title: 1,3-Dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor.
abstract: A series of 1,3-dihydro-2,1,3-benzothiadiazol-2,2-diones (I) and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones (II) were prepared. While the five-member ring series (I) did not show good affinity for opioid receptors, the six-member ring series (II) exhibited extremely high affinity and selectivity for the NOP receptor and showed full agonist activity, as determined by stimulation of GTPgamma[35S] binding.
authors.affiliation: Discovery Research, Purdue Pharma LP, 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. richard.goehring@pharma.com
authors.forename: R Richard
authors.initials: RR
authors.lastname: Goehring
authors.forename: John F W
authors.initials: JF
authors.lastname: Whitehead
authors.forename: K
authors.initials: K
authors.lastname: Brown
authors.forename: Khondaker
authors.initials: K
authors.lastname: Islam
authors.forename: Xin
authors.initials: X
authors.lastname: Wen
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Zhou
authors.forename: Zhengming
authors.initials: Z
authors.lastname: Chen
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Valenzano
authors.forename: Wendy S
authors.initials: WS
authors.lastname: Miller
authors.forename: Shen
authors.initials: S
authors.lastname: Shan
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Kyle
mesh_terms: D000818:Animals; D006801:Humans; D066298:In Vitro Techniques; D008024:Ligands; D011869:Radioligand Assay; D051381:Rats; D017450:Receptors, Opioid, mu / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D008024:Ligands; D017450:Receptors, Opioid, mu; D013843:Thiazines; D013844:Thiazoles