Product Name :
Clocapramine (Clocarpramine)
Description:
Clocapramine is an antagonist of the D2, 5-HT2A receptors. Clocapramine has a moderate affinity for D2-receptors in vitro. Clocapramine shows higher affinity for 5-HT2A than for D2-receptors in vitro. Clocapramine shows the lowest potency for D2-occupancy in vivo. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D2 and frontal serotonin-5-HT2 receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT2 versus D2 receptors that fall between these two groups (ED50 of 14.5 mg/kg for D2, 4.9 mg/kg for 5-HT2). . Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. . Sumiyoshi T, et al. Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Neuropsychopharmacology. 1995 Feb;12(1):57-64.
CAS:
47739-98-0
Molecular Weight:
481.07
Formula:
C28H37ClN4O
Chemical Name:
1′-(3-{5-chloro-2-azatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-2-yl}propyl)-[1,4′-bipiperidine]-4′-carboxamide
Smiles :
NC(=O)C1(CCN(CCCN2C3=CC=CC=C3CCC3=CC=C(Cl)C=C23)CC1)N1CCCCC1
InChiKey:
QAZKXHSIKKNOHH-UHFFFAOYSA-N
InChi :
InChI=1S/C28H37ClN4O/c29-24-12-11-23-10-9-22-7-2-3-8-25(22)33(26(23)21-24)18-6-15-31-19-13-28(14-20-31,27(30)34)32-16-4-1-5-17-32/h2-3,7-8,11-12,21H,1,4-6,9-10,13-20H2,(H2,30,34)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Digitonin} site|{Digitonin} Protocol|{Digitonin} Formula|{Digitonin} supplier|{Digitonin} Cancer}
Additional information:
Clocapramine is an antagonist of the D2, 5-HT2A receptors. Clocapramine has a moderate affinity for D2-receptors in vitro.{{Fmoc-Thr(tBu)-OH} MedChemExpress|{Fmoc-Thr(tBu)-OH} {Amino Acid Derivatives}|{Fmoc-Thr(tBu)-OH} Technical Information|{Fmoc-Thr(tBu)-OH} References|{Fmoc-Thr(tBu)-OH} custom synthesis|{Fmoc-Thr(tBu)-OH} Cancer} Clocapramine shows higher affinity for 5-HT2A than for D2-receptors in vitro.PMID:23546012 Clocapramine shows the lowest potency for D2-occupancy in vivo. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D2 and frontal serotonin-5-HT2 receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT2 versus D2 receptors that fall between these two groups (ED50 of 14.5 mg/kg for D2, 4.9 mg/kg for 5-HT2). . Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. . Sumiyoshi T, et al. Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Neuropsychopharmacology. 1995 Feb;12(1):57-64.|Product information|CAS Number: 47739-98-0|Molecular Weight: 481.07|Formula: C28H37ClN4O|Chemical Name: 1′-(3-{5-chloro-2-azatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-2-yl}propyl)-[1,4′-bipiperidine]-4′-carboxamide|Smiles: NC(=O)C1(CCN(CCCN2C3=CC=CC=C3CCC3=CC=C(Cl)C=C23)CC1)N1CCCCC1|InChiKey: QAZKXHSIKKNOHH-UHFFFAOYSA-N|InChi: InChI=1S/C28H37ClN4O/c29-24-12-11-23-10-9-22-7-2-3-8-25(22)33(26(23)21-24)18-6-15-31-19-13-28(14-20-31,27(30)34)32-16-4-1-5-17-32/h2-3,7-8,11-12,21H,1,4-6,9-10,13-20H2,(H2,30,34)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|