Cannabaceae

Tavapadon
Clinical data
Other namesCVL-751; PF-6649751; PF-06649751
Identifiers
  • (−)-(6Ξ)-1,5-dimethyl-6-(2-methyl-4-[(3-[trifluoromethyl]pyridin-2-yl)oxy]phenyl)pyrimidine-2,4(1H,3H)-dione
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H16F3N3O3
Molar mass391.350 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC(=C1)OC2=C(C=CC=N2)C(F)(F)F)C3=C(C(=O)NC(=O)N3C)C
  • InChI=1S/C19H16F3N3O3/c1-10-9-12(28-17-14(19(20,21)22)5-4-8-23-17)6-7-13(10)15-11(2)16(26)24-18(27)25(15)3/h4-9H,1-3H3,(H,24,26,27)
  • Key:AKQXQLUNFKDZBN-UHFFFAOYSA-N

Tavapadon (developmental code names CVL-751, PF-06649751) is a dopamine receptor agonist for the treatment of Parkinson's disease.[1][2][3], under development by Cerevel Therapeutics who acquired Tavapadon from Pfizer in 2018. It acts as a selective partial agonist of the dopamine D1 (Ki = 8.54 nM) and D5 receptors.[2][3] It also shows biased agonism for Gs-coupled signaling.[2] As of July 2021, tavapadon is in phase 3 clinical trials for Parkinson's disease.[1]

See also[edit]

References[edit]

  1. ^ a b "Tavapadon - Cerevel Therapeutics". Adis Insight. Springer Nature Switzerland AG.
  2. ^ a b c Cerri S, Blandini F (December 2020). "An update on the use of non-ergot dopamine agonists for the treatment of Parkinson's disease". Expert Opinion on Pharmacotherapy. 21 (18): 2279–2291. doi:10.1080/14656566.2020.1805432. PMID 32804544. S2CID 221163451.
  3. ^ a b Hall A, Provins L, Valade A (January 2019). "Novel Strategies To Activate the Dopamine D1 Receptor: Recent Advances in Orthosteric Agonism and Positive Allosteric Modulation". Journal of Medicinal Chemistry. 62 (1): 128–140. doi:10.1021/acs.jmedchem.8b01767. PMID 30525590. S2CID 54469910.

One thought on “Cannabaceae

  1. Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
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