ライフサイエンスコーパス: morphinan

1 ties compared to the univalent 2-substituted morphinans.

2 an ester moiety as the spacer in the dimeric morphinans.

3 ng and completes the pentacyclic core of the morphinans.

4 ve as an efficient route to access the other morphinans.

5 ved STORR but does not produce promorphinans/morphinans.

6 say, ligands 13, 17, and 19 and their parent morphinans 1 and 2 stimulated [(35)S]GTPgammaS binding m

7 and chemical characterization of a series of morphinans 3a-c, structural analogues of cyclorphan [(-)

8 al structure of the murine muOR bound to the morphinan agonist BU72 and a G protein mimetic camelid a

9 peptide antagonist (Dmt-Tic) and a mu/kappa morphinan agonist butorphan (MCL 101) through a two meth

10 olic group of the potent mu and kappa opioid morphinan agonist/antagonists cyclorphan and butorphan w

11 Morphinan alkaloids from the opium poppy are used for pa

12 y enhanced the conversion of salutaridine to morphinan alkaloids.

13 gy is applied to a formal total synthesis of morphinan alkaloids.

14 f uOR agonists, including partial and biased morphinan and fentanyl analogues.

15 or molecular modeling of interaction between morphinans and the mu receptor.

16 5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolo morphinans), and the effect of the N-substituent on opio

17 sis of THIQ, aporphine, tetrahydroberberine, morphinan, and androcymbine natural products.

18 ural plant hosts, including protoberberines, morphinans, and phthalideisoquinolines.

19 use micro-OR in complex with an irreversible morphinan antagonist.

20 covered a unique combination of BPRMU191 and morphinan antagonists that produced potent antinocicepti

21 a 3-phenylpropoxy at the 14-position of the morphinan as a mixed mu opioid receptor (MOR) agonist an

22 ed enantiomeric analogues of traditional (-)-morphinans as having TLR9 antagonist properties on repor

23 The identification of a morphinan-based novel small-molecule structure with TLR9

24 A series of aminothiazole-derived morphinans, benzomorphans, and morphine were synthesized

25 The direction of metabolites to morphinan biosynthesis requires isomerization of (S)- to

26 Bivalent morphinan compounds containing ester linkers were synthe

27 ovel series of kappa agonists related to the morphinan (-)-cyclorphan (3a) and the benzomorphan (-)-c

28 he results of the present study suggest that morphinan derivatives related to 16 and 14 may provide u

29 nt kappa-OR-selective ligands, including the morphinan-derived antagonists norbinaltorphimine and 5'-

30 tions were investigated at the 3-OH group of morphinans: levorphanol (2a), cyclorphan (2b), and MCL-1

31 tein-coupled receptors published so far, the morphinan ligand binds deeply within a large solvent-exp

32 potent opioid agonist activity (N-pentyl) in morphinan-like ligands which interact with the mu-recept

33 presentative aminothiazolomorphinan with the morphinan mixed-KOR/MOR agonist butorphan (MCL-101) on b

34 t a hydroxyl group at the 14-position of the morphinan moiety displayed agonist activity at the micro

35 alpha-epoxy-6beta-[(4'-pyridyl) carboxamido] morphinan (NAP), a peripherally acting MOR-selective ant

36 on to the salt-bridge binding mode common to morphinan opiates, fentanyl can move deeper and form a s

37 ry potency among structurally highly similar morphinan opioids (IC(50) ranged from 6.4 muM for dextro

38 The C(3)-substituent in morphinan opioids is of critical importance; the 3-OH gr

39 inter alia on the 3-OMe and 14-OMe motifs in morphinan opioids, is suggested with the aid of DFT calc

40 Ligand 12, a compound containing only one morphinan pharmacophore and a long-chain ester group, ha

41 which were formed by coupling two identical morphinan pharmacophores (cyclorphan (1) or MCL 101 (2))

42 osition and ligands 8 and 9 in which the two morphinan pharmacophores were coupled by ether moieties

43 ion protein STORR may enable microbial-based morphinan production.

44 hexadienone that generates three of the four morphinan ring junction stereocenters in one step.

45 The ether linkage of C4-C5 in the morphinan ring leads to a strong reduction of inhibitory

46 ubsets of residues, despite sharing a common morphinan scaffold.

47 Although most of the 2-substituted morphinans showed considerably lower affinities compared

48 Position 6 of the morphinan skeleton plays a key role in the mu-opioid rec

49 with the aminothiazole on the C-ring of the morphinan skeleton.

50 of the address moiety with the C ring of the morphinan structure enhances delta antagonist potency an

51 ential for the evolution of the promorphinan/morphinan subclass of benzylisoquinoline alkaloids (BIAs

52 synthesis of more than just the promorphinan/morphinan subclass of BIAs in the Papaveraceae.

53 oxamido replacement (compounds 46-48) in the morphinan subseries resulted in similar affinities compa

54 t appropriate molecular manipulations of the morphinan templates could provide ligands with mixed mic

55 A novel series of morphinans were synthesized, and their binding affinity

56 ese dimeric ligands can be viewed as dimeric morphinans, which were formed by coupling two identical

57 STORR gene fusion also contain promorphinans/morphinans with one important exception.