- Muscarinic acetylcholine receptor binding affinities of pethidine analogs
-
A series of pethidine analogs were synthesized and their affinities for the [3H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M1, M3 or M5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M1, M3 and M5 mAChRs (Ki = 0.67, 0.37, and 0.38 μM, respectively).
- Lee, Na-Ra,Zhang, Xuan,Darna, Mahesh,Dwoskin, Linda P.,Zheng, Guangrong
-
p. 5032 - 5035
(2015/11/09)
-
- NAPHTHYL ETHER COMPOUNDS AND THEIR USE
-
Compounds having the following structure wherein R1, R2, R3, R4, R5, R6, R7 m and n are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically-acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same.
- -
-
-
- 4-phenylpiperidine compounds and their use
-
Piperidine compounds having the formula STR1 wherein R1 is hydrogen, (C1-6 -alkoxyaryl)alkyl, diphenylmethozy-C1-6 -alkyl, C1-8 -alkyl, C4-10 -cycloalkylalkyl, phenoxy-C1-8 -alkyl, or C1-6 -alkoxy-C1-6 -alkyl; and R is STR2 or CH=NOR' wherein R' is C1-6 -alkyl, C3-7 -cycloalkyl, C1-6 -alkoxy-C1-6 -alkyl, aryl-C0-6 -alkyl, which may optionally be substituted with one or more halogen and (1-5 -alkoxy, thienyl, or C4-7 -cycloalkylalkyl. The novel compounds are useful for the treatment of pain conditions and as neuroleptics.
- -
-
-