5-HT1D binding sites in various species: similar pharmacological profile in dog, monkey, calf, guinea-pig and human brain membranes.
Radioligand binding studies were performed in membranes of calf caudate, guinea-pig cortex, dog caudate and whole brain, monkey caudate and whole brain, and human caudate using the novel iodinated radioligand, Serotonin-5-O-Carboxymethyl-Glycyl[125I] Tyrosinamide (abbreviated [125I]GTI for the sake of simplicity), a ligand known to label 5-HT1B and 5-HT1D sites. In all membrane preparations tested, [125I]GTI labelled high affinity sites with the following rank order of affinity: 5-carboxamidotryptamine greater than 5-HT = DHE = ergotamine greater than or equal to sumatriptan greater than or equal to metergoline = CGS 12066 greater than or equal to yohimbine = methysergide greater than or equal to methiothepin greater than 8-OH-DPAT greater than or equal to mianserin greater than or equal to CP 93129 greater than or equal to (-)pindolol = ketanserin greater than or equal to isamoltane = mesulergine greater than or equal to corynanthine = spiperone greater than MDL 72222. The affinity profiles were very similar in the membranes of the different species, especially in dog, monkey and human brain. The pharmacological profile of [125I]GTI binding (determined with up to 25 different drugs) was fully comparable to the binding profile reported previously in human substantia nigra (using [125I]GTI) or in a variety of brain preparations known to contain 5-HT1D sites using [3H]5-HT as a radioligand.(ABSTRACT TRUNCATED AT 250 WORDS)
Bruinvels
A T
AT
Preclinical Research, Sandoz Pharma Ltd, Basel, Switzerland.
Lery
H
H
Nozulak
J
J
Palacios
J M
JM
Hoyer
D
D
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002417:Cattle; D004151:Dipeptides / Q000494:pharmacology; D004285:Dogs; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D008024:Ligands; D008253:Macaca mulatta; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012701:Serotonin / Q000031:analogs & derivatives / Q000494:pharmacology; D013045:Species Specificity; D013378:Substantia Nigra / Q000187:drug effects / Q000378:metabolism
D004151:Dipeptides; D008024:Ligands; D011985:Receptors, Serotonin; C072128:serotonin-O-carboxymethyl-Gly-Tyr; D012701:Serotonin