146362-70-1 Usage
Uses
SR 48692 has been used as a neurotensin?high-affinity receptor 1 (NTSR1) antagonist: to explore the function of NTSR1 in glioblastoma (GBM) cells to determine the roles of neurotensin (NT) in the regulation of bile acid?(BA) uptake, in vivo to explore the involvement of NTSR1 versus NTSR2 in mice
Biological Activity
ki: 8.6 nm for ht-29 cellssr 48692 is a nonpeptide neurotensin antagonist.neurotensin is a tridecapeptide and is distributed in both the central and peripheral nervous systems. neurotensin shows a wide spectrum of biological activities resulting in fulfilling a dual function as a neurotransmitter/neuromodulator in the brain and working as a hormone/cellular mediator in peripheral tissues.
Biochem/physiol Actions
SR 48692 is a high affinity, orally bioavailable and selective nonpeptide NT1 neurotensin receptor antagonist that antagonizes neurotensin-induced calcium mobilization with a pA2 of 8.13 in HT-29 human colon carcinoma cell line, and blocks the ability of neurotensin to increase GABA levels in the prefrontal cortex.
in vitro
sr 48692 was found to inhibit the binding of [3h]- or [125i]-neurotensin to membrane preparations from mouse brains and ht-29 cells. in ht-29 cells, sr 48692 also antagonized the neurotensin-induced mobilization of intracellular calcium, which was consistent with previous findings. moreover, in rat cerebellar slices, sr 48692 could block the cyclic gmp level increase in a dose-dependent manner [1].
in vivo
sr 48692 could antagonize the increase in rat brain mesolimbic dopamine turnover which was induced by the systemically active neurotensin peptide ei. whereas, sr 48692 did not antagonize ei-induced decrease in mouse body temperature and spontaneous locomotor activity [1].
references
[1] pugsley ta,akunne hc,whetzel sz,demattos s,corbin ae,wiley jn,wustrow dj,wise ld,heffner tg. differential effects of the nonpeptide neurotensin antagonist, sr 48692, on the pharmacological effects of neurotensin agonists. peptides.1995;16(1):37-44.[2] zerbib f,piche t,charles f,galmiche jp,bruley des varannes s. sr 48692, a specific neurotensin receptor antagonist, has no effect on oesophageal motility in humans. aliment pharmacol ther.2004 apr 15;19(8):931-9.
Check Digit Verification of cas no
The CAS Registry Mumber 146362-70-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,6,3,6 and 2 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 146362-70:
(8*1)+(7*4)+(6*6)+(5*3)+(4*6)+(3*2)+(2*7)+(1*0)=131
131 % 10 = 1
So 146362-70-1 is a valid CAS Registry Number.
InChI:InChI=1/C32H31ClN4O5/c1-41-27-4-3-5-28(42-2)29(27)26-16-24(36-37(26)25-8-9-34-23-15-21(33)6-7-22(23)25)30(38)35-32(31(39)40)19-11-17-10-18(13-19)14-20(32)12-17/h3-9,15-20H,10-14H2,1-2H3,(H,35,38)(H,39,40)
146362-70-1Relevant articles and documents
The synthesis of neurotensin antagonist SR 48692 for prostate cancer research
Baxendale,Cheung,Kitching,Ley,Shearman
, p. 4378 - 4387 (2013/07/27)
An improved synthesis of the molecule SR 48692 is presented and its use as a neurotensin antagonist biological probe for use in cancer research is described. The preparation includes an number of enhanced chemical conversions and strategies to overcome some of the limiting synthetic transformations in the original chemical route.
