List of works - Mika Scheinin

3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α2-adrenoceptor compared to the imidazoline I1 receptor

scientific article published on 11 November 2010

A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin

scientific article

A polymorphism in the protein kinase C gene PRKCB is associated with α2-adrenoceptor-mediated vasoconstriction

scientific article published on March 2013

Amino Acid Plasma Profiles from a Prolonged-Release Protein Substitute for Phenylketonuria: A Randomized, Single-Dose, Four-Way Crossover Trial in Healthy Volunteers

scientific article published on 02 June 2020

Antinociceptive synergism of MD-354 and clonidine. Part II. The alpha-adrenoceptor component.

scientific article published on 28 March 2010

CYP2A6 genetic variation and dexmedetomidine disposition

scientific article

Candida antarctica Lipase A-Based Enantiorecognition of a Highly Strained 4-Dibenzocyclooctynol (DIBO) Used for PET Imaging

scientific article published on 17 February 2020

Cardiovascular and sedation reversal effects of intramuscular administration of atipamezole in dogs treated with medetomidine hydrochloride with or without the peripheral α2-adrenoceptor antagonist vatinoxan hydrochloride

scientific article published on 01 October 2019

Cardiovascular effects of premedication with medetomidine alone and in combination with MK-467 or glycopyrrolate in dogs subsequently anesthetized with isoflurane.

scientific article published in November 2017

Clinical effects and pharmacokinetic variables of romifidine and the peripheral α2 -adrenoceptor antagonist MK-467 in horses.

scientific article published on 26 February 2016

Comparison of simultaneous measurement of mouse locomotor activity by radiotelemetry and photobeam methods

scientific article published on 16 September 2014

Decreased Myocardial Free Fatty Acid Uptake in Patients With Idiopathic Dilated Cardiomyopathy: Evidence of Relationship With Insulin Resistance and Left Ventricular Dysfunction

article

Detecting a dexmedetomidine-evoked reduction of noradrenaline release in the human brain with the alpha2C-adrenoceptor PET ligand [11C]ORM-13070.

scientific article published on 12 November 2015

Detomidine and the combination of detomidine and MK-467, a peripheral alpha-2 adrenoceptor antagonist, as premedication in horses anaesthetized with isoflurane

scientific article

Different Metabolic Responses of Human Brown Adipose Tissue to Activation by Cold and Insulin

article

Differential Internalization Rates and Postendocytic Sorting of the Norepinephrine and Dopamine Transporters Are Controlled by Structural Elements in the N Termini.

scientific article published on 19 January 2016

Dorsal hand vein responses to the α₁-adrenoceptor agonist phenylephrine do not predict responses to the α₂-adrenoceptor agonist dexmedetomidine

scientific article published on 11 December 2010

Effect of oral KETOPROFEN treatment in acute respiratory disease outbreaks in finishing pigs.

scientific article published on 6 March 2018

Effects of MK-467 on the antinociceptive and sedative actions and pharmacokinetics of medetomidine in dogs.

scientific article

Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene.

scientific article published on 15 August 2013

Effects of dexmedetomidine and MK-467 on plasma glucose, insulin and glucagon in a glibenclamide-induced canine hypoglycaemia model

scientific article published on 21 September 2018

Effects of terbinafine and itraconazole on the pharmacokinetics of orally administered tramadol

scientific article published on 06 January 2015

Effects of the peripherally acting α2-adrenoceptor antagonist MK-467 on cardiopulmonary function in sheep sedated by intramuscular administration of medetomidine and ketamine and reversed by intramuscular administration of atipamezole

scientific article published on 01 September 2018

Effects of the α2-adrenoceptor agonist medetomidine on the distribution and clearance of alfaxalone during coadministration by constant rate infusion in dogs

scientific article published in August 2017

Effects of variation in the human alpha2A- and alpha2C-adrenoceptor genes on cognitive tasks and pain perception.

scientific article

Effects of vatinoxan on cardiorespiratory function and gastrointestinal motility during constant-rate medetomidine infusion in standing horses

scientific article published on 14 March 2019

Effects of vatinoxan on cardiorespiratory function, fecal output and plasma drug concentrations in horses anesthetized with isoflurane and infusion of medetomidine

scientific article published on 27 July 2019

Evidence that the multiflorine-derived substituted quinazolidine 55P0251 augments insulin secretion and lowers blood glucose via antagonism at α2 -adrenoceptors in mice

scientific article published on 07 November 2019

Fluorinated analogues of marsanidine, a highly α2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities

scientific article published on 28 September 2014

Foundations of human consciousness: Imaging the twilight zone

scientific article published on 28 December 2020

Gene expression profiles and signaling mechanisms in α2B-adrenoceptor-evoked proliferation of vascular smooth muscle cells

scientific article

Genetic variations in the α(2A)-adrenoreceptor are associated with blood pressure response to the agonist dexmedetomidine

scientific article

High-throughput screening with a miniaturized radioligand competition assay identifies new modulators of human α2-adrenoceptors.

scientific article

Identification of a novel 12-nucleotide insertion polymorphism in the promoter region of ADRA2B: full linkage with the 9-nucleotide deletion in the coding region and influence on transcriptional activity.

scientific article

Imaging of α2C-adrenoceptors in the living brain: a method to monitor noradrenaline release?

scientific article published on 12 June 2015

In vivo PET imaging of beta-amyloid deposition in mouse models of Alzheimer's disease with a high specific activity PET imaging agent [(18)F]flutemetamol

scientific article published on August 2014

Increased Energy Expenditure, Lipolysis and Hyperinsulinemia Confer Resistance to Central Obesity and Type 2 Diabetes in Mice Lacking Alpha2α-Adrenoceptors

scientific article published on 24 July 2018

Influence of MK-467, a peripherally acting α2-adrenoceptor antagonist on the disposition of intravenous dexmedetomidine in dogs

scientific article

Intranasal naloxone rapidly occupies brain mu-opioid receptors in human subjects

scientific article published on 13 March 2019

Involvement of the first transmembrane segment of human α(2) -adrenoceptors in the subtype-selective binding of chlorpromazine, spiperone and spiroxatrine.

scientific article

Longitudinal amyloid imaging in mouse brain with 11C-PIB: comparison of APP23, Tg2576, and APPswe-PS1dE9 mouse models of Alzheimer disease.

scientific article

Mechanism-based population pharmacokinetic and pharmacodynamic modeling of intravenous and intranasal dexmedetomidine in healthy subjects.

scientific article published on 2 August 2015

Might the observed α(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?

scientific article published on 31 January 2012

Molecular mechanisms underlying mifepristone's agonistic action on ovarian cancer progression

scientific article published on 26 August 2019

Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine

scientific article

Oral bioavailability of ospemifene improves with food intake.

scientific article published in October 2013

Peripheral α 2 -adrenoceptor antagonism affects the absorption of intramuscularly coadministered drugs

scientific article published on 03 February 2018

Pharmacodynamic and pharmacokinetic profile of SM-1, a triple-drug combination to increase total sleep time

scientific article published on 01 November 2019

Pharmacokinetics and Sedative Effects of Intranasal Dexmedetomidine in Ambulatory Pediatric Patients

scientific article published on 01 April 2020

Pharmacokinetics of [¹⁸F]flutemetamol in wild-type rodents and its binding to beta amyloid deposits in a mouse model of Alzheimer's disease.

scientific article published on 17 July 2012

Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors

scientific article (publication date: 17 August 2001)

Plasma concentration and cardiovascular effects of intramuscular medetomidine combined with three doses of the peripheral alpha2-antagonist MK-467 in dogs.

scientific article

Plasma drug concentrations and clinical effects of a peripheral alpha-2-adrenoceptor antagonist, MK-467, in horses sedated with detomidine.

scientific article

Population Modelling of Dexmedetomidine Pharmacokinetics and Haemodynamic Effects After Intravenous and Subcutaneous Administration

scientific article published on 27 May 2020

Potentiation of Glibenclamide Hypoglycaemia in Mice by MK-467, a Peripherally Acting Alpha2-Adrenoceptor Antagonist.

scientific article published on 30 July 2015

Premedication with intranasal dexmedetomidine decreases barbiturate requirement in pediatric patients sedated for magnetic resonance imaging: a retrospective study

scientific article published on 13 February 2019

Probiotic With or Without Fiber Controls Body Fat Mass, Associated With Serum Zonulin, in Overweight and Obese Adults-Randomized Controlled Trial

scientific article

Quantitative determination of α(2B)-adrenoceptor-evoked myosin light chain phosphorylation in vascular smooth muscle cells.

scientific article

Radiosynthesis and Preclinical Evaluation of an α2A-Adrenoceptor Tracer Candidate, 6-[18F]Fluoro-marsanidine

scientific article published on 01 October 2019

Reply to “Letter to the editor: ‘Deconstructing the dogma of sympathetic restraint and its role in the cardiovascular response to exercise’”

scientific article published on 01 February 2014

Rifampicin markedly decreases the exposure to oral and intravenous tramadol

scientific article published on 15 December 2012

Safety and efficacy of AMG 714 in adults with coeliac disease exposed to gluten challenge: a phase 2a, randomised, double-blind, placebo-controlled study

scientific article published on 04 September 2019

Safety, Tolerability, and Antihypertensive Effect of SER100, an Opiate Receptor-Like 1 (ORL-1) Partial Agonist, in Patients With Isolated Systolic Hypertension

scientific article published on 29 December 2016

Sedation with Dexmedetomidine or Propofol Impairs Hypoxic Control of Breathing in Healthy Male Volunteers: A Nonblinded, Randomized Crossover Study.

scientific article published in August 2016

Sedative Plasma Concentrations and Delirium Risk in Critical Illness.

scientific article published in January 2018

Sensitivity of [(11)C]ORM-13070 to increased extracellular noradrenaline in the CNS - a PET study in human subjects

scientific article published on 29 April 2015

Single-dose and steady-state pharmacokinetics of ospemifene, a selective estrogen receptor modulator, in postmenopausal women

scientific article published on 01 November 2013

Subcutaneously administered dexmedetomidine is efficiently absorbed and is associated with attenuated cardiovascular effects in healthy volunteers.

scientific article

Sublingual administration of detomidine to calves prior to disbudding: a comparison with the intravenous route

scientific article

Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines

scientific article published on 25 November 2011

Test-retest reliability of (11)C-ORM-13070 in PET imaging of α2C-adrenoceptors in vivo in the human brain

scientific article published on 9 September 2014

The effect of an apple polyphenol extract rich in epicatechin and flavan-3-ol oligomers on brachial artery flow-mediated vasodilatory function in volunteers with elevated blood pressure.

scientific article published on 27 October 2017

The impact of MK-467 on plasma drug concentrations, sedation and cardiopulmonary changes in sheep treated with intramuscular medetomidine and atipamezole for reversal.

scientific article published on 19 January 2018

Ticlopidine inhibits both O-demethylation and renal clearance of tramadol, increasing the exposure to it, but itraconazole has no marked effect on the ticlopidine-tramadol interaction

scientific article published on 26 October 2012

Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies

scientific article published on 14 March 2016

Treating gambling disorder with as needed administration of intranasal naloxone: a pilot study to evaluate acceptability, feasibility and outcomes

scientific article published on 21 August 2019

Trimetazidine, a metabolic modulator, has cardiac and extracardiac benefits in idiopathic dilated cardiomyopathy

scientific article

Upper Airway Collapsibility during Dexmedetomidine and Propofol Sedation in Healthy Volunteers: A Nonblinded Randomized Crossover Study

scientific article published on 01 November 2019

Validation of [(11) C]ORM-13070 as a PET tracer for alpha2c -adrenoceptors in the human brain

scientific article published on 8 January 2015

Variation in the α(2A) adrenoceptor gene and the effect of dexmedetomidine on plasma insulin and glucose.

scientific article published on September 2013

¹¹C-ORM-13070, a novel PET ligand for brain α₂C-adrenoceptors: radiometabolism, plasma pharmacokinetics, whole-body distribution and radiation dosimetry in healthy men.

scientific article

α2-adrenoceptor regulation of blood glucose homeostasis.

scientific article published on 11 April 2011

List of works by Mika Scheinin

3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α2-adrenoceptor compared to the imidazoline I1 receptor

A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin

A polymorphism in the protein kinase C gene PRKCB is associated with α2-adrenoceptor-mediated vasoconstriction

Amino Acid Plasma Profiles from a Prolonged-Release Protein Substitute for Phenylketonuria: A Randomized, Single-Dose, Four-Way Crossover Trial in Healthy Volunteers

Antinociceptive synergism of MD-354 and clonidine. Part II. The alpha-adrenoceptor component.

CYP2A6 genetic variation and dexmedetomidine disposition

Candida antarctica Lipase A-Based Enantiorecognition of a Highly Strained 4-Dibenzocyclooctynol (DIBO) Used for PET Imaging

Cardiovascular and sedation reversal effects of intramuscular administration of atipamezole in dogs treated with medetomidine hydrochloride with or without the peripheral α2-adrenoceptor antagonist vatinoxan hydrochloride

Cardiovascular effects of premedication with medetomidine alone and in combination with MK-467 or glycopyrrolate in dogs subsequently anesthetized with isoflurane.

Clinical effects and pharmacokinetic variables of romifidine and the peripheral α2 -adrenoceptor antagonist MK-467 in horses.

Comparison of simultaneous measurement of mouse locomotor activity by radiotelemetry and photobeam methods

Decreased Myocardial Free Fatty Acid Uptake in Patients With Idiopathic Dilated Cardiomyopathy: Evidence of Relationship With Insulin Resistance and Left Ventricular Dysfunction

Detecting a dexmedetomidine-evoked reduction of noradrenaline release in the human brain with the alpha2C-adrenoceptor PET ligand [11C]ORM-13070.

Detomidine and the combination of detomidine and MK-467, a peripheral alpha-2 adrenoceptor antagonist, as premedication in horses anaesthetized with isoflurane

Different Metabolic Responses of Human Brown Adipose Tissue to Activation by Cold and Insulin

Differential Internalization Rates and Postendocytic Sorting of the Norepinephrine and Dopamine Transporters Are Controlled by Structural Elements in the N Termini.

Dorsal hand vein responses to the α₁-adrenoceptor agonist phenylephrine do not predict responses to the α₂-adrenoceptor agonist dexmedetomidine

Effect of oral KETOPROFEN treatment in acute respiratory disease outbreaks in finishing pigs.

Effects of MK-467 on the antinociceptive and sedative actions and pharmacokinetics of medetomidine in dogs.

Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene.

Effects of dexmedetomidine and MK-467 on plasma glucose, insulin and glucagon in a glibenclamide-induced canine hypoglycaemia model

Effects of terbinafine and itraconazole on the pharmacokinetics of orally administered tramadol

Effects of the peripherally acting α2-adrenoceptor antagonist MK-467 on cardiopulmonary function in sheep sedated by intramuscular administration of medetomidine and ketamine and reversed by intramuscular administration of atipamezole

Effects of the α2-adrenoceptor agonist medetomidine on the distribution and clearance of alfaxalone during coadministration by constant rate infusion in dogs

Effects of variation in the human alpha2A- and alpha2C-adrenoceptor genes on cognitive tasks and pain perception.

Effects of vatinoxan on cardiorespiratory function and gastrointestinal motility during constant-rate medetomidine infusion in standing horses

Effects of vatinoxan on cardiorespiratory function, fecal output and plasma drug concentrations in horses anesthetized with isoflurane and infusion of medetomidine

Evidence that the multiflorine-derived substituted quinazolidine 55P0251 augments insulin secretion and lowers blood glucose via antagonism at α2 -adrenoceptors in mice

Fluorinated analogues of marsanidine, a highly α2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities

Foundations of human consciousness: Imaging the twilight zone

Gene expression profiles and signaling mechanisms in α2B-adrenoceptor-evoked proliferation of vascular smooth muscle cells

Genetic variations in the α(2A)-adrenoreceptor are associated with blood pressure response to the agonist dexmedetomidine

High-throughput screening with a miniaturized radioligand competition assay identifies new modulators of human α2-adrenoceptors.

Identification of a novel 12-nucleotide insertion polymorphism in the promoter region of ADRA2B: full linkage with the 9-nucleotide deletion in the coding region and influence on transcriptional activity.

Imaging of α2C-adrenoceptors in the living brain: a method to monitor noradrenaline release?

In vivo PET imaging of beta-amyloid deposition in mouse models of Alzheimer's disease with a high specific activity PET imaging agent [(18)F]flutemetamol

Increased Energy Expenditure, Lipolysis and Hyperinsulinemia Confer Resistance to Central Obesity and Type 2 Diabetes in Mice Lacking Alpha2α-Adrenoceptors

Influence of MK-467, a peripherally acting α2-adrenoceptor antagonist on the disposition of intravenous dexmedetomidine in dogs

Intranasal naloxone rapidly occupies brain mu-opioid receptors in human subjects

Involvement of the first transmembrane segment of human α(2) -adrenoceptors in the subtype-selective binding of chlorpromazine, spiperone and spiroxatrine.

Longitudinal amyloid imaging in mouse brain with 11C-PIB: comparison of APP23, Tg2576, and APPswe-PS1dE9 mouse models of Alzheimer disease.

Mechanism-based population pharmacokinetic and pharmacodynamic modeling of intravenous and intranasal dexmedetomidine in healthy subjects.

Might the observed α(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?

Molecular mechanisms underlying mifepristone's agonistic action on ovarian cancer progression

Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine

Oral bioavailability of ospemifene improves with food intake.

Peripheral α 2 -adrenoceptor antagonism affects the absorption of intramuscularly coadministered drugs

Pharmacodynamic and pharmacokinetic profile of SM-1, a triple-drug combination to increase total sleep time

Pharmacokinetics and Sedative Effects of Intranasal Dexmedetomidine in Ambulatory Pediatric Patients

Pharmacokinetics of [¹⁸F]flutemetamol in wild-type rodents and its binding to beta amyloid deposits in a mouse model of Alzheimer's disease.

Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors

Plasma concentration and cardiovascular effects of intramuscular medetomidine combined with three doses of the peripheral alpha2-antagonist MK-467 in dogs.

Plasma drug concentrations and clinical effects of a peripheral alpha-2-adrenoceptor antagonist, MK-467, in horses sedated with detomidine.

Population Modelling of Dexmedetomidine Pharmacokinetics and Haemodynamic Effects After Intravenous and Subcutaneous Administration

Potentiation of Glibenclamide Hypoglycaemia in Mice by MK-467, a Peripherally Acting Alpha2-Adrenoceptor Antagonist.

Premedication with intranasal dexmedetomidine decreases barbiturate requirement in pediatric patients sedated for magnetic resonance imaging: a retrospective study

Probiotic With or Without Fiber Controls Body Fat Mass, Associated With Serum Zonulin, in Overweight and Obese Adults-Randomized Controlled Trial

Quantitative determination of α(2B)-adrenoceptor-evoked myosin light chain phosphorylation in vascular smooth muscle cells.

Radiosynthesis and Preclinical Evaluation of an α2A-Adrenoceptor Tracer Candidate, 6-[18F]Fluoro-marsanidine

Reply to “Letter to the editor: ‘Deconstructing the dogma of sympathetic restraint and its role in the cardiovascular response to exercise’”

Rifampicin markedly decreases the exposure to oral and intravenous tramadol

Safety and efficacy of AMG 714 in adults with coeliac disease exposed to gluten challenge: a phase 2a, randomised, double-blind, placebo-controlled study

Safety, Tolerability, and Antihypertensive Effect of SER100, an Opiate Receptor-Like 1 (ORL-1) Partial Agonist, in Patients With Isolated Systolic Hypertension

Sedation with Dexmedetomidine or Propofol Impairs Hypoxic Control of Breathing in Healthy Male Volunteers: A Nonblinded, Randomized Crossover Study.

Sedative Plasma Concentrations and Delirium Risk in Critical Illness.

Sensitivity of [(11)C]ORM-13070 to increased extracellular noradrenaline in the CNS - a PET study in human subjects

Single-dose and steady-state pharmacokinetics of ospemifene, a selective estrogen receptor modulator, in postmenopausal women

Subcutaneously administered dexmedetomidine is efficiently absorbed and is associated with attenuated cardiovascular effects in healthy volunteers.

Sublingual administration of detomidine to calves prior to disbudding: a comparison with the intravenous route

Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines

Test-retest reliability of (11)C-ORM-13070 in PET imaging of α2C-adrenoceptors in vivo in the human brain

The effect of an apple polyphenol extract rich in epicatechin and flavan-3-ol oligomers on brachial artery flow-mediated vasodilatory function in volunteers with elevated blood pressure.

The impact of MK-467 on plasma drug concentrations, sedation and cardiopulmonary changes in sheep treated with intramuscular medetomidine and atipamezole for reversal.

Ticlopidine inhibits both O-demethylation and renal clearance of tramadol, increasing the exposure to it, but itraconazole has no marked effect on the ticlopidine-tramadol interaction

Transfer of SAR information from hypotensive indazole to indole derivatives acting at α-adrenergic receptors: In vitro and in vivo studies

Treating gambling disorder with as needed administration of intranasal naloxone: a pilot study to evaluate acceptability, feasibility and outcomes

Trimetazidine, a metabolic modulator, has cardiac and extracardiac benefits in idiopathic dilated cardiomyopathy

Upper Airway Collapsibility during Dexmedetomidine and Propofol Sedation in Healthy Volunteers: A Nonblinded Randomized Crossover Study

Validation of [(11) C]ORM-13070 as a PET tracer for alpha2c -adrenoceptors in the human brain