Opioid and nonopioid components independently contribute to the mechanism of action of tramadol, an'atypical'opioid analgesic.

RB Raffa, E Friderichs, W Reimann, RP Shank… - … of Pharmacology and …, 1992 - ASPET
Tramadol hydrochloride produced dose-related antinociception in mouse abdominal
constriction [ED50= 1.9 (1.2-2.6) mg/kg ip], hot-plate [48 degrees C, ED50= 21.4 (18.4-25.3)
mg/kg sc; 55 degrees C, ED50= 33.1 (28.2-39.1) mg/kg sc] and tail-flick [ED50= 22.8 (19.2 …

Complementary and synergistic antinociceptive interaction between the enantiomers of tramadol.

RB Raffa, E Friderichs, W Reimann, RP Shank… - … of Pharmacology and …, 1993 - ASPET
The explanation for the co-existence of opioid and nonopioid components of tramadol-
induced antinociception appears to be related to the different, but complementary and
interactive, pharmacologies of its enantiomers. The (+) enantiomer had Ki values of only …

Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception.

EE Codd, RP Shank, JJ Schupsky, RB Raffa - Journal of Pharmacology and …, 1995 - ASPET
Although it is well established that the analgesic effects of morphine are mediated by opioid
receptors, previous studies have shown that some opioids additionally inhibit the uptake of
serotonin and norepinephrine. The present investigation of a diverse group of opioids …

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl) piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl) amide, a high affinity TRPV1 (VR1 …

DM Swanson, AE Dubin, C Shah… - Journal of medicinal …, 2005 - ACS Publications
High throughput screening using the recombinant human TRPV1 receptor was used to
identify a series of pyridinylpiperazine ureas (3) as TRPV1 vanilloid receptor ligands.
Exploration of the structure− activity relationships by parallel synthesis identified the …

Molecular cloning and characterization of the human voltage-gated calcium channel α2δ-4 subunit

N Qin, S Yagel, ML Momplaisir, EE Codd… - Molecular …, 2002 - ASPET
The voltage-gated calcium channel is composed of a pore-forming α 1 subunit and several
regulatory subunits: α 2 δ, β, and γ. We report here the identification of a novel α 2 δ subunit,
α 2 δ-4, from the expressed sequence tag database followed by its cloning and …

Binding of a growth hormone releasing hexapeptide to specific hypothalamic and pituitary binding sites

EE Codd, AYL Shu, RF Walker - Neuropharmacology, 1989 - Elsevier
Abstract The drug SK&F 110679 (His-d-Trp-Ala-Trp-d-Phe-LysNH 2), is an enkephalin-
derived hexapeptide, which specifically releases growth hormone in a wide variety of
species in vivo and in vitro. Previous binding studies, using ligands which are specific for mu …

Molecular cloning and functional expression of the human sodium channel β1B subunit, a novel splicing variant of the β1 subunit

N Qin, MR D'andrea, ML Lubin… - European journal of …, 2003 - Wiley Online Library
The voltage gated sodium channel comprises a pore‐forming α subunit and regulatory β
subunits. We report here the identification and characterization of a novel splicing variant of
the human β1 subunit, termed β1B. The 807 bp open reading frame of the human β1Β …

Oral activity of the growth hormone releasing peptide His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 in rats, dogs and monkeys

RF Walker, EE Codd, FC Barone, AH Nelson… - Life sciences, 1990 - Elsevier
The purpose of this study was to evaluate the growth hormone (GH) releasing activity of
orally administered His-D-Trp-Ala-D-Phe-Lys-NH 2 (GHRP-6, SK&F 110679) in rats, dogs
and monkeys. Rats were administered GHRP-6 orally by gavage or parenterally through …

Gas chromatographic method using nitrogen–phosphorus detection for the measurement of tramadol and its O-desmethyl metabolite in plasma and brain tissue of …

Q Tao, DJ Stone Jr, MR Borenstein, V Jean-Bart… - … of Chromatography B …, 2001 - Elsevier
A method that allows the measurement of plasma and brain levels of the centrally-acting
analgesic tramadol and its major metabolite (O-desmethyl tramadol) in mice and rats was
developed using gas chromatography equipped with nitrogen–phosphorus detection (GC …

Composition comprising a tramadol material and an anticonvulsant drug

EE Codd, RP Martinez, KE Rogers - US Patent 6,562,865, 2003 - Google Patents
This invention relates to a pharmaceutical composition comprising a combination of a
tramadol material and an anticonvulsant drug and to the pharmacological use of the
composition in treating conditions of pain and neurologic or psychiatric disorders. The …