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Pergolide
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===Pharmacodynamics=== Pergolide acts as an agonist of [[dopamine receptor|dopamine]] [[Dopamine receptor D2|D<sub>2</sub>]] and [[Dopamine receptor D1|D<sub>1</sub>]] and [[serotonin receptor|serotonin]] [[5-HT1A|5-HT<sub>1A</sub>]], [[5-HT1B|5-HT<sub>1B</sub>]], [[5-HT2A|5-HT<sub>2A</sub>]], [[5-HT2B|5-HT<sub>2B</sub>]], and [[5-HT2C|5-HT<sub>2C</sub>]] [[receptor (biochemistry)|receptor]]s. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline. Although pergolide is more potent as an agonist of the D<sub>2</sub> receptor, it has high D<sub>1</sub> receptor [[affinity (pharmacology)|affinity]] and is one of the most potent D<sub>1</sub> receptor agonists of the [[dopamine receptor agonist]]s that are clinically available.<ref name="McClureHarvey2010">{{cite journal | vauthors = McClure MM, Harvey PD, Goodman M, Triebwasser J, New A, Koenigsberg HW, Sprung LJ, Flory JD, Siever LJ | display-authors = 6 | title = Pergolide treatment of cognitive deficits associated with schizotypal personality disorder: continued evidence of the importance of the dopamine system in the schizophrenia spectrum | journal = Neuropsychopharmacology | volume = 35 | issue = 6 | pages = 1356–1362 | date = May 2010 | pmid = 20130535 | pmc = 3055340 | doi = 10.1038/npp.2010.5 }}</ref> The agonist activity of pergolide at the D<sub>1</sub> receptor somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease. Pergolide has been said to be [[hallucinogenic]] due to activation of 5-HT<sub>2A</sub> receptors.<ref name="pmid19925619">{{cite journal | vauthors = Gillman PK | title = Triptans, serotonin agonists, and serotonin syndrome (serotonin toxicity): a review | journal = Headache | volume = 50 | issue = 2 | pages = 264–272 | date = February 2010 | pmid = 19925619 | doi = 10.1111/j.1526-4610.2009.01575.x | s2cid = 221752556 | doi-access = free }}</ref><ref name="pmid18703043">{{cite journal | vauthors = Cussac D, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Martel JC, Danty N, Rauly-Lestienne I | title = Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells | journal = European Journal of Pharmacology | volume = 594 | issue = 1–3 | pages = 32–38 | date = October 2008 | pmid = 18703043 | doi = 10.1016/j.ejphar.2008.07.040 }}</ref> However, other sources have stated that the drug is non-hallucinogenic.<ref name="GumpperRoth2024">{{cite journal | vauthors = Gumpper RH, Roth BL | title = Psychedelics: preclinical insights provide directions for future research | journal = Neuropsychopharmacology | volume = 49 | issue = 1 | pages = 119–127 | date = January 2024 | pmid = 36932180 | doi = 10.1038/s41386-023-01567-7 | url = | pmc = 10700551 }}</ref> It has been associated with [[cardiac valvulopathy]] due to activation of 5-HT<sub>2B</sub> receptors.<ref name="pmid24361689">{{cite journal | vauthors = Cavero I, Guillon JM | title = Safety Pharmacology assessment of drugs with biased 5-HT(2B) receptor agonism mediating cardiac valvulopathy | journal = Journal of Pharmacological and Toxicological Methods | volume = 69 | issue = 2 | pages = 150–161 | date = 2014 | pmid = 24361689 | doi = 10.1016/j.vascn.2013.12.004 }}</ref> {| class="wikitable" |+ {{Nowrap|Activities of pergolide at various sites<ref name="pmid12388666">{{cite journal | vauthors = Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A | title = Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 303 | issue = 2 | pages = 791–804 | date = November 2002 | pmid = 12388666 | doi = 10.1124/jpet.102.039867 | s2cid = 6200455 }}</ref><ref name="pmid12388667">{{cite journal | vauthors = Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ | title = Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 303 | issue = 2 | pages = 805–814 | date = November 2002 | pmid = 12388667 | doi = 10.1124/jpet.102.039875 | s2cid = 35238120 }}</ref><ref name="pmid12388668">{{cite journal | vauthors = Newman-Tancredi A, Cussac D, Quentric Y, Touzard M, Verrièle L, Carpentier N, Millan MJ | title = Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 303 | issue = 2 | pages = 815–822 | date = November 2002 | pmid = 12388668 | doi = 10.1124/jpet.102.039883 | s2cid = 19260572 }}</ref><ref name="PDSPKiDatabase">{{cite web |url=https://pdsp.unc.edu/databases/pdsp.php?testFreeRadio=testFreeRadio&testLigand=Pergolide&doQuery=Submit+Query |title=PDSP Database - UNC |website=pdsp.unc.edu |access-date=15 January 2022 |archive-url=https://web.archive.org/web/20210413033753/https://pdsp.unc.edu/databases/pdsp.php?testFreeRadio=testFreeRadio&testLigand=Pergolide&doQuery=Submit+Query |archive-date=13 April 2021 |url-status=dead}}</ref>}} ! Site ! Affinity (K<sub>i</sub> [nM]) ! Efficacy (E<sub>max</sub> [%]) ! Action |- | [[D1 receptor|D<sub>1</sub>]] | 339 | ? | ? |- | [[D2S receptor|D<sub>2S</sub>]] | 32 | 112 | Full agonist |- | [[D2L receptor|D<sub>2L</sub>]] | 26 | 52 | Partial agonist |- | [[D3 receptor|D<sub>3</sub>]] | 5.5 | 71 | Partial agonist |- | [[D4 receptor|D<sub>4</sub>]] | 59 | 56 | Partial agonist |- | [[D5 receptor|D<sub>5</sub>]] | 33 | ? | ? |- | [[5-HT1A receptor|5-HT<sub>1A</sub>]] | 1.9 | 63 | Partial agonist |- | [[5-HT1B receptor|5-HT<sub>1B</sub>]] | 282 | 90 | Partial agonist |- | [[5-HT1D receptor|5-HT<sub>1D</sub>]] | 13 | 86 | Partial agonist |- | [[5-HT2A receptor|5-HT<sub>2A</sub>]] | 8.3 | 103 | Full agonist |- | [[5-HT2B receptor|5-HT<sub>2B</sub>]] | 7.1 | 113 | Full agonist |- | [[5-HT2C receptor|5-HT<sub>2C</sub>]] | 295 | 87 | Partial agonist |- | [[5-HT6 receptor|5-HT<sub>6</sub>]] | 30 | ? | ? |- | [[5-HT7 receptor|5-HT<sub>7</sub>]] | 1.0–18 | ? | ? |- | [[α1A-Adrenergic receptor|α<sub>1A</sub>]] | 1,047 | ? | ? |- | [[α1B-Adrenergic receptor|α<sub>1B</sub>]] | 692 | ? | ? |- | [[α1D-Adrenergic receptor|α<sub>1D</sub>]] | 295 | ? | ? |- | [[α2A-Adrenergic receptor|α<sub>2A</sub>]] | 50 | 31 | Partial agonist |- | [[α2B-Adrenergic receptor|α<sub>2B</sub>]] | 32 | 70 | Partial agonist |- | [[α2C-Adrenergic receptor|α<sub>2C</sub>]] | 68 | 16 | Partial agonist |- | [[α2D-Adrenergic receptor|α<sub>2D</sub>]] | 692 | ? | ? |- | [[β1-Adrenergic receptor|β<sub>1</sub>]] | >10,000 | – | – |- | [[β2-Adrenergic receptor|β<sub>2</sub>]] | >10,000 | – | – |- | [[H1 receptor|H<sub>1</sub>]] | 1,698 | ? | ? |- | [[Muscarinic acetylcholine receptor M1|M<sub>1</sub>]] | >10,000 | – | – |- | [[Sigma-1 receptor|σ<sub>1</sub>]] | >10,000 | – | – |- | [[Sigma-2 receptor|σ<sub>2</sub>]] | 923 | ? | ? |- class="sortbottom" | colspan="4" style="width: 1px; background-color:#eaecf0; text-align: center;" | '''Notes:''' All receptors are human except α<sub>2D</sub>-adrenergic, which is rat (no human counterpart), and 5-HT<sub>6</sub>, 5-HT<sub>7</sub>, σ<sub>1</sub>, and σ<sub>2</sub>, which are all rodent (rat or guinea pig).<ref name="pmid12388666" /><ref name="PDSPKiDatabase" /> |}
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