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From: Lamont Granquist
Newsgroups: sci.med.psychobiology,sci.med.pharmacy,alt.psychoactives,alt.drugs
Subject: SSRI Neurochemistry
Date: 10 Sep 1994 23:13:54 GMT
Message-ID: <34teji$f6t@news.u.washington.edu>


As mentioned in the original article, these drugs typically have active
metabolites which may be significant.  Thus, actual in vivo activity may
be slightly different.

                     Receptor Affinities for SSRI drugs
              (Values normalized to the IC50 for 5-HT reuptake)
     [Data Taken from: Internatn-Clin-Psychopharm, 9 suppl 1: 19-26 (1994)]


Clomiprimine    Fluoxetine      Sertraline       Paroxetine      Fluvoxamine
                 (Prozac)        (Zoloft)          (Paxil)  
5HTRI:      1  5HTRI:      1  5HTRI:        1  5HTRI:        1  5HTRI:       1
NARI:      14  NARI:      54  DARI:       250  NARI:       280  NARI:      160
H1:        36  5HT2A:    100  NARI:       840  ACh:        720  Alpha2:    500
5HT2A      36  5HT2C:    235  ACh:      5,800  DARI:    18,000  Alpha1:  1,300
Alpha1:    40  Beta:     264  Alpha2:   9,500  D1:      52,000  5HT2C:   1,800
ACh:       45  Alpha2:   410  Alpha1:  15,000  5HT2A:   62,000  H1:      2,900
D1:       130  ACh:      445  D1:      33,000  H1:      66,000  5HT2A:   3,200
D2:       290  H1:       470  5HT2A:   45,000  Alpha1:  66,000  ACh:     8,900
Alpha2: 1,200  DARI:     740  H1:      53,000  5HT2C:   69,000  DARI:   11,000
5HT1A:  1,900  D1:     1,500  Beta:    74,000  Beta:   120,000  D2:     17,000
DARI:   2,900  Alpha1: 2,000  D2:     130,000  D2:     180,000  Beta:   23,000
Beta:  15,000  D2:     4,700  5HT1A: >530,000  Alpha2: 300,000  D1:    >26,000
5HT2C:    NA   5HT1A: 12,000  5HT2C:     NA    5HT1A: >340,000  5HT1A: >26,000

Citalopram

5HTRI:      1
H1:       220
5HT2C:    350
Alpha1:   890
Alpha2: 1,000
ACh:    3,100
5HT2A:  3,100
NARI:   3,400
5HT1A:  8,300
D1:    12,000
D2:    18,000
DARI:  22,000
Beta: >56,000

Radioligands used in binding: 
D1: SCH23390; D2: Spiperone; 5-HT1A: 5-OH-DPAT; 5-HT2A: Ketanserin;
5-HT2C: Ly278584; Alpha1: Prazosin; Alpha2: Idazoxan; Beta: Dihydroalprenolol;
H1: Mepyramine; ACh: QNB.

-- 
Lamont Granquist
"In a saner world his [Noam Chomsky's] tireless efforts to promote justice
 would have long since won him the Nobel Peace Prize, but the committee keeps
 giving it to people like Henry Kissinger."  -- Arthur Naiman