Publications
109 results found
Kalk NJ, Owen D, Reynolds R, et al., 2012, Affinity of commonly-prescribed benzodiazepines for the 18 kDa translocator protein (TSPO): implications for imaging studies, 9th International Symposium on Functional Neuroreceptor Mapping of the Living Brain (NRM), Publisher: NATURE PUBLISHING GROUP, Pages: S52-S53, ISSN: 0271-678X
Tyacke RJ, Fisher A, Robinson ESJ, et al., 2012, Evaluation and initial in vitro and ex vivo characterization of the potential positron emission tomography ligand, BU99008 (2-(4,5-Dihydro-1H-imidazol-2-yl)-1-methyl-1H-indole), for the imidazoline2 binding site, SYNAPSE, Vol: 66, Pages: 542-551, ISSN: 0887-4476
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- Citations: 35
Carhart-Harris RL, Erritzoe DE, Williams TM, et al., 2012, The neural correlates of the psychedelic state as determined by fMRI studies with psilocybin, Proceedings of the National Academy of Sciences of USA
Psychedelic drugs have a long history of use in healing ceremonies, but despite renewed interest in their therapeutic potential, we continue to know very little about howthey work in the brain. Here we used psilocybin, a classic psychedelic found in magic mushrooms, and a task-free functional MRI (fMRI) protocol designed to capture the transition from normalwaking consciousness to the psychedelic state. Arterial spin labeling perfusion and blood-oxygen leveldependent (BOLD) fMRI were used to map cerebral blood flow and changes in venous oxygenation before and after intravenous infusions of placebo and psilocybin. Fifteen healthy volunteers were scanned with arterial spin labeling and a separate 15 with BOLD. As predicted, profound changes in consciousness were observed after psilocybin, but surprisingly, only decreases in cerebral blood flow and BOLD signal were seen, and these were maximal in hub regions, such as the thalamus and anterior and posterior cingulate cortex (ACC and PCC). Decreased activity in the ACC/medial prefrontal cortex (mPFC) was a consistent finding and the magnitude of this decrease predicted the intensity of the subjective effects. Based on these results, a seed-based pharmaco-physiological interaction/functional connectivity analysis was performed using a medial prefrontal seed. Psilocybin caused a significant decrease in the positive coupling between the mPFC and PCC. These results strongly imply that the subjective effects of psychedelic drugs are caused by decreased activity and connectivity in the brain’s key connector hubs, enabling a state of unconstrained cognition.
Carhart-Harris RL, Williams TM, Sessa B, et al., 2011, The administration of psilocybin to healthy, hallucinogen-experienced volunteers in a mock-functional magnetic resonance imaging environment: a preliminary investigation of tolerability, JOURNAL OF PSYCHOPHARMACOLOGY, Vol: 25, Pages: 1562-1567, ISSN: 0269-8811
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- Citations: 30
Quelch DR, Nutt DJ, Parker CA, et al., 2011, EFFECTS OF CELLULAR ENVIRONMENTS ON PET RADIOLIGAND BINDING - AN APPLICATION TO DOPAMINE AND OPIOID RECEPTOR IMAGING, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A60-A60, ISSN: 0269-8811
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- Citations: 1
Carhart-Harris RL, Erritzoe DE, Williams TM, et al., 2011, DECREASED CEREBRAL BLOOD FLOW AFTER INTRAVENOUS PSILOCYBIN, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A39-A39, ISSN: 0269-8811
Tyacke RJ, Durant CF, Paterson LM, et al., 2011, EFFECTS OF ACUTE INHALATION OF VAPORIZED CANNABIS OR PLACEBO ON CARDIOVASCULAR AND SACCADIC EYE MOVEMENT MEASURES: A PILOT STUDY, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A37-A37, ISSN: 0269-8811
Quelch DR, Tyacke RJ, Nutt DJ, et al., 2011, Assessment of cellular environments on radioligand binding - an application to opioid receptor PET imaging, European-College-of-Neuropsychopharmacology Workshop on Neuropsychopharmacology for Young Scientists in Europe, Publisher: ELSEVIER SCIENCE BV, Pages: S7-S8, ISSN: 0924-977X
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- Citations: 1
Kealey S, Husbands SM, Casey E, et al., 2011, Synthesis and in vivo evaluation of [<SUP>11</SUP>C]BU99008 as a ligand for the imidazoline I<sub>2</sub> binding site, JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, Vol: 54, Pages: S304-S304, ISSN: 0362-4803
Paterson LM, Tyacke RJ, Nutt DJ, et al., 2010, Measuring endogenous 5-HT release by emission tomography: promises and pitfalls, JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM, Vol: 30, Pages: 1682-1706, ISSN: 0271-678X
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- Citations: 108
Tyacke RJ, Lingford-Hughes A, Reed LJ, et al., 2010, GABAB Receptors in Addiction and Its Treatment, Vol: 58, Pages: 373-396
The GABAB receptor plays an important role in the control of neuro- transmitter release, and experiments using preclinical models have shown that modulation of this receptor can have profound effects on the reward process. This ability to affect the reward process has led to clinical investiga- tions into the possibility that this could be a viable target in the treatment of addiction. Presented here is an overview of a number of studies testing this hypothesis in different drug dependencies. The studies reviewed have used the GABAB receptor agonist baclofen, which is currently the only GABAB agonist for use in humans. In addition, studies using the non-specific GABAB receptor agonists vigabatrin and tiagabine have been included. In some of the studies these were found to have efficacy in the initiation and mainte- nance of abstinence, as an anti-craving treatment and alleviation of with- drawal syndromes, while in other studies showing limited effects. However, there is enough evidence to suggest that modulators of the GABAB receptor have potential as adjunct treatments to aid in the initiation of abstinence, maintenance of abstinence, and prevention of cue-related relapse in some addictions. This potential is at present poorly understood or studied and warrants further investigation.
Harrison L, Griffith L, Koukouni E, et al., 2010, NEUROPSYCHOLOGICAL CHARACTERISTICS OF PATIENTS UNDERGOING DEEP BRAIN STIMULATION FOR TREATMENT RESISTANT DEPRESSION: BASELINE MEASURES AND SINGLE CASE REPORT, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A53-A53, ISSN: 0269-8811
Kealey S, Husbands S, Casey EM, et al., 2010, Synthesis and in vivo evaluation of [11C]BU99008 as a ligand for the imidazoline 12 binding site, 8th International Symposium on Functional Neuroreceptor Mapping of the Living Brain, Publisher: ACADEMIC PRESS INC ELSEVIER SCIENCE, Pages: S127-S128, ISSN: 1053-8119
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- Citations: 4
Carhart-Harris RL, Williams TM, Sessa B, et al., 2010, THE ADMINISTRATION OF PSILOCYBIN TO HEALTHY HALLUCINOGEN-EXPERIENCED VOLUNTEERS IN A MOCK-FMRI ENVIRONMENT: A PRELIMINARY INVESTIGATION OF TOLERABILITY, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A60-A60, ISSN: 0269-8811
Budd M, Tyacke RJ, Wilson SJ, et al., 2010, SUBJECTIVE AND OBSERVED MOOD CHANGES WITH ACUTE DEEP BRAIN STIMULATION OF THE SUBGENUAL CINGULATE (SGC), OF THE VENTRAL CAPSULE OR OF THE NUCLEUS ACCUMBENS (VACNAC): PRELIMINARY RESULTS FROM A DOUBLE BLIND CROSSOVER STUDY, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A82-A82, ISSN: 0269-8811
Tyacke RJ, Robinson ESJ, Harris A, et al., 2009, Paradoxical effects of GABA on the in vivo uptake of the partial inverse GABA agonist [3H]Ro15-4513 in rat brain, 22nd Congress of the European-College-of-Neuropsychopharmacology, Publisher: ELSEVIER SCIENCE BV, Pages: S276-S277, ISSN: 0924-977X
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- Citations: 2
Kimura A, Tyacke RJ, Robinson JJ, et al., 2009, Identification of an imidazoline binding protein: Creatine kinase and an imidazoline-2 binding site, BRAIN RESEARCH, Vol: 1279, Pages: 21-28, ISSN: 0006-8993
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- Citations: 30
Tyacke RJ, Reid RHA, Grant EJ, et al., 2008, Hydrocortisone induces limbic, hippocampal and limbic/paralimbic cerebral perfusion changes as measured by 3T blood oxygenation level dependent (BOLD) phMRI, 21st Congress of the European-College-of-Neuropsychopharmacology, Publisher: ELSEVIER SCIENCE BV, Pages: S269-S269, ISSN: 0924-977X
Parker CA, Tyacke RJ, Rabiner EA, et al., 2008, [<SUP>11</SUP>C](+)RX-821024:: A novel tracer for imaging α<sub>2</sub>-adrenoceptors, 7th International Symposium on Functional Neuroreceptor Mapping of the Living Brain, Publisher: ACADEMIC PRESS INC ELSEVIER SCIENCE, Pages: T98-T98, ISSN: 1053-8119
Bailey JE, Phillips SM, Papadopoulos A, et al., 2007, The further development of a new model of GAD:: no effect of 7.5% CO<sub>2</sub> on HPA axis activation in healthy volunteers, 20th Congress of the European-College-of-Neuropsychopharmacology, Publisher: ELSEVIER SCIENCE BV, Pages: S521-S521, ISSN: 0924-977X
Tyacke RJ, Reid A, Holmes R, et al., 2007, Subjective effects of acute dose of hydrocortisone in healthy volunteers, 20th Congress of the European-College-of-Neuropsychopharmacology, Publisher: ELSEVIER SCIENCE BV, Pages: S288-S289, ISSN: 0924-977X
Paterson LM, Tyacke RJ, Robinson ESJ, et al., 2007, In vitro and in vivo effect of BU99006 (5-isothiocyanato-2-benzofuranyl-2-imidazoline) on I<sub>2</sub> binding in relation to MAO:: Evidence for two distinct I<sub>2</sub> binding sites, NEUROPHARMACOLOGY, Vol: 52, Pages: 395-404, ISSN: 0028-3908
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- Citations: 12
Saczewski F, Tabin P, Tyacke RJ, et al., 2006, 2-(4,5-Dihydroimidazol-2-yl)benzimidazoles as highly selective imidazoline I<sub>2</sub>/adrenergic α<sub>2</sub> receptor ligands, BIOORGANIC & MEDICINAL CHEMISTRY, Vol: 14, Pages: 6679-6685, ISSN: 0968-0896
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- Citations: 9
Anderson NJ, Tyacke RJ, Husbands SM, et al., 2006, In vitro and ex vivo distribution of [<SUP>3</SUP>H]harmane, an endogenous β-carboline, in rat brain, NEUROPHARMACOLOGY, Vol: 50, Pages: 269-276, ISSN: 0028-3908
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- Citations: 40
Anderson NJ, Tyacke RJ, Husbands SM, et al., 2005, Distribution of the endogenous B-carboline, harmane, in rat brain, Summer Meeting of the British-Association-for-Psychopharmacology, Publisher: SAGE PUBLICATIONS LTD, Pages: A38-A38, ISSN: 0269-8811
Saczewski F, Kobierska E, Tyacke RJ, et al., 2005, Synthesis of 2,3,5,6-tetrahydro-3H-imidazo[2,1-b] [1,3,5]benzotriazepines and their oxidative ring contraction into 1-(4,5-dihydro-1H-imidazol-2-yl)-1H-benzimidazoles., Farmaco, Vol: 60, Pages: 127-134, ISSN: 0014-827X
Syntheses of novel 5-aryl-2,3,5,6-tetrahydro-3H-imidazo[2,1-b] [1,3,5]benzotriazepine derivatives 3a-g were performed by reacting 2-(2-aminoarylimino)imidazolidines 1a-b with corresponding aryl aldehydes. The compounds 3 incorporating aminal group upon treatment with 2,3-dichloro-5,6-dicyano-1,2-benzoqinone (DDQ) underwent the oxidative ring contraction to give 1-(4,5-dihydro-1H-imidazol-2-yl)-2-aryl-benzimidazoles 4a-g. Reactions of the compounds 1a-c with carbonyldiimidazole (CDI) afforded novel 2,3,5,6-tetrahydro-1H-imidazo[2,1-b] [1,3,5]benzotriazepin-5-ones 5a-c which when heated in boiling methanol gave the corresponding 1-(4,5-dihydro-1H-imidazol-2-yl)-1,3-dihydro-2H-benzimidazol-2-ones 6a-c. Radioligand binding studies using rat central imidazoline I2 receptors and alpha2-adrenoceptors demonstrated that benzimidazoles 4a-g display a low affinity (microM) for these receptors while benzimidazol-2-ones 6a-b elicited a moderate affinity for I2 receptor with Ki values of 490 and 220 nM, respectively.
Tyacke RJ, Robinson ESJ, Lalies MDM, et al., 2005, Estimation of endogenous noradrenaline release in rat brain in vivo using [<SUP>3</SUP>H]RX 821002, SYNAPSE, Vol: 55, Pages: 126-132, ISSN: 0887-4476
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- Citations: 8
Kornicka A, Saczewski F, Petrusewicz J, et al., 2005, Synthesis and biological activities of novel 1,2,3,5-tetrahydroimidazo[2,1-<i>b</i>]quinazoline derivatives, POLISH JOURNAL OF CHEMISTRY, Vol: 79, Pages: 89-100, ISSN: 0137-5083
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- Citations: 2
Kornicka A, Saczewski F, Tyacke RJ, et al., 2005, Preparation, structure and affinity for imidazoline I2 receptors and alpha2-adrenoceptors of 1-[(4,5-dihydroimidazolidin-2-yl)imino]indan-2-ols., Acta Pol Pharm, Vol: 62, Pages: 497-502, ISSN: 0001-6837
Two enantiomers IR, 2S-(+)-cis (3a) and IS, 2R-(-)-cis (3b) of 1-[(4,5-dihydroimidazolidin-2-yl)imino]indan-2-ol were prepared by reacting 2-chloro-4,5-dihydroimidazole (1) with corresponding 1-amino-indan-2-ols (2a-b). The compounds obtained are structural analogues of PMS 952 agent containing imino bridge in place of methylene group. Compound 3a exhibited moderate almost equal activity at both imidazoline I2 receptors and alpha2-adrenoceptors, while enantiomer 3b was found to be selective for alpha2-adrenoceptors (alpha2/I2 selectivity ratio = 10.4).
Parker CA, Anderson NJ, Robinson ESJ, et al., 2004, Harmane and harmalan are bioactive components of classical clonidine-displacing substance, BIOCHEMISTRY, Vol: 43, Pages: 16385-16392, ISSN: 0006-2960
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- Citations: 32
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