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At least 19 recordsLinked to original sources

Distribution of dopamine receptors and dopamine receptor homologs in the brain of the honey bee, Apis mellifera L.

In the brain of the honey bee, Apis mellifera, the radioligands [3H]-SCH23390 and [3H]-spiperone recognise D1- and D2-like receptors, respectively. In addition to being pharmacologically distinct and exhibiting significantly different expression profiles during the lifetime of the bee, [3H]-SCH23390- and [3H]-spiperone-binding sites differ markedly in their distribution within the brain. Estimates of [3H]-SCH23390-binding site density are highest in the somatal rind, whereas [3H]-spiperone-binding sites are most concentrated in the beta lobe neuropil of the mushroom bodies. Molecular cloning techniques have been used to identify two honey bee genes encoding dopamine receptor homologs. The first is the honey bee counterpart of a Drosophila D1-like dopamine receptor and is expressed in the mushroom bodies of both workers and drones. The second is related to D2-like dopamine receptors from vertebrates and is expressed in the brain of the bee, but the precise distribution of expression is not yet known.

Animals↗

Association analysis for dopamine D3 receptor, dopamine D4 receptor and dopamine transporter genetic polymorphisms and P300 event-related potentials for normal young females.

OBJECTIVE: It has been demonstrated that the P300 components, a positive event-related potential, are heritable and are influenced by dopaminergic activity. We tested the genetic effects of the dopaminergic system in P300 components by association study. METHODS: In a sample population consisting of 120 normal young Han-Chinese females, we explored the association between the P300 components, and, the genetic polymorphisms including the dopamine D3 receptor (serine-to-glycine polymorphism in exon I), the dopamine D4 receptor (variable number tandem repeat polymorphism in exon III), and the dopamine transporter (variable number tandem repeat polymorphism in promoter region). RESULTS: No associations were demonstrated between the polymorphisms of these three genes and the P300 components. CONCLUSIONS: Our negative findings suggest that these genetic polymorphisms do not play a major role in the modulation of P300 event-related potentials.

Adult↗

Subclassification of peripheral dopamine receptors.

Dopamine receptors in peripheral tissues have been subclassified using agonists and antagonists. The vascular dopamine receptors in the dog and cat mesenteric vascular beds are similar; those in the rabbit isolated splenic artery are similar to those in the human isolated basilar artery, but appear to differ in some respects from those in the mesenteric vascular beds. The dopamine receptors in the chemoreceptor trigger zone of the dog and the neuronal dopamine receptors on the sympathetic nerve terminals supplying the cat heart and nictitating membrane and the dog femoral vascular bed seem to be the same. However they are all clearly different from the vascular dopamine receptors. The neuronal dopamine receptors on the cholinergic nerve terminals of the rabbit rectococcygeus muscle appear different from other neuronal receptors. The results suggest that sub-types of vascular and neuronal dopamine receptors may exist.

Animals↗

The renal dopamine receptors.

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.

Humans↗

Molecular characteristics of mammalian dopamine receptors.

Dopamine receptors belong to a large super-gene family of receptors which are linked to their signal transduction pathways through heterotrimeric G proteins. A variety of signalling events are known to be regulated by dopamine receptors including adenylate cyclase and phospholipase activities and various ion channels. Prior to the advent of molecular cloning technology, dopamine receptors were believed to belong to two subtypes, D1 and D2. This distinction was based on both pharmacological and functional criteria. We now know that at least five different dopamine receptors exist although they can still be described as to belonging within "D1" and "D2" subfamilies. The D1 subfamily consists of two receptors-the D1 and D5, whereas the D2, D3 and D4 receptors comprise the D2 subfamily. The cloning and molecular characteristics of these five receptors are described in this review.

Adenylyl Cyclases↗

Solubilization and characterization of striatal dopamine receptors.

Dopamine receptor binding proteins were solubilized with the detergent 3-(3-cholamidopropyl) dimethylammonio-2-hydroxy-1-propanesulfonate (CHAPSO) from bovine and rat striatal membranes. The binding of the dopamine antagonist [3H]spiroperidol [( 3H]Spi) to the solubilized dopamine receptors was determined by the polyethyleneglycol method. The CHAPSO-solubilized dopamine receptor binding proteins remain in the supernatant fraction following centrifugation at 100,000 X g for 2 h. The CHAPSO-solubilized dopamine receptor proteins, as well as the prelabeled [3H]Spi-receptor protein complex, bind specifically to wheat germ agglutinin (WGA)-agarose columns, which is consistent with an identification as glycoproteins, HPLC analysis of the CHAPSO-solubilized, prelabeled [3H]Spi-receptor protein complex (CHAPSO preparation) reveals association with a high molecular weight form, indicating the formation of aggregates and/or micelles. Treatment of the WGA-agarose-bound [3H]Spi-receptor protein complex with digitonin (CHAPSO-digitonin preparation) results in dissociation of the high molecular weight form into lower molecular weight forms. The HPLC profile of the prelabeled [3H]Spi-receptor complex in the CHAPSO-digitonin preparation reveals two radioactive peaks. The major peak had a retention time of 16 min, corresponding to an apparent MW of 175,000, whereas the minor peak had a retention time of 21 min, corresponding to an apparent MW of 49,000. The CHAPSO-solubilized dopamine receptor binding proteins are sensitive to modulation by GTP, indicating that the association with the GTP binding component is preserved in the "soluble" state. The potencies of dopamine antagonists and agonists for inhibiting the binding of [3H]Spi to CHAPSO-solubilized dopamine receptor proteins are similar to those for membrane-bound proteins.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗

The subcommissural organ expresses D2, D3, D4, and D5 dopamine receptors.

Dopamine receptors have been found in certain populations of non-neuronal cells in the brain, viz., discrete areas of ciliated ependyma and the ependymal cells of the choroid plexus. We have studied the presence of both tyrosine-hydroxylase-immunoreactive nerve fibers and dopamine receptors in the subcommissural organ (SCO), an ependymal brain gland that is located in the roof of the third ventricle and that secretes, into the cerebrospinal fluid, glycoproteins that aggregate to form Reissner's fiber (RF). Antibodies against D2, D3, D4, and D5 dopamine receptors were used in immunoblots of bovine striatum, fresh SCO, and organ-cultured SCO, and in immunocytochemistry of the bovine, rat, and mouse SCO. Only a few tyrosine-hydroxylase fibers appeared to reach the SCO. However, virtually all the secretory ependymal and hypendymal cells of the SCO immunoreacted with antibodies against D2, D4, and D5 receptors, with the last-mentioned rendering the strongest reaction, especially at the ventricular cell pole of the secretory ependymocytes, suggesting that dopamine might reach the SCO via the cerebrospinal fluid. The antibodies against the four subtypes of receptors revealed corresponding bands in immunoblots of striatum and fresh SCO. Although the cultured SCO displayed dopamine receptors, dopamine had no apparent effect on the expression of the SCO-spondin gene/protein or on the release of RF-glycoproteins (SCO-spondin included) by SCO explants, suggesting that dopamine affects the function(s) of the SCO differently from the secretion of RF-glycoproteins.

Animals↗

Molecular biology of the invertebrate dopamine receptors.

Dopamine is found in the nervous systems of both vertebrates and invertebrates. However, the specific actions of dopamine depend on the dopamine receptor type that is expressed in the target cell. As in mammals, different subtypes of dopamine receptors have been cloned and characterized from invertebrates, and these receptor subtypes have different structural and functional properties. Understanding how these receptors respond to dopamine and in which cells each receptor type is expressed is key to our understanding of the role of dopamine signaling. Comparison of the amino acid sequences and experimentally determined functional properties suggest that there are at least three distinct types of dopamine receptors in invertebrates. This review focuses on invertebrate dopamine receptors for which the genes have been isolated and identified, and examines our current knowledge of the functional and structural properties of these receptors, and their pharmacology and expression.

Amino Acid Sequence↗

Continuous treatment with the D2 dopamine receptor agonist quinpirole decreases D2 dopamine receptors, D2 dopamine receptor messenger RNA and proenkephalin messenger RNA, and increases mu opioid receptors in mouse striatum.

Dopamine-mediated behaviors and certain biochemical and molecular events associated with these behaviors were examined following continuous infusion of the D1 dopamine agonist SKF38393 or the D2 dopamine agonist quinpirole into mice for six days. SKF38393 produced a transient grooming behavior while quinpirole initially induced stereotypy, which was followed by an increased locomotor behavior. Continuous infusion of quinpirole caused a significant down-regulation of striatal D2 dopamine receptors without significantly changing the density of D1 receptors. This was accompanied by a decrease in the level of D2 receptor messenger RNA in striatum as measured by Northern analysis. The down-regulation of dopamine receptors was selective for D2 dopamine receptors, since treatment with SKF38393 had no significant effects on either D1 or D2 dopamine receptors, nor did it alter the messenger RNAs for the D1 and D2 receptors. Continuous treatment with quinpirole resulted in a significant increase in striatal mu opioid receptor levels without significant changing delta opioid receptors. This treatment also induced a significant decrease in proenkephalin messenger RNA in striatum. Taken together, these results suggest that the down-regulation of D2 dopamine receptor and D2 receptor messenger RNA is the result of the persistent stimulation of D2 receptors and that the up-regulation of mu opioid receptors may be a compensatory response to a decreased biosynthesis of enkephalin. They suggest further that the biochemical and molecular changes that take place in dopaminergic and enkephalinergic systems following continuous treatment with dopamine agonists may underlie the mechanisms by which certain dopamine-mediated behaviors occur.

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-ben↗

Dopamine transporter blockade increases LTP in the CA1 region of the rat hippocampus via activation of the D3 dopamine receptor.

Dopamine has been demonstrated to be involved in the modulation of long-term potentiation (LTP) in the CA1 region of the hippocampus. As monoamine transporter blockade will increase the actions of endogenous monoamine neurotransmitters, the effect of a dopamine transporter (DAT) antagonist on LTP was assessed using field excitatory postsynaptic potentials recorded in the CA1 region of the rat hippocampal slice preparation. Application of the DAT-specific blocker GBR 12,935 produced a significant enhancement in LTP of Schaffer collateral synapses in the CA1 at concentrations as low as 100 nM. A selective D1/D5 dopamine receptor antagonist (SCH 23,390, 1 microM) did not affect the ability of GBR 12,935 to enhance LTP, whereas application of the D3 dopamine receptor antagonist U 99,194 (1 microM) blocked the GBR 12,935-induced enhancement in LTP. In addition, a D3 dopamine receptor agonist (7-OH-DPAT, 1 microM) caused a significant increase in LTP, an effect that was also blocked by U 99,194 (3 microM). These results suggest that either endogenously released dopamine (facilitated by DAT blockade) or exogenously applied dopamine agonist can act to increase LTP in the CA1 of the hippocampus via activation of the D3 subtype of dopamine receptor.

Animals↗

Dynamin-2 associates with the dopamine receptor signalplex and regulates internalization of activated D2 receptors.

Dopamine receptors (DRs) are implicated in modulating a variety of important neuronal processes including those involved in development and plasticity. Although dopamine receptors are known to be internalized in response to ligand activation, the mechanisms regulating this process have not been clearly defined. Here, we show that D2 dopamine receptors (D2Rs) undergo dynamin-2-dependent internalization in response to agonist treatment. Using a cleavable biotin assay to quantify receptor internalization, we found that expression of dynamin-2 mutants defective in GTPase function virtually abolished agonist-induced D2R internalization. In contrast, expression of a dynamin-1 mutant did not alter D2R internalization. In human embryonic kidney (HEK) 293 cells and primary striatal neurons, dynamin-2 was found to localize to sites of D2R internalization. Dynamin/D2R association was examined in adult rat forebrain using subcellular fractionation and coimmunoprecipitation methods. D2Rs and dynamin-2 were coexpressed in non-synaptosomal fractions, and dynamin-2 was found to coimmunoprecipitate with the D2R signalling complex (signalplex). Taken together, our findings suggest that dynamin-2 regulates D2R internalization and thus is likely to play an important role in D2R mediated dopaminergic transmission.

Animals↗

Pharmacological characterisation of the dopamine-sensitive adenylate cyclase in cockroach brain: evidence for a distinct dopamine receptor.

Dopamine increases cyclic AMP production in crude membrane preparations of cockroach brain with plateaus in cyclic AMP production occurring between 1-10 microM and at 10 mM. Maximal production of cyclic AMP is 2.25 fold greater than that of control values. Octopamine also increases cyclic AMP production with a Ka of 1.4 microM and maximal production 3.5 fold greater than that of control. 5-Hydroxytryptamine does not increase cyclic AMP production. The effects of octopamine and dopamine are fully additive. The vertebrate dopamine agonists ADTN and epinine stimulate the dopamine-sensitive adenylate cyclase (AC) with Ka values of 4.5 and 0.6 microM respectively and with maximal effectiveness 1.7 fold greater than that of control. The selective D2-dopamine agonist LY-171555 stimulates cyclic AMP production to a similar extent with a Ka of 50 microM. Other dopamine agonists (apomorphine, SKF-82526, SKF-38393) have no stimulatory effects. The octopamine-sensitive AC is inhibited by a variety of antagonists known to affect octopamine and dopamine receptors, with the following order of potency: mianserin greater than phentolamine greater than cyproheptadine greater than piflutixol greater than cis-flupentixol greater than SCH-23390 greater than (+)-butaclamol greater than SKF-83566 greater than SCH-23388 greater than sulpiride greater than spiperone greater than haloperidol. The dopamine-sensitive AC is inhibited by the same compounds with the following order of potency: piflutixol greater than cis-flupentixol greater than (+)-butaclamol greater than spiperone greater than or equal to SCH-23390 greater than cyproheptadine greater than SKF-83566 greater than SCH 23388 greater than mianserin greater than phentolamine greater than sulpiride greater than haloperidol. With the exception of mianserin, 3H-piflutixol is displaced from brain membranes by dopamine antagonists with an order of potency similar to that observed for the inhibition of dopamine-sensitive AC. The results indicate that the octopamine- and dopamine-sensitive AC in cockroach brain can be distinguished pharmacologically and the dopamine receptors coupled to AC have pharmacological characteristics distinct from vertebrate D1- and D2-dopamine receptors.

Adenylyl Cyclases↗

Synthesis and processing of D2 dopamine receptors.

Dopamine receptors belong to a superfamily of neurotransmitter receptors that are functionally coupled to guanine nucleotide binding proteins. In this study, we have used Chinese hamster ovary (CHO) cells stably transfected with the rat D2L receptor, in conjunction with specific anti-peptide antibodies that we have developed, in order to visualize this protein and the course of its synthesis. The newly synthesized receptor exists as a 45-kDa protein which undergoes further processing to a 75-kDa glycosylated receptor in the CHO cells. In pulse-chase experiments it was noticed that a 35-kDa precursor was present which disappeared after 30 min. In order to determine whether this 35-kDa protein represents an unprocessed form of the receptor, we have employed an in vitro translation system with cDNA constructs coding for both the murine D2 and D3 dopamine receptor isoforms. In the absence of processing, the D2 and D3 receptors have an apparent molecular mass of 35 kDa. The translated proteins were shown to be the full length receptors by immunoprecipitation with various anti-peptide antibodies and by the demonstration that they can undergo glycosylation to apparent molecular masses of approximately 45 kDa in an in vitro system.

Affinity Labels↗

Neuronal dopamine receptors of the rabbit ear artery: pharmacological characterization of the receptor.

Dopamine and apomorphine were examined in the rabbit isolated perfused ear artery for both direct effects on vascular smooth muscle and effects on the response to field stimulation of sympathetic nerve terminals. The neuroinhibitory effect of both dopamine (EC50 = 37 nM) and apomorphine (EC50 = 44 nM) occurred at concentrations which did not produce vasoconstriction. The neuroinhibitory effect of dopamine was shown to be due to inhibition of noradrenaline release by measurement of 3H-overflow from prelabelled tissues. At relatively high concentrations dopamine produced vasoconstriction. In a superfused segment of ear artery, dopamine was found to be a full agonist at the alpha 1-adrenoreceptor, with an EC50 (15 microM) about 75 fold higher than the EC50 for noradrenaline. At concentrations up to 3 microM, apomorphine had no vasoconstrictor activity in the perfused ear artery. Representative examples of several classes of dopamine antagonists, including the phenothiazines, butyrophenones, diphenylbutylpiperidines and benzamides produced competitive antagonism of dopamine or apomorphine-induced inhibition, with nearly identical Kb values against these two agonists. The pharmacological characteristics of the neuronal dopamine receptor on the rabbit ear artery would indicate this receptor to be typical of the D2 subclass, and this tissue to be a useful model for quantitative studies on dopamine receptor agonists and antagonists.

Animals↗

Cholinergic lesions of mouse striatum induced by AF64A alter D2 dopaminergic behavior and reduce D2 dopamine receptors and D2 dopamine receptor mRNA.

To determine whether dopamine receptors are expressed in acetylcholine-containing neurons intrinsic to the striatum, and to study further the interactions between the dopaminergic and cholinergic systems, the irreversibly acting cholinergic neurotoxin, ethylcholine mustard aziridinium ion (AF64A), was injected unilaterally into the mouse corpus striatum, and rotational behavior induced by dopamine agonists and certain molecular events associated with this lesion were determined 7 days after lesioning. Brains were analyzed for D2 dopamine receptors by autoradiography, using [3H](-)sulpiride as a ligand, and for D2 dopamine receptor mRNA and glutamic acid decarboxylase mRNA by Northern blot analysis, using selective radiolabelled oligonucleotide probes. Choline uptake sites were determined by binding assays using [3H]hemicholinium-3, a selective choline reuptake blocker, as a ligand. Mice with intrastriatal injections of AF64A showed ipsilateral rotational responses to the non-selective dopamine agonist apomorphine and to the D2 dopamine agonists, pergolide and quinpirole, but not to the D1 dopamine agonist SKF 38393. This was associated with a significant reduction in D2 dopamine receptors in the ipsilateral striatum and a significant decrease in the amount of D2 dopamine receptor mRNA. That AF64A produced a relatively selective cholinergic deficit was supported by the evidence showing that AF64A lesions significantly reduced [3H]hemicholinium-3 binding sites but did not alter glutamic acid decarboxylase (GAD) mRNA. Further, hemicholinium-3, prevented the AF64A-induced changes in rotational behavior. These results suggest that striatal cholinergic interneurons contain D2 dopamine receptors and express the D2 dopamine receptor gene, and that these interneurons are involved in dopamine-mediated rotational behavior.

Animals↗

Distribution of D1- and D2-dopamine receptors, and dopamine and its metabolites in the human brain.

Densities and distribution of D1-dopamine and D2-dopamine receptors were investigated in vitro using [3H]SCH 23390 and [3H]raclopride in receptor binding assays and autoradiography on human post mortem whole hemisphere slices to serve as anatomical correlates to PET studies using [11C]SCH 23390 and [11C]raclopride. In addition, the levels of dopamine and its metabolites were determined by HPLC in various brain regions. Both dopamine receptor subtypes, as well as dopamine, HVA and DOPAC, were primarily found in the basal ganglia. Very high densities of D1-dopamine receptors were found particularly in the medial caudate nucleus, whereas D2-dopamine receptors were evenly distributed throughout the caudate. The densities of D1- and D2-dopamine receptors were similar in the caudate nucleus and the putamen, whereas there were 4 to 7 times higher densities of the D1- than of the D2-dopamine receptors in several limbic and neocortical regions. The receptor distribution in the autoradiographic study was consistent with that demonstrated in the living human brain using [11C]SCH 23390 and [11C]raclopride.

3,4-Dihydroxyphenylacetic Acid↗

Expression of stereotyped behaviour requires stimulation of nigral D1 dopamine receptors.

Dopamine receptors in the pars reticulata of the substantia nigra were inactivated following bilateral injections of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ). Loss of D1, but not D2, receptors was associated with a significant decrease in the incidence of stereotyped head-down sniffing elicited by the mixed D1/D2 receptor agonist, apomorphine. The results support the hypothesis that D1 receptors in the substantia nigra are necessary for the expression of dopamine mediated stereotyped behaviour.

Animals↗