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Details

Stereochemistry ACHIRAL
Molecular Formula C23H32N2O4
Molecular Weight 399.5119
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0
Stereo Comments Cis/trans ring substitution

SHOW SMILES / InChI
Structure of MK-8278 C-11

SMILES

CN(CCN1CCCCC1)C(=O)[C@H]2CC[C@@]3(CC2)OC(=O)C4=CC(O[11CH3])=CC=C34

InChI

InChIKey=AEWLECDUIOHVBW-YVGPUXTASA-N
InChI=1S/C23H32N2O4/c1-24(14-15-25-12-4-3-5-13-25)21(26)17-8-10-23(11-9-17)20-7-6-18(28-2)16-19(20)22(27)29-23/h6-7,16-17H,3-5,8-15H2,1-2H3/t17-,23-/i2-1

HIDE SMILES / InChI

Molecular Formula C23H32N2O4
Molecular Weight 399.5119
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Approval Year

Substance Class Chemical
Created
by admin
on Sat Dec 16 11:53:12 GMT 2023
Edited
by admin
on Sat Dec 16 11:53:12 GMT 2023
Record UNII
IO4B35679F
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MK-8278 C-11
Common Name English
5'-(METHOXY-11C)-N-METHYL-3'-OXO-N-(2-(1-PIPERIDYL)ETHYL)SPIRO(CYCLOHEXANE-4,1'-ISOBENZOFURAN)-1-CARBOXAMIDE
Systematic Name English
SPIRO(CYCLOHEXANE-1,1'(3'H)-ISOBENZOFURAN)-4-CARBOXAMIDE, 5'-(METHOXY-11C)-N-METHYL-3'-OXO-N-(2-(1-PIPERIDINYL)ETHYL)-, TRANS-
Systematic Name English
TRANS-5'-(METHOXY-11C)-N-METHYL-3'-OXO-N-(2-(1-PIPERIDINYL)ETHYL)SPIRO(CYCLOHEXANE-1,1'(3'H)-ISOBENZOFURAN)-4-CARBOXAMIDE
Systematic Name English
(11C)MK 8278
Code English
Code System Code Type Description
FDA UNII
IO4B35679F
Created by admin on Sat Dec 16 11:53:12 GMT 2023 , Edited by admin on Sat Dec 16 11:53:12 GMT 2023
PRIMARY
CAS
1246765-07-0
Created by admin on Sat Dec 16 11:53:12 GMT 2023 , Edited by admin on Sat Dec 16 11:53:12 GMT 2023
PRIMARY
Related Record Type Details
TARGET->INVERSE AGONIST
Related Record Type Details
ACTIVE MOIETY
RESULTS: The mean effective dose for (11)C-MK-8278 was 5.4 +/- 1.1 .MU.Sv/MBq. Human brain kinetics showed rapid high uptake and fast washout. Binding potential values can be assessed using the pons as a reference region, with a test-retest repeatability of 7%. Drug RO data showed low interindividual variability per dose (mean RO SD, 2.1%), and a targeted 90% RO can be reached for both IAs at clinically feasible doses. CONCLUSION: (11)C-MK-8278 is a useful novel PET radioligand for determination of human cerebral H3 receptor binding and allows highly reproducible in vivo brain occupancy of H3-targeting drugs, hereby enabling the evaluation of novel compounds in early development to select doses and schedules.