Ulrika Lind,
Magnus Alm Rosenblad,
Linda Hasselberg Frank,
Susanna Falkbring,
Lars Brive,
Jonne M Laurila,
Katariina Pohjanoksa,
Anne Vuorenpää,
Jyrki P Kukkonen,
Lina Gunnarsson,
Mika Scheinin,
Lena G E Mårtensson Lindblad and
Anders Blomberg
Abstract
We now report that medetomidine induces hyperactivity in the barnacle larvae to disrupt the settling process. To identify the molecular targets of medetomidine, we cloned five octopamine receptors from the barnacle Balanus improvisus. We show by phylogenetic analyses that one receptor (BiOctalpha) b...
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PMID: 20488921
PDF is available here.
Abstract
We found two partial sequences of putative octopamine receptors in the desert locust Schistocerca gregaria (SgOctalphaR and SgOctbetaR) and investigated their transcript levels in males and females of both phases and during the transition between long-term solitarious and gregarious locusts. The tra...
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PMID: 20223248
PDF is available here.
Jeong-Sik Lee,
Deok-Jin Jang,
Nuribalhae Lee,
Hyoung-Gon Ko,
Hyoung Kim,
Yong-Seok Kim,
Byungwoo Kim,
Junehee Son,
Sung Hyun Kim,
Heekyoung Chung,
Mun-Yong Lee,
Woon Ryoung Kim,
Woong Sun,
Min Zhuo,
Ted Abel,
Bong-Kiun Kaang and
Hyeon Son
Abstract
We have tested whether the antidepressive effect of the cAMP cascade is mediated by VEGF in the adult hippocampus. We used a conditional genetic system in which the Aplysia octopamine receptor (Ap oa(1)), a G(s)-coupled receptor, is transgenically expressed in the forebrain neurons of mice. Chronic...
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PMID: 19571140
PDF is available here.
Abstract
We studied the roles of octopaminergic and dopaminergic neurons in appetitive and aversive memory recall in olfactory and visual conditioning in crickets. We found that pharmacological blockade of octopamine and dopamine receptors impaired aversive memory recall and appetitive memory recall, respect...
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PMID: 19653886
PDF is available here.
Abstract
p-Tyramine induced a concentration-dependent (0.1-3 mM) vasoconstriction. The maximum response and pD(2) value for p-tyramine was unaffected by endothelium removal or pre-treatment with antagonists for adrenoceptors, histamine, dopamine or 5-HT receptors. beta-PEA also produced a concentration-depen...
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PMID: 18604230
PDF is available here.
Abstract
We examined the pharmacological and functional properties of the cloned OA receptor, using OA enantiomers. The wild-type OA receptor exhibited significant stereoselectivity for OA enantiomers in cAMP production and binding affinity, but not in calcium signaling response. On the contrary, the Y412F m...
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PMID: 18395516
PDF is available here.
Carolina C Isiegas,
Conor C McDonough,
Ted T Huang,
Robbert R Havekes,
Sara S Fabian,
Long-Jun LJ Wu,
Hui H Xu,
Ming-Gao MG Zhao,
Jae-Ick JI Kim,
Yong-Seok YS Lee,
Hye-Ryeon HR Lee,
Hyoung-Gon HG Ko,
Nuribalhae N Lee,
Sun-Lim SL Choi,
Jeong-Sik JS Lee,
Hyeon H Son,
Min M Zhuo,
Bong-Kiun BK Kaang and
Ted T Abel
Abstract
We have developed a novel conditional genetic system in mice based on the heterologous expression of an Aplysia octopamine receptor, a G-protein-coupled receptor whose activation by its natural ligand octopamine leads to rapid and transient increases in cAMP. We find that activation of this receptor...
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PMID: 18550764
PDF is available here.
Abstract
We investigated the cardiac effects of the trace amines p-tyramine, beta-phenylethylamine, octopamine, and tryptamine. Isolated rat hearts were perfused in the presence of trace amines, monitoring the hemodynamic variables. In addition, radioligand binding experiments with [3H]-p-tyramine and [125I]...
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PMID: 18486124
PDF is available here.
Abstract
AY333178 (from Periplaneta americana, 628 AAs) was selected as a target octopamine receptor (OAR) class OAR2 for this study using Discovery Studio (DS Modeling1.1/1.2, Accelrys Inc.). Blast similarity search was performed and identified that AY333178 contains N-terminal domain of GPCR. Based upon Bl...
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PMID: 18430608
PDF is available here.
Abstract
We examined the effects of some monoamine receptor antagonists (including beta-adrenergic receptor antagonist propranolol, beta-adrenergic receptor antagonist/5-HT1A/1B receptor antagonist pindolol, alpha2-adrenergic receptor antagonists yohimbine and idazoxan and 5-HT3 receptor antagonist tropisetr...
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PMID: 18717332
PDF is available here.
Abstract
These results indicate that normal cellular redox is crucial for olfactory processing, and chelation of iron prevents ROS-mediated oxidative stress. Furthermore, octopamine receptor disruption, and FAC-mediated oxidative stress confer two independent mechanisms that impair olfactory learning and mem...
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PMID: 18410182
PDF is available here.
Abstract
The molecular mechanisms of action of the polycationic peptides--polylysine homo- and heterodendrimers on functional activity of biogenic amines- and peptide hormones-sensitive adenylyl; cyclase signaling system (AC system) in the myocardium and the brain of rats were studied. These peptides are exp...
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PMID: 19198542
PDF is available here.
Abstract
We have investigated the presence of neurohormone GPCRs in Tribolium and compared them with those from the fruit fly Drosophila melanogaster (Diptera) and the honey bee Apis mellifera (Hymenoptera). We found 20 biogenic amine GPCRs in Tribolium (21 in Drosophila; 19 in the honey bee), 48 neuropeptid...
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PMID: 18054377
PDF is available here.
Abstract
Insect thoracic ganglia contain efferent octopaminergic unpaired median neurons (UM neurons) located in the midline, projecting bilaterally and modulating neuromuscular transmission, muscle contraction kinetics, sensory sensitivity and muscle metabolism. In locusts, these neurons are located dorsall...
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PMID: 18021797
PDF is available here.
Abstract
We created a drug-drug interaction network from drug package inserts and characterized drug interactions. The known information about the potential risk of drug interactions is described in drug package inserts. Japanese drug package inserts are stored in the JAPIC (Japan Pharmaceutical Information...
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PMID: 19425139
PDF is available here.
Abstract
Our data suggest that although tyraminergic and octopaminergic signaling yield identical phenotypes in these olfactory assays, they act independently through distinct receptors to modulate the ASH-mediated locomotory circuit and that C. elegans is a useful model to study the aminergic modulation of...
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PMID: 18057198
PDF is available here.
Abstract
We employed bioinformatics to identify genes encoding putative B. malayi BARs. Surprisingly, the B. malayi genome contains half of the genes predicted to encode BARs in the genomes of free-living nematodes such as Caenorhabditis elegans or C. briggsae; however, all of the predicted B. malayi recepto...
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PMID: 18027007
PDF is available here.
Abstract
Results in this study are consistent with those of Murdock and his colleagues who clearly demonstrated that clonidine, an agonist of octopaminergic receptors in some insects, significantly increases sucrose feeding. Their studies, however, did not examine the effect of clonidine on protein feeding....
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PMID: 17692332
PDF is available here.
Abstract
We investigate the effect of an octopamine receptor agonist and an antagonist on the locomotor behavior of stung and control cockroaches. We show that in cockroaches stung by a wasp the octopamine receptor agonist chlordimeform induces a significant increase in spontaneous walking. In good agreement...
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PMID: 18055629
PDF is available here.
Abstract
'Click resins' enable solid phase supported reactions to work under nearly perfect conditions fulfilling the requirements of click chemistry. Utilizing the formylpyrrolylmethyltriazole (FPMT) linker 6, which is readily available via copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), a BAL strat...
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PMID: 17827018
PDF is available here.
Abstract
We tested 88,000 chemicals for the ability to extend the lifespan of adult Caenorhabditis elegans nematodes. Here we report that a drug used as an antidepressant in humans increases C. elegans lifespan. In humans, this drug blocks neural signalling by the neurotransmitter serotonin. In C. elegans, t...
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PMID: 18033297
PDF is available here.
Abstract
The receptor binding affinities of the three drug candidates 1 (SLV310), 2 (SLV313), and 3 (SLV314) were positioned against the results from nine (a)typical antipsychotic drugs. The receptor binding data from sixteen monoaminergic receptors served as the input in a principal component analysis (PCA)...
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PMID: 17880057
PDF is available here.
Abstract
We have sequenced this putative octopamine receptor gene in tick strains from America. The American ticks have a sequence almost identical to that of the Australian ticks with no deletions or additions in the open reading frame. In a Brazilian strain and a Mexican strain that are very resistant to a...
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PMID: 17662534
PDF is available here.
Abstract
Octopamine functions as a neuromodulator, neurotransmitter, and neurohormone in insect nervous systems. Octopamine has a prominent role in influencing multiple physiological events: (a) as a neuromodulator, it regulates desensitization of sensory inputs, arousal, initiation, and maintenance of vario...
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PMID: 17484052
PDF is available here.
Abstract
Noradrenaline and serotonin have previously been demonstrated to facilitate the transmission between descending reticulospinal tracts fibres and commissural interneurons coordinating left-right hindlimb muscle activity. The aim of the present study was to investigate the contribution of subclasses o...
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PMID: 17767499
PDF is available here.
Abstract
We have identified a putative TA receptor (Bm4) in the recently completed Brugia malayi genome and compared its pharmacology to its putative Caenorhabditis elegans orthologue, TYRA-2, under identical expression and assay conditions. TYRA-2 and Bm4 are the most closely related C. elegans and B. malay...
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PMID: 17537528
PDF is available here.
Abstract
We previously reported the isolation of an OAR (BmOAR1) from Bombyx mori. In the study presented here, five mutated BmOAR1s were constructed with a point mutation in the putative binding crevice and expressed in HEK-293 cells. The S202A mutant receptor was found to retain the cAMP response to OA as...
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PMID: 17469804
PDF is available here.
Abstract
Mining of the human genome has revealed approximately 7000 novel proteins, which could serve as potential targets for the development of novel therapeutics. Of these, approximately 2000 are predicted to be G-protein coupled receptors. Within this group of proteins, a family of 18 mammalian receptors...
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PMID: 18473983
PDF is available here.
Abstract
Classical biogenic amines (adrenaline, noradrenaline, dopamine, serotonin and histamine) interact with specific families of G protein-coupled receptors (GPCRs). The term 'trace amines' is used when referring to p-tyramine, beta-phenylethylamine, tryptamine and octopamine, compounds that are present...
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PMID: 17088868
PDF is available here.
Abstract
A cDNA encoding an octopamine (OA) receptor (BmOAR1) was isolated from the nerve tissue of silkworm (Bombyx mori) larvae. Comparison of amino acid sequences showed that BmOAR1 is highly identical to OA receptors isolated from Periplaneta americana (Pa oa(1)), Apis mellifera (AmOA1), and Drosophila m...
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PMID: 17201769
PDF is available here.
Abstract
We give a review of our current knowledge on Drosophila melanogaster GPCRs and use this information to annotate the neurohormone GPCR genes present in the recently sequenced genome from the honey bee Apis mellifera. We found 35 neuropeptide receptor genes in the honey bee (44 in Drosophila) and two...
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PMID: 17070981
PDF is available here.
Abstract
We cloned two putative serotonin receptors (Ms5HT1A and Ms5HT1B) and one putative OA (MsOAR) receptor from the moth Manduca sexta. Ms5HT1A and Ms5HT1B were both similar to 5HT1-type receptors but differed from each other in their N-terminus and 3rd cytoplasmic loop. Ms5HT1A was nearly identical to a...
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PMID: 16935223
PDF is available here.
Abstract
Research was done on pharmacological-physiological development of the bronchial receptor system on the smooth muscles of trachea in the newborn children, alive-born and stillborn children. Monitored was the response on: acetylcholine, dopamine, histamine and serotonin in different molar concentratio...
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PMID: 16995853
PDF is available here.
Abstract
We summarize current knowledge concerning the aminergic control of cockroach salivary glands and discuss our efforts to characterize Periplaneta biogenic amine receptors molecularly....
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PMID: 16783825
PDF is available here.
Abstract
RS-8359 is a new reversible inhibitor of monoamine oxidase A (RIMA). With a selectivity ratio of about 2200 for the A:B enzyme types, it is one of the most specific of this class of compounds. As a result, it shows relatively little effect upon blood pressure when administered together with tyramine...
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PMID: 9466163
PDF is available here.
Abstract
These results are consistent with previous evidence that antidepressant drugs have a tendency to substitute for clozapine and that muscarinic receptor antagonism may mediate the discriminative stimulus properties of 5.0 mg/kg clozapine. The lack of stimulus generalization from either clozapine train...
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PMID: 16495726
PDF is available here.
Abstract
We chose dopamine receptor genes (DRD1 and DRD2), NCAM, and COMT as examples of genes with CpG islands around the promoter region, and serotonin receptor genes (HTR2A and HTR3A), HCRT, and DRD3 as genes without CpG islands. Methylation states were investigated in fetal brain, fetal liver, placenta,...
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PMID: 16544050
PDF is available here.
Abstract
We have cloned this gene and expressed it in Chinese hamster ovary cells. After testing various ligands for G protein-coupled receptors, we found that the receptor was specifically activated by tyramine (EC(50), 5x10(-7)M) and that it showed no cross-reactivity with beta-phenylethylamine, octopamine...
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PMID: 16274665
PDF is available here.
Abstract
From codeine, four different 2-aryl substituted apomorphines were synthesised in 6 steps each. Oxidation of codeine with IBX followed by acid catalysed rearrangement gave morphothebaine, which was selectively triflylated at the 2-position and subsequently O-acetylated at the 11-position. The resulti...
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PMID: 16267586
PDF is available here.
Abstract
Insect octopamine receptors are G-protein coupled receptors. They can be coupled to second messenger pathways to mediate either increases or decreases in intracellular cyclic AMP levels or the generation of intracellular calcium signals. Insect octopamine receptors were originally classified on the...
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PMID: 16211376
PDF is available here.
Abstract
We summarize current thinking on: (i) the extent to which different 'atypical' drugs induce weight gain; (ii) the possible roles of various neurotransmitters and neuropeptides in this adverse drug reaction; and (iii) the state of development of animal models in this area. We also outline major areas...
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PMID: 16050940
PDF is available here.
Abstract
We studied the effects of OA and DA receptor antagonists on appetitive olfactory learning with water reward, and aversive olfactory learning with saline punishment in the cricket Gryllus bimaculatus. Crickets injected with epinastine or mianserin, OA receptor antagonists, into the hemolymph exhibite...
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PMID: 16190895
PDF is available here.
Abstract
Tyramine (TA), a biogenic amine, attenuates intracellular cAMP production by acting on its receptor in insects. Several non-biogenic amines were examined for their actions on native and heterologously expressed silkworm TA receptors. 5-(4-Hydroxyphenyl)oxazole, which showed an attenuating effect on...
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PMID: 15986379
PDF is available here.
Abstract
We report the isolation, cloning, and tissue expression of a putative octopamine/tyramine receptor from the locust, Locusta migratoria. Degenerate oligonucleotides in PCR reactions were first used to obtain partial cDNA sequences and then these partial sequences were used in screens to obtain a full...
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PMID: 15986383
PDF is available here.
Abstract
We report here a preliminary investigation into the true extent of the distribution of this type of transporter using RT-PCR with a set of degenerate primers selective for monoamine transporters on cDNAs made from the nervous systems of a range of arthropods. PCR products encoding the N-terminal reg...
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PMID: 15986385
PDF is available here.
Abstract
The receptors of amine subfamily are specifically major drug targets for therapy of nervous disorders and psychiatric diseases. The recognition of novel amine type of receptors and their cognate ligands is of paramount interest for pharmaceutical companies. In the past, Chou and co-workers have show...
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PMID: 15980444
PDF is available here.
Abstract
We have identified a second C. elegans gene, tyra-2 (F01E11.5) that encodes a tyramine receptor. This is the first identification of multiple tyramine receptor genes in any invertebrate. Membranes from COS-7 cells expressing TYRA-2 bind [(3)H]tyramine with high affinity with a K(d) of 20 +/- 5 nM. O...
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PMID: 15953361
PDF is available here.
Abstract
Trace amines (TAs) are endogenous compounds that are related to biogenic amine neurotransmitters and are present in the mammalian nervous system in trace amounts. Although their pronounced pharmacological effects and tight link to major human disorders such as depression and schizophrenia have been...
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PMID: 15860375
PDF is available here.
Abstract
We describe the functional characterization of two genes from Drosophila melanogaster that encode three octopamine receptors. The first gene (Dmoa1) codes for two polypeptides that are generated by alternative splicing. When heterologously expressed, both receptors cause oscillatory increases of the...
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PMID: 15816867
PDF is available here.
Abstract
This paper reports the role of the tyramine (TA) receptor cascade in the insecticidal activity of plant essential oils. A TA receptor cDNA encoding a putative seven transmembrane domain G-protein coupled receptor was amplified from Drosophila melanogaster head cDNA phage library. The encoded protein...
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PMID: 15763467
PDF is available here.
Abstract
This study reveals that the tyramine receptor gene, Amtyr1, is expressed in the developing brain, as well as in the brain of the adult worker honey bee. Changes in levels of Amtyr1 expression were examined using Northern analysis. Age-related increases in Amtyr1 transcript levels were observed not o...
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PMID: 15672398
PDF is available here.
Abstract
We present evidence that a form of experience-dependent plasticity of aggression in crickets is mediated by octopamine, the invertebrate counterpart of noradrenaline. In a forced-fight paradigm, the experience of flying maximized the aggressiveness of crickets at their first encounter and accelerate...
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PMID: 15703397
PDF is available here.
Abstract
We show that spider peripheral mechanoreceptors are innervated by octopamine-containing efferents. The mechanosensory neurons have octopamine receptors colocalized with synapsin labeling in the efferent fibers. In addition, octopamine enhances the electrical response of the sensory neurons to mechan...
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PMID: 15703413
PDF is available here.
Abstract
The flatworm nervous system employs a wide repertoire of neuroactive substances, including small chemical messengers, the so called classical transmitters, and several types of neuropeptides. A large body of research accumulated over four decades has provided a wealth of information on the tissue lo...
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PMID: 16569290
PDF is available here.
Abstract
Cross-genome phylogenetic analyses were performed to identify eight major groups of GPCRs dividing them into 32 clusters of 371 human and 113 Drosophila proteins (excluding olfactory, taste and gustatory receptors) and reveal unexpected levels of evolutionary conservation across human and Drosophila...
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PMID: 16091152
PDF is available here.
Abstract
We have characterized alternatively spliced Caenorhabditis elegans tyramine receptor isoforms (SER-2 and SER-2A) that differ by 23 amino acids within the mid-region of the third intracellular loop. Membranes prepared from cells expressing either SER-2 or SER-2A bind [3H]lysergic acid diethylamide (L...
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PMID: 15569254
PDF is available here.
Abstract
We have cloned three amine receptors, serotonin, tyramine, and dopamine, from cDNA derived from foreleg tarsus of P. xuthus, and determined structures of both cDNA and genomic genes. The phenylethylamine (tyramine and dopamine) receptors were expressed preferentially in brain and chemosensory organs...
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PMID: 15544938
PDF is available here.
Abstract
To identify amino acid residues interacting with tyramine (TA) in the Bombyx mori TA (BmTA) receptor, several mutant receptors were expressed in HEK-293 cells and examined for their abilities to bind TA and to attenuate forskolin-stimulated cAMP production in response to TA. The D134A BmTA receptor...
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PMID: 15373809
PDF is available here.
Abstract
The binding site in G protein-coupled cationic biogenic amine receptors is formed in the cleft of the seven transmembrane segments. Upon binding the ligand, the receptors are activated or inactivated through the conformational changes of the transmembrane segments. G protein-coupled receptors bind f...
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PMID: 15368572
PDF is available here.