Spiperones

Correlation between clinical effectiveness and receptor affinities, however, can be seen with other receptors in addition to the dopamine D2 receptor. These include other dopaminergic receptors, as well as noradrenergic and serotonergic receptors. For example, most antipsychotics also have high affinity for a -adrenoceptors and 5-HT2 receptors (225). Some antipsychotics have been shown to be selective for the adrenoceptor versus the a -adrenoceptor, for example, spiperone [749-02-0] (226) and risperidone (61) (221]... 

Ch oro -p-fluorobutyrophenone Benperidol D roper idol Melitracen Pipamperone Spiperone... 

Fluoro uracil mercury Tegafur Formaldehyde Biperiden Bronopol Cortivazol Edetate disodium Glaziovine Hexetidine Meptazinol Metampicillin sodium Methylol riboflavin Nifurfoline Nifurtoinol Noxytiolin Oxymetazoline HCI Phenindamine tartrate Pipebuzone Thihexinol Timonacic sodium Triclobisonium chloride T romethamine Tyloxapol Formamide Cimetide Primidone Protriptyline Razo xane Spiperone Formic acid Bupivacaine... 

C H oClFO 3874-54-2) see Benperidol Bromperidol Droperidol Fluanisone Haloperidol Melperone Moperone Pipamperone Primaperone Spiperone Timiperone Trifluperidol... 

Ci4Hii,N20 14578-20-2) see Azatadine 4-oxo-l-phenyl-1,3<8-triazaspiro[4.5]decane (C13H17N3O 1021-25-6) see Fluspirilene Spiperone (25,6R)-S-oxo-6-phthalimido-2-(2-thienyl)perhydro-l,4-thiazepinc... 

The biplots show which binding tests are predictive for which pharmacological tests. Binding to the haloperidol and apomorphine labeled receptors corresponds with inhibition of agitation and stereotypy in rats, binding to the spiperone receptor... 

The selective blockade of 5-HT, receptors by 300 nM 5-HT reduces the number of 3H-LSD binding sites to the Bmax of 5-HT2 receptors and, conversely, the occupancy of 5-HT2 receptors by 30 nM of spiperone allows the binding of 3H-LSD to sites qualitatively and quantitatively similar to the 5-HT, receptors (87). Because of this specific interaction of LSD with 5-HT receptors, the hallucinogen can be used as a probe for in vitro studies on such receptors in various... 

H]spiperone binding test) and in vivo (catalepsy induction, and antagonism of apomorphine-induced stereotypy in rats antagonism of apomorphine-induced emesis in dogs). On the other hand, antagonism of cisplatin-induced emesis in the dog and ferret was retained. Several representative /J-keto, ji-hydroxy and / -methoxy analogues are shown in Table 7.1. 

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