)
4.	Ponikowski, Piotr: 10 articles (11/2019 - 01/2010)
5.	Teerlink, John R: 9 articles (11/2019 - 05/2011)
6.	Voors, Adriaan A: 9 articles (11/2019 - 05/2011)
7.	Cotter, Gad: 7 articles (01/2018 - 01/2010)
8.	Dittrich, Howard C: 7 articles (01/2018 - 01/2010)
9.	Cunha, Rodrigo A: 6 articles (09/2020 - 01/2007)
10.	Davison, Beth A: 6 articles (01/2018 - 11/2011)

Related Diseases

1.	Neoplasms (Cancer) 05/01/2015 - "We sought to determine whether blockade of A2A receptors could enhance the efficacy of anti-PD-1 mAb. The expression of CD73 by tumor cells limited the efficacy of anti-PD-1 mAb in two tumor models, and this was alleviated with concomitant treatment with an A2A adenosine receptor antagonist. " 01/01/2023 - "Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A2A/A3 Adenosine Receptor Antagonists and Their Cancer Immunotherapeutic Activity." 08/20/2022 - "Here, we focused on the efficacy of adenosine receptor antagonists and their enhancement in anti-cancer immunotherapy." 12/09/2021 - "Adenosine Receptor Antagonists as Potential Cancer Therapy." 09/08/2020 - "Tumor Immunotherapy Using A2A Adenosine Receptor Antagonists."
2.	Seizures (Absence Seizure) 04/29/1999 - "Following a subconvulsant audiogenic stimulus of 83 dB, all adenosine receptor antagonists induced both tonic and clonic seizures. " 04/29/1999 - "In the absence of auditory stimulation, the adenosine receptor antagonists increased the incidence of both clonic and tonic seizures in DBA/2 mice. " 01/01/2011 - "Conversely, adenosine augmentation therapies are effective in seizure suppression and prevention, whereas adenosine receptor antagonists such as methylxanthines generally exacerbate seizures. " 06/08/2001 - "Similarly, A1/A2 agonist, 5'-N-ethylcarboxamidoadenosine, protected against seizures evoked by the intracerebral administration of 3-NPA, and this effect was reversed by the co-application of adenosine receptor antagonist, 8-(p-sulfophenyl)theophylline. " 11/01/2007 - "Also, the adenosine receptor antagonist, aminophylline, prevented these effects of IL-6 on hyperthermia-induced seizures. "
3.	Heart Failure 11/01/2009 - "Cardio-renal effects of the A1 adenosine receptor antagonist SLV320 in patients with heart failure." 01/01/2014 - "Predictors of postdischarge outcomes from information acquired shortly after admission for acute heart failure: a report from the Placebo-Controlled Randomized Study of the Selective A1 Adenosine Receptor Antagonist Rolofylline for Patients Hospitalized With Acute Decompensated Heart Failure and Volume Overload to Assess Treatment Effect on Congestion and Renal Function (PROTECT) Study." 11/01/2011 - "The Placebo-controlled Randomized study of the selective A(1) adenosine receptor antagonist rolofylline for patients hospitalized with acute heart failure and volume Overload to assess Treatment Effect on Congestion and renal funcTion (PROTECT) pilot study was a multicenter, double-blind study of patients with AHF. " 05/10/2011 - "This study sought to assess the effects of rolofylline on renal function in patients with acute heart failure (AHF) and renal dysfunction randomized in PROTECT (Placebo-Controlled Randomized Study of the Selective A(1) Adenosine Receptor Antagonist Rolofylline for Patients Hospitalized With Acute Decompensated Heart Failure and Volume Overload to Assess Treatment Effect on Congestion and Renal Function). " 01/01/2010 - "This manuscript describes the rationale underlying the design of the phase 3 PROTECT (Placebo-controlled Randomized study of the selective A(1) adenosine receptor antagonist rolofylline for patients hospitalized with acute heart failure and volume Overload to assess Treatment Effect on Congestion and renal funcTion) trial. "
4.	Parkinson Disease (Parkinson's Disease) 01/01/2014 - "The obatined results might be helpful in rational design of novel candidate of A2A adenosine receptor antagonist for treatment of Parkinson's disease. " 08/01/2014 - "In contrast, A(2A) adenosine receptor antagonists have progressed to late-stage clinical trials in Parkinson disease, yet evidence of their role in oncology is limited. " 02/02/2011 - "A(2A) adenosine receptor antagonists are currently under investigation as potential therapeutic agents for Parkinson's disease (PD). " 11/27/2008 - "Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease." 05/14/2004 - "Multigram-scale syntheses, stability, and photoreactions of A2A adenosine receptor antagonists with 8-styrylxanthine structure: potential drugs for Parkinson's disease."
5.	Hypoglycemia (Reactive Hypoglycemia) 03/01/2002 - "From a pharmacological point of view, the adenosine-receptor antagonist theophylline might be beneficial in the management of hypoglycemia unawareness. " 01/01/2022 - "Application of the A2A adenosine receptor antagonist ZM-241385 eliminated hypoglycemia-evoked astrocyte Ca2+ increases and reduced arteriole dilations by 44% (p < 0.05). " 01/01/1996 - "Because the adenosine receptor antagonist 8PT attenuated this hyperemic response, it is concluded that adenosine is involved in eliciting the increase in retinal blood flow that accompanies hypoglycemia." 01/01/1996 - "In the other (n = 5), the nonspecific adenosine receptor antagonist 8-phenyltheophylline (8PT) was administered intravenously approximately 15 minutes before hypoglycemia to examine the role of adenosine in the hemodynamic response to hypoglycemia. " 12/01/1997 - "Cerebral blood flow was measured by the [14C]iodoantipyrine method in conscious rats during insulin-induced, moderate hypoglycemia (2 to 3 mmol/L glucose in arterial plasma) after intravenous injections of 10 to 20 mg/kg of caffeine, an adenosine receptor antagonist, or intracisternal infusion of 1 to 2 mumol/L glibenclamide, a KATP channel inhibitor. "

Related Drugs and Biologics

1.	rolofylline
2.	Theophylline (Theon)
3.	Purinergic P1 Receptors (Adenosine Receptor)
4.	Aminophylline (Carine)
5.	Vasopressins (Vasopressin)
6.	Tolvaptan
7.	Caffeine (No Doz)
8.	Adenosine (Adenocard)
9.	Haloperidol (Haldol)
10.	Relaxin

Related Therapies and Procedures

1.	Therapeutics
2.	Immunotherapy
3.	Oral Administration
4.	Length of Stay
5.	Intraperitoneal Injections