Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

NESS-0327

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
NESS-0327
Identifiers
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC24H23Cl3N4O
Molar mass489.83 g·mol−1
3D model (JSmol)
  • Clc3cc(Cl)ccc3-n4c2-c1ccc(Cl)cc1CCCc2c(n4)C(=O)NN5CCCCC5
  • InChI=1S/C24H23Cl3N4O/c25-16-7-9-18-15(13-16)5-4-6-19-22(24(32)29-30-11-2-1-3-12-30)28-31(23(18)19)21-10-8-17(26)14-20(21)27/h7-10,13-14H,1-6,11-12H2,(H,29,32) ☒N
  • Key:NCXBPZJQQSNIRA-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

NESS-0327 is a drug used in scientific research which acts as an extremely potent and selectiveantagonist of thecannabinoid receptorCB1. It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligandrimonabant, with aKi at CB1 of 350fM (i.e. 0.00035nM) and a selectivity of over 60,000x for CB1 over CB2.[1]Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM[2] and18.4nM[3]).Also unlike rimonabant, NESS-0327 does not appear to act as aninverse agonist at higher doses, instead being a purelyneutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own.[4]

See also

[edit]

References

[edit]
  1. ^Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, Tambaro S, et al. (July 2003). "Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor".The Journal of Pharmacology and Experimental Therapeutics.306 (1):363–70.doi:10.1124/jpet.103.049924.hdl:11380/1212092.PMID 12663689.S2CID 32018707.
  2. ^Stoit AR, Lange JH, Hartog AP, Ronken E, Tipker K, Stuivenberg HH, et al. (August 2002)."Design, synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists".Chemical & Pharmaceutical Bulletin.50 (8):1109–13.doi:10.1248/cpb.50.1109.PMID 12192147.
  3. ^Zhang Y, Burgess JP, Brackeen M, Gilliam A, Mascarella SW, Page K, et al. (June 2008). "Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations".Journal of Medicinal Chemistry.51 (12):3526–39.doi:10.1021/jm8000778.PMID 18512901.
  4. ^Tambaro S, Mongeau R, Dessi C, Pani L, Ruiu S (November 2005). "Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors".European Journal of Pharmacology.525 (1–3):150–3.doi:10.1016/j.ejphar.2005.09.058.hdl:11380/1212113.PMID 16271359.
Phytocannabinoids
(comparison)
Cannabibutols
Cannabichromenes
Cannabicyclols
Cannabidiols
Cannabielsoins
Cannabigerols
Cannabiphorols
Cannabinols
Cannabitriols
Cannabivarins
Delta-3-tetrahydrocannabinols
Delta-4-tetrahydrocannabinols
Delta-7-tetrahydrocannabinols
Delta-8-tetrahydrocannabinols
Delta-9-tetrahydrocannabinols
Delta-10-Tetrahydrocannabinols
Delta-11-Tetrahydrocannabinols
Miscellaneous cannabinoids
Active metabolites
Endocannabinoids
Synthetic
cannabinoid
receptor
agonists /
neocannabinoids
Classical cannabinoids
(dibenzopyrans)
Non-classical
cannabinoids
Adamantoylindoles
Benzimidazoles
Benzoylindoles
Cyclohexylphenols
Eicosanoids
Indazole-3-
carboxamides
Indole-3-carboxamides
Indole-3-carboxylates
Naphthoylindazoles
Naphthoylindoles
Naphthoylpyrroles
Naphthylmethylindenes
Naphthylmethylindoles
Phenylacetylindoles
Pyrazolecarboxamides
Tetramethylcyclo-
propanoylindazoles
Tetramethylcyclo-
propanoylindoles
Others
AllostericCBRTooltip Cannabinoid receptorligands
Endocannabinoid
enhancers

(inactivation inhibitors)
Anticannabinoids
(antagonists/inverse
agonists/antibodies)


Stub icon

Thiscannabinoid related article is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=NESS-0327&oldid=1294740070"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp