3- spiperone

Chemicel Name 8- [4-(4-fluorophenyl)-4-oxobutyl] -1-phenyl-1,3,8-triazaspiro[4.5] decan-4-one 

A mixture of 4-carbamoyl-4-N-anilinopiperidine and formamide is heated for 12 hours at 170°C. After cooling, the reaction mixture is divided between 100 parts water and 900 parts chloroform. The organic layer is separated, dried over MgSO, filtered and the filtrate is evaporated. The semisolid residue is stirred in ethyl acetate. The undissolved part is filtered off, washed with ethyl acetate, and dried, yielding 1-oxo-4-phenyl-2,4,8-triazaspiro-(4.5)decane. 

A mixture of 3.2 parts 4-chloro-p-fluoro-butyrophenone, 3.5 parts 1-oxo-4-phenyl-2,4,8-triazaspiro(4,5)decane, 2 parts Na COs hd 0.1 part Kl in 200 parts hexone is refluxed with stirring for 50 hours. The mixture is cooled to room temperature, 200 parts water are added and the layers are separated. The organic layer is dried over 10 parts MgSO,  

Janssen, P.A.J. U.S. Patent 3,155,669 November 3, 1964 assigned to Research Labora-torium Dr. C. Janssen NV, Belgium 

Peters, V.J. U.S. Patent 3,272,706 September 13,1966 assigned to The Upjohn Company Nara,T., Takasawa, S., Okachi, R., Kavyamoto, I., Kumakawa, M., Yamamoto, M. and Sato, S. U.S. Patent 3319,485 June 25,1974 assigned to Abbott Laboratories 

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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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