The Effect of SV 293, a D2 Dopamine Receptor-Selective Antagonist, on D2 Receptor-Mediated GIRK Channel Activation and Adenylyl Cyclase Inhibition

Pharmacology ◽  
2013 ◽  
Vol 92 (1-2) ◽  
pp. 84-89 ◽  
Author(s):  
Renqi Huang ◽  
Suzy A. Griffin ◽  
Michelle Taylor ◽  
Suwanna Vangveravong ◽  
Robert H. Mach ◽  
...  
Keyword(s):  
Adenylyl Cyclase ◽  
Dopamine Receptor ◽  
D2 Receptor ◽  
D2 Dopamine Receptor ◽  
Channel Activation ◽  
Selective Antagonist ◽  
Girk Channel

The A1 allele of the human D2 dopamine receptor gene predicts low D2 receptor availability in healthy volunteers

1998 ◽  
Vol 3 (3) ◽  
pp. 256-260 ◽  
Author(s):  
T Pohjalainen ◽  
J O Rinne ◽  
K Någren ◽  
P Lehikoinen ◽  
K Anttila ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Dopamine Receptor ◽  
Receptor Gene ◽  
D2 Receptor ◽  
D2 Dopamine Receptor ◽  
Dopamine Receptor Gene ◽  
D2 Dopamine Receptor Gene

scholarly journals The renal dopamine receptors.

1992 ◽  
Vol 2 (8) ◽  
pp. 1265-1278
Author(s):  
P A Jose ◽  
J R Raymond ◽  
M D Bates ◽  
A Aperia ◽  
R A Felder ◽  
...  
Keyword(s):  
Amino Acids ◽  
Adenylyl Cyclase ◽  
Dopamine Receptors ◽  
Dopamine Receptor ◽  
D2 Receptor ◽  
D2 Receptors ◽  
Receptor Subtypes ◽  
Renal Dopamine ◽  
The Brain ◽  
Stimulation Of

Dopamine is an endogenous catecholamine that modulates many functions including behavior, movement, nerve conduction, hormone synthesis and release, blood pressure, and ion fluxes. Dopamine receptors in the brain have been classically divided into D1 and D2 subtypes, based on pharmacological data. However, molecular biology techniques have identified many more dopamine receptor subtypes. Several of the receptors cloned from the brain correspond to the classically described D1 and D2 receptors. Several D1 receptor subtypes have been cloned (D1A, D1B, and D5) and are each coupled to the stimulation of adenylyl cyclase. The D2 receptor has two isoforms, a shorter form, composed of 415 amino acids, is termed the D2short receptor. The long form, called the D2long receptor, is composed of 444 amino acids; both are coupled to the inhibition of adenylyl cyclase. The D3 and D4 receptors are closely related to, but clearly distinct from, the D2 receptor. They have not yet been linked to adenylyl cyclase activity. Outside of the central nervous system, the peripheral dopamine receptors have been classified into the DA1 and DA2 subtypes, on the basis of synaptic localization. The pharmacological properties of DA1 receptors roughly approximate those of D1 and D5 receptors, whereas those of DA2 receptors approximate those of D2 receptors. A renal dopamine receptor with some pharmacological features of the D2 receptor but not linked to adenylyl cyclase has been described in the renal cortex and inner medulla. In the inner medulla, this D2-like receptor, termed DA2k, is linked to stimulation of prostaglandin E2 production, apparently due to stimulation of phospholipase A2. Of the cloned dopamine receptors, only the mRNA of the D3 receptor has been reported in the kidney. The DA1 receptor in the kidney is associated with renal vasodilation and an increase in electrolyte excretion. The DA1-related vasodilation and inhibition of electrolyte transport is mediated by cAMP. The role of renal DA2 receptors remains to be clarified. Although DA1 and DA2 receptors may act in concert to decrease transport in the renal proximal convoluted tubule, the overall function of DA2 receptors may be actually the opposite of those noted for DA1 receptors. Dopamine has been postulated to act as an intrarenal natriuretic hormone. Moreover, an aberrant renal dopaminergic system may play a role in the pathogenesis of some forms of hypertension. A decreased renal production of dopamine and/or a defective transduction of the dopamine signal is/are present in some animal models of experimental hypertension as well as in some forms of human essential hypertension.

scholarly journals The Human D2 Dopamine Receptor Synergizes with the A2A Adenosine Receptor to Stimulate Adenylyl Cyclase in PC12 Cells

2003 ◽  
Vol 28 (7) ◽  
pp. 1317-1327 ◽  
Author(s):  
Oliver Kudlacek ◽  
Herwig Just ◽  
Vladimir M Korkhov ◽  
Nina Vartian ◽  
Markus Klinger ◽  
...  
Keyword(s):  
Adenylyl Cyclase ◽  
Dopamine Receptor ◽  
Pc12 Cells ◽  
Adenosine Receptor ◽  
D2 Dopamine Receptor ◽  
A2a Adenosine Receptor

scholarly journals Dopamine Reduces Odor- and Elevated-K+-Induced Calcium Responses in Mouse Olfactory Receptor Neurons In Situ

2004 ◽  
Vol 91 (4) ◽  
pp. 1492-1499 ◽  
Author(s):  
Colleen C. Hegg ◽  
Mary T. Lucero
Keyword(s):  
Receptor Antagonist ◽  
Dopamine Receptor ◽  
Olfactory Receptor ◽  
D2 Receptor ◽  
Olfactory Receptor Neurons ◽  
D2 Dopamine Receptor ◽  
Dopamine Receptor Antagonist ◽  
Voltage Gated ◽  
Dopaminergic Modulation ◽  
Receptor Neurons

Although D2 dopamine receptors have been localized to olfactory receptor neurons (ORNs) and dopamine has been shown to modulate voltage-gated ion channels in ORNs, dopaminergic modulation of either odor responses or excitability in mammalian ORNs has not previously been demonstrated. We found that <50 μM dopamine reversibly suppresses odor-induced Ca2+ transients in ORNs. Confocal laser imaging of 300-μm-thick slices of neonatal mouse olfactory epithelium loaded with the Ca2+-indicator dye fluo-4 AM revealed that dopaminergic suppression of odor responses could be blocked by the D2 dopamine receptor antagonist sulpiride (<500 μM). The dopamine-induced suppression of odor responses was completely reversed by 100 μM nifedipine, suggesting that D2 receptor activation leads to an inhibition of L-type Ca2+ channels in ORNs. In addition, dopamine reversibly reduced ORN excitability as evidenced by reduced amplitude and frequency of Ca2+ transients in response to elevated K+, which activates voltage-gated Ca2+ channels in ORNs. As with the suppression of odor responses, the effects of dopamine on ORN excitability were blocked by the D2 dopamine receptor antagonist sulpiride (<500 μM). The observation of dopaminergic modulation of odor-induced Ca2+ transients in ORNs adds to the growing body of work showing that olfactory receptor neurons can be modulated at the periphery. Dopamine concentrations in nasal mucus increase in response to noxious stimuli, and thus D2 receptor-mediated suppression of voltage-gated Ca2+ channels may be a novel neuroprotective mechanism for ORNs.

D2 dopamine receptor-induced sensitization of adenylyl cyclase type 1 is Gαs independent

2006 ◽  
Vol 50 (5) ◽  
pp. 576-584 ◽  
Author(s):  
Timothy A. Vortherms ◽  
Chau H. Nguyen ◽  
Murat Bastepe ◽  
Harald Jüppner ◽  
Val J. Watts
Keyword(s):  
Adenylyl Cyclase ◽  
Dopamine Receptor ◽  
D2 Dopamine Receptor
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