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At least 109 records · Page 6Linked to original sources
PubMed1989

Structure of a kappa-opioid receptor misfit: (1S,5R,8R,9R)-2'-hydroxy-5,9-dimethyl-8,2-epoxyethano-6,7-benzomorphan hydrochloride.

C16H22NO+2.Cl-, Mr = 295.808, monoclinic, P2(1), a = 11.967 (1), b = 12.529 (1), c = 9.9369 (9) A, beta = 93.00 (1) degrees, V = 1487.8 (2) A3, Z = 4, Dm = 1.32 (2), Dx = 1.321 Mg m-3, lambda(Cu K alpha) = 1.54178 A, mu(Cu K alpha) = 2.289 mm-1, F(000) = 632, T = 291 K, final R = 0.040 for 2448 observed reflections. The two molecules present in the asymmetric unit are linked by an extensive network of hydrogen bonds, including several of the less common (C-)H...O and (C-)-H...Cl types. This interpretation is substantiated by a Mulliken population analysis resulting from CNDO/2 calculations. The major effect of the presence of the epoxyethano bridge is a marked flattening about the N atom of the piperidinium ring. Whether this is sufficient to explain the inactivity of the compound at the opioid kappa receptor is not clear.

Benzomorphans↗
PubMed1988

Selective protection of benzomorphan binding sites against inactivation by N-ethylmaleimide. Evidence for kappa-opioid receptors in frog brain.

Selective binding of [3H]bremazocine and [3H]-ethylketocyclazocine to kappa-opioid receptor sites in frog (Rana esculenta) brain membranes is irreversibly inactivated by the sulfhydryl group alkylating agent N-ethylmaleimide (NEM). Pretreatment of the membranes with kappa-selective compounds [ethylketocyclazocine (EKC), dynorphin (1-13), or U-50,488H] but not with [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DAGO; mu specific ligand) or [D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin (DADLE; delta specific ligand) strongly protects the binding of the radioligands against NEM inactivation. These results provide more evidence for the existence of kappa-opioid receptors in frog brain. The relatively high concentrations of NEM that are needed to decrease the specific binding of [3H]bremazocine together with the observation of an almost complete protection of its binding sites by NaCl suggest that bremazocine may act as an opioid antagonist in frog brain.

Animals↗
PubMed1983

Ontogeny of benzomorphan-selective (kappa) sites: a computerized analysis.

In an investigation of the postnatal development of kappa opiate receptors, the affinity and capacity of 0.5 nM [3H]-ethylketocyclazocine (EKC) binding in crude rat brain homogenates was measured by displacement with unlabeled EKC, morphine, or D-ala2-D-leu5-enkephalin (DADL). Displacement curves were analyzed using a weighted, non-linear regression, curve fitting computer program. At all stages of development, [3H]-EKC binding fit a two site model significantly better than a one site model. Affinities of EKC, morphine, or DADL for the high affinity [3H]-EKC binding site did not change during the postnatal period. The density of the high affinity [3H]-EKC binding site increased linearly with age, whereas the levels of the low affinity site rose more rapidly during the second week.

Aging↗