cgs-24012 and 8-(3-chlorostyryl)caffeine

cgs-24012 has been researched along with 8-(3-chlorostyryl)caffeine* in 1 studies

Other Studies

1 other study(ies) available for cgs-24012 and 8-(3-chlorostyryl)caffeine

Article	Year
Adenosine receptor interactions alter cardiac contractility in rat heart. Clinical and experimental pharmacology & physiology, 2010, Volume: 37, Issue:1 1. The effect of the adenosine A(2) receptor (AdoA(2)R) agonist N(6)-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)-ethyl]adenosine (DPMA) on adenosine A(1) receptor (AdoA(1)R)-mediated negative inotropic responses was investigated in rat heart. 2. Hearts from male Wistar rats (250-350 g) were perfused with Krebs'-Henseleit solution at constant flow in non-recirculating Langendorff mode. Hearts were paced at 5 Hz (5 ms duration, supramaximal voltage) via ventricular electrodes. After 30 min equilibration, (R)-N(6)-phenylisopropyl adenosine (R-PIA) concentration-response curves were constructed in the absence or presence of DPMA. 3. In paced hearts, R-PIA induced concentration-dependent decreases in triple product (heart rate x peak systolic developed pressure x dP / dt(max)), which were significantly attenuated by 1 nmol / L DPMA with a shift in pEC(50) from 8.0 +/- 0.5 (n = 9) in control hearts to 6.63 +/- 1.03 (n = 5) in treated tissues (P < 0.05). The AdoA(2A)R antagonist 8-(3-chlorostyryl)caffeine (1 micromol / L) and the adenylyl cyclase inhibitor cis-N-(2-phenylcyclopentyl)-azacyclotridec-1-en-2-amine hydrochloride (MDL12330A; 100 nmol / L) reversed the effects of DPMA on AdoA(1)R-mediated negative inotropic actions, whereas the AdoA(2B)R antagonist alloxazine (3 micromol / L) had no effect on DPMA activity. 4. The results of the present study show that stimulation of the AdoA(2)R attenuates AdoA(1)R-dependent reductions in inotropic state. The receptor involved appears to be the AdoA(2A)R and its action involves stimulation of adenylyl cyclase activity. Topics: Adenosine; Adenosine A2 Receptor Agonists; Adenosine A2 Receptor Antagonists; Adenylyl Cyclase Inhibitors; Adenylyl Cyclases; Animals; Caffeine; Depression, Chemical; Dose-Response Relationship, Drug; Drug Interactions; Enzyme Inhibitors; Flavins; Imines; In Vitro Techniques; Male; Myocardial Contraction; Phenylisopropyladenosine; Rats; Rats, Wistar; Receptor, Adenosine A1; Receptors, Adenosine A2; Stimulation, Chemical	2010

Article

Year

Adenosine receptor interactions alter cardiac contractility in rat heart.

Clinical and experimental pharmacology & physiology, 2010, Volume: 37, Issue:1

1. The effect of the adenosine A(2) receptor (AdoA(2)R) agonist N(6)-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)-ethyl]adenosine (DPMA) on adenosine A(1) receptor (AdoA(1)R)-mediated negative inotropic responses was investigated in rat heart. 2. Hearts from male Wistar rats (250-350 g) were perfused with Krebs'-Henseleit solution at constant flow in non-recirculating Langendorff mode. Hearts were paced at 5 Hz (5 ms duration, supramaximal voltage) via ventricular electrodes. After 30 min equilibration, (R)-N(6)-phenylisopropyl adenosine (R-PIA) concentration-response curves were constructed in the absence or presence of DPMA. 3. In paced hearts, R-PIA induced concentration-dependent decreases in triple product (heart rate x peak systolic developed pressure x dP / dt(max)), which were significantly attenuated by 1 nmol / L DPMA with a shift in pEC(50) from 8.0 +/- 0.5 (n = 9) in control hearts to 6.63 +/- 1.03 (n = 5) in treated tissues (P < 0.05). The AdoA(2A)R antagonist 8-(3-chlorostyryl)caffeine (1 micromol / L) and the adenylyl cyclase inhibitor cis-N-(2-phenylcyclopentyl)-azacyclotridec-1-en-2-amine hydrochloride (MDL12330A; 100 nmol / L) reversed the effects of DPMA on AdoA(1)R-mediated negative inotropic actions, whereas the AdoA(2B)R antagonist alloxazine (3 micromol / L) had no effect on DPMA activity. 4. The results of the present study show that stimulation of the AdoA(2)R attenuates AdoA(1)R-dependent reductions in inotropic state. The receptor involved appears to be the AdoA(2A)R and its action involves stimulation of adenylyl cyclase activity.

Topics: Adenosine; Adenosine A2 Receptor Agonists; Adenosine A2 Receptor Antagonists; Adenylyl Cyclase Inhibitors; Adenylyl Cyclases; Animals; Caffeine; Depression, Chemical; Dose-Response Relationship, Drug; Drug Interactions; Enzyme Inhibitors; Flavins; Imines; In Vitro Techniques; Male; Myocardial Contraction; Phenylisopropyladenosine; Rats; Rats, Wistar; Receptor, Adenosine A1; Receptors, Adenosine A2; Stimulation, Chemical

2010