MK-8278 C-11

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 Search

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

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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


					D9SCP0G3HF

HISTAMINE H3 RECEPTOR

TARGET->INVERSE AGONIST

Related Record Type Details


					IO4B35679F

MK-8278 C-11

ACTIVE MOIETY

Comments:

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.