Dopamine Dopamine Serotonin Lisuride

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FMI 14 - Modes of action of Valentonin and of 6–methoxy-harmalan FMI 14 - Modes of action of Valentonin and of 6–methoxy-harmalan Clonidine and its analogues (antihypertensive α2 adrenergic receptor agonists 3. Action on dopaminergic D1 and D2 receptors Dopaminergic agonists — such as ergoline derivatives (Lisuride, Bromocriptine, which cause drowsiness) are valentonergics (see figure 8). etc.) and Quinagolide — used in the treatment of Parkinson’s disease are valentonergics HO (see figure 9). HO HO Noradrenalin Serotonin H H N Dopamine N N H Dopamine H H H N H H HO HO N H HO H OH H HO N H N H3C N OMe HO N Cl N C N H H C Guanoxabenz C HO N O N N N N Moxonidine H N N Serotonin CH OH H Cl H H H 3 Lisuride H3C O N H N CH H C 3 Cl O N N O H O C Clonidine Cl C N C H N Rilmenidine O CH O N H 3 N H C Cl N C H C N N H N 3 O H CO H CH 3 H N 3 H H H H Metergoline Cl O C N H N Bromocriptine CH3 N H Valentonin N O H Guanfacine N C H N Br CH O H CH2 3 Cl H N N C N d d CH O C 3 H C H3CO 3 CH2 Valentonin N : Allosteric ligand N H CH3 N H H3CO CH3 Figure 8: The chemical structures of Valentonin and noradrenergic agonists like Clonidine and its analogues α2 6-methoxy-harmalan N Lysergide (LSD) have common structural elements essential to the activation, via allosteric modulation, of noradrenergic α2 receptors H N (lower BP and HR) and serotonergic 5-HT receptors (hypnotic activity). 2C d H d Valentonin’s pharmacological actions provide an explanation not only of the here- : Allosteric ligand tofore unexplained action of Clonidine and its analogues on sympathetic tonus (lower BP and HR) used in the treatment of hypertension (noradrenergic agonist with CNS α2 Figure 9: The presence in Lisuride, Metergoline and Bromocriptine molecules of an allosteric ligand - a carbonyl C=O action) but also the drowsiness side effects of this class of medications (serotonergic group - explains why these antiparkinsonian and antiprolactin medications can activate, like VLT, dopaminergic D1/D2 5–HT2C receptors, even though the substituents on their tertiary amine (N) functional groups are too large. Of further note is that Lysergide (LSD), whose lysergic acid carbonyl (C=O) group has an unfavorable position and orientation for allosteric receptor agonists). modulation, cannot activate dopaminergic receptors, but rather blocks them. 10 8 10 9.

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Product List March 2019 - Page 1 of 53
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Selective Labeling of Serotonin Receptors Byd-[3H]Lysergic Acid
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Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
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Gianluca BW.Indd
Use and safety of psychotropic drugs in elderly patients Gianluca Trifi rò GGianlucaianluca BBW.inddW.indd 1 225-May-095-May-09 111:22:461:22:46 AAMM Th e work presented in this thesis was conducted both at the Department of Medical Informatics of the Erasmus Medical Center, Rotterdam, Th e Netherlands and the Depart- ment of Clinical and Experimental Medicine and Pharmacology of University of Messina, Messina, Italy. Th e studies reported in chapter 2.2 and 4.3 were respectively supported by grants from the Italian Drug Agency and Pfi zer. Th e contributions of the general practitioners participating in the IPCI, Health Search/ Th ales, and Arianna databases are greatly acknowledged. Financial support for printing and distribution of this thesis was kindly provided by IPCI, SIMG/Health Search, Eli Lilly Nederland BV, Boehringer-Ingelheim B.V., Novartis Pharma B.V. and University of Messina. Cover design by Emanuela Punzo, Antonio Franco e Gianluca Trifi rò. Th e background photo in the cover is a landscape from Santa Lucia del Mela (Sicily) and was kindly pro- vided by Franco Trifi rò. Th e photo of the elderly person is from Antonio Franco Trifi rò. Layout and print by Optima Grafi sche Communicatie, Rotterdam, Th e Netherlands. GGianlucaianluca BBW.inddW.indd 2 225-May-095-May-09 111:22:481:22:48 AAMM Use and Safety of Psychotropic Drugs in Elderly Patients Gebruik en veiligheid van psychotropische medicaties in de oudere patienten Proefschrift ter verkrijging van de graad van doctor aan de Erasmus Universiteit Rotterdam op gezag van de rector magnifi cus Prof.dr.
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