65705-83-1 Usage
Biological Activity
bw 246c is a dp receptor agonist.the prostaglandin d2 (pgd2) receptors, members of g protein-coupled receptors, bind and are activated by prostaglandin d2. pgd2 receptors include the following proteins prostaglandin d2 receptor 1 (dp1) and prostaglandin d2 receptor 2 (dp2).
in vitro
bw 246c was found to be the less active c-8 diastereomer of the dp receptor agonist its analog bw 245c, having 70-fold less activity than that of bw 245c. for bw 245c, a significant species variation was observed in the anti-aggregatory potency so that it was about one hundred times more effective than in the human in the rat. however, the relative potencies of pgi2 and pge1 were found to be similar in both species. moreove, it was observed that in radioligand binding studies bw 245c had a high affinity and selectivity for pgd2 platelet receptors, and the binding to pgi2 or pge2 receptors was not found [1].
in vivo
animal study showed that, an intravenous bolus injection of 250 μg/kg bw 245c to spontaneously hypertensive rats was able to lower both systolic (-23%) and diastolic (-34%) blood pressure [1].
references
[1] town, m. h.,casals-stenzel, j. and schillinger, e. pharmacological and cardiovascular properties of a hydantoin derivative, bw 245 c, with high affinity and selectivity for pgd2 receptors. prostaglandins 25, 13-28 (1983).
Check Digit Verification of cas no
The CAS Registry Mumber 65705-83-1 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,5,7,0 and 5 respectively; the second part has 2 digits, 8 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 65705-83:
(7*6)+(6*5)+(5*7)+(4*0)+(3*5)+(2*8)+(1*3)=141
141 % 10 = 1
So 65705-83-1 is a valid CAS Registry Number.
65705-83-1Relevant articles and documents
Heterocyclic Prostaglandin Analogues. Part 3. The Relationship of Configuration to Biological Activity for Some Hydantoin Prostanglandin Analogues
Brockwell, Michael A.,Caldwell, A. Gordon,Whittaker, Norman,Begley, Michael J.
, p. 706 - 711 (2007/10/02)
The enantiomers of the two diastereomers of 5-(6-carboxyhexyl)-1-(3-cyclohexyl-3-hydroxypropyl)hydantoin have been synthesised.Potent inhibition of platelet aggregation in this series is associated with the configuration corresponding to that in the natural inhibitors, such as prostaglandins E1 and D2.
