Synonym
Pentiapine maleate; CGS10746B; CGS-10746B; CGS 10746B
IUPAC/Chemical Name
5-(4-methylpiperazin-1-yl)benzo[f]imidazo[2,1-b][1,3,5]thiadiazepine maleate
InChi Key
VVNCUDFIJWCVHI-BTJKTKAUSA-N
InChi Code
InChI=1S/C15H17N5S.C4H4O4/c1-18-8-10-19(11-9-18)14-17-12-4-2-3-5-13(12)21-15-16-6-7-20(14)15;5-3(6)1-2-4(7)8/h2-7H,8-11H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code
CN1CCN(C2=Nc3c(Sc4n2ccn4)cccc3)CC1.OC(/C=C\C(O)=O)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
415.47
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Manzanedo C, Serrano A, Aguilar MA, Rodríguez-Arias M, Miñarro J. Effects of CGS 10746B on hyperactivity and place preference induced by morphine. Behav Brain Res. 2001 Nov 29;126(1-2):23-32. doi: 10.1016/s0166-4328(01)00237-6. PMID: 11704248.
2: French D, Witkin JM. Effects of the dopamine release inhibitor, CGS 10746B, on the locomotor stimulant and discriminative stimulus effects of cocaine and methamphetamine. Pharmacol Biochem Behav. 1993 Dec;46(4):989-93. doi: 10.1016/0091-3057(93)90233-j. PMID: 8309980.
3: Schechter MD, Boja JW. CGS 10746B is able to attenuate the effects of amphetamine: further evidence for dopaminergic mediation. Pharmacol Biochem Behav. 1988 Aug;30(4):1089-92. doi: 10.1016/0091-3057(88)90145-1. PMID: 2906435.
4: Calcagnetti DJ, Schechter MD. Conditioned place aversion following the central administration of a novel dopamine release inhibitor CGS 10746B. Pharmacol Biochem Behav. 1991 Oct;40(2):255-9. doi: 10.1016/0091-3057(91)90548-g. PMID: 1687164.
5: Meehan SM, Schechter MD. Discriminative stimulus properties of CGS 10746B: similarity to dopamine D1 receptor antagonists. Behav Brain Res. 1996 Jan;74(1-2):199-205. doi: 10.1016/0166-4328(95)00167-0. PMID: 8851930.
6: Schechter MD. Cocaine discrimination is attenuated by isradipine and CGS 10746B. Pharmacol Biochem Behav. 1993 Mar;44(3):661-4. doi: 10.1016/0091-3057(93)90183-t. PMID: 8095726.
7: Wood PL, Altar CA, Kim HS. Presynaptic inhibition of nigrostriatal dopamine release in the mouse: lack of cross tolerance between apomorphine, GBL and CGS 10746B. Life Sci. 1988;42(16):1503-6. doi: 10.1016/0024-3205(88)90006-9. PMID: 3352463.
8: Altar CA, Wasley AM, Liebman J, Gerhardt S, Kim H, Welch JJ, Wood PL. CGS 10746B: an atypical antipsychotic candidate that selectively decreases dopamine release at behaviorally effective doses. Life Sci. 1986 Aug 25;39(8):699-705. doi: 10.1016/0024-3205(86)90017-2. PMID: 2874470.
9: Manzanedo C, Aguilar MA, Rodríguez-Arias M, Miñarro J. Sensitization to the rewarding effects of morphine depends on dopamine. Neuroreport. 2005 Feb 8;16(2):201-5. doi: 10.1097/00001756-200502080-00028. PMID: 15671878.
10: Bilsky EJ, Montegut MJ, Nichols ML, Reid LD. CGS 10746B, a novel dopamine release inhibitor, blocks the establishment of cocaine and MDMA conditioned place preferences. Pharmacol Biochem Behav. 1998 Jan;59(1):215-20. doi: 10.1016/s0091-3057(97)00424-3. PMID: 9443558.
