dormouse (Member) 04-19-00 10:14 No 122819				Fentanyl analogue -hypo	Bookmark
						Author  Topic:   Fentanyl analogue  hypo Member   posted 12-25-1999 10:53 AM           -------------------------------------------------------------------------------- I stumbled on this article: Iwasawa Y. et al: J. Med. Chem. 42/25 (Dec. 16), 1, (1999). It describes opioid antagonists of fentanyl class. But compound 13 seems to be pretty good, unselective agonist binder (low nanomolar binding constants). The compound has alpha(o-chlorophenethyl) on 1-N (instead of beta phenethyl) and 2-benzimidazolone-1-yl instead of N-phenylpropionamide. Does anyone have an idea how this substitution pattern can affect the bioactivity? Did anyone try to put an OH group in meta or ortho-position of the aniline phenyl? Appreciate your input.
		Rhodium (Chief Bee) 09-09-02 06:18 No 354583				ORL-1 receptor agonist	Bookmark
						This seems to be a very special opioid agonist, because it does not bind to any of the ordinary opioid receptors, but instead the ORL-1 receptor. Read the article at ../rhodium/pdf /orl1.agonist.pdf Compound 13 is the agonist, the others are antagonists.
		Cyrax (Hive Bee) 09-09-02 07:44 No 354599				Receptors	Bookmark
						This is a nice review of the different kind of opioid receptors: http://www.tocris.com/opioidreview.htm There are also links to cannabinoid, dopamine, GABA, ... receptors - with a lot of refs.